Home Cell Cycle CDK inhibitor PD-0332991 (Palbociclib) Isethionate

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PD-0332991 (Palbociclib) Isethionate CDK4/6 inhibitor

Cat.No.S1579

Palbociclib Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.
PD-0332991 (Palbociclib) Isethionate CDK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 573.66

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Quality Control

Batch: Purity: 99.99%
99.99

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H157 Growth Inhibition Assay 0-100 μM 72 h IC50=9 μM 26390342
H2170 Growth Inhibition Assay 0-100 μM 72 h IC50=5 μM 26390342
H520 Growth Inhibition Assay 0-100 μM 72 h IC50=0.73 μM 26390342
H596 Growth Inhibition Assay 0-100 μM 72 h IC50=12 μM 26390342
IMR-32 Growth Inhibition Assay 48 h DMSO IC50=261 nM 26225123
SH-SY5Y Growth Inhibition Assay 48 h DMSO IC50=676 nM 26225123
NGP Growth Inhibition Assay 48 h DMSO IC50=2.077 μM 26225123
SH-EP Growth Inhibition Assay 48 h DMSO IC50=2.211 μM 26225123
IMR-32 Growth Inhibition Assay 1 μM 24 h DMSO induces G1 arrest 26225123
SH-SY5Y Growth Inhibition Assay 1 μM 24 h DMSO induces G1 arrest 26225123
NGP Growth Inhibition Assay 1 μM 24 h DMSO induces G1 arrest 26225123
SH-EP Growth Inhibition Assay 1 μM 24 h DMSO induces G1 arrest 26225123
NGP Fuction Assay 0-1 μM 24 h DMSO reduces the expression of TOP2A, CCNE2, and TK1 in a dose-dependent manner 26225123
IMR-32 Fuction Assay 0-1 μM 24 h DMSO reduces the expression of TOP2A, CCNE2, and TK1 in a dose-dependent manner 26225123
U-CH2 Growth Inhibition Assay 0-1 μM 72 h IC50=50.2 nM 26183925
U-CH3 Growth Inhibition Assay 0-1 μM 72 h IC50=52 nM 26183925
U-CH6 Growth Inhibition Assay 0-1 μM 72 h IC50=90 nM 26183925
U-CH7 Growth Inhibition Assay 0-1 μM 72 h IC50=98 nM 26183925
U-CH11 Growth Inhibition Assay 0-1 μM 72 h IC50=340 nM 26183925
MCF7 Fuction Assay 2.5-250 nM 24 h reduces Rb phosphorylation 25991817
MV4-11 Apoptosis Assay 0.5 μM 24 h enhances apoptosis induced by sorafenib and AC220 25487917
MOLM13 Apoptosis Assay 0.5 μM 24 h enhances apoptosis induced by sorafenib and AC220 25487917
MOLM13-ITD alone Growth Inhibition Assay IC50=0.089 ± 0.009 μM 25487917
MV4-11-ITD alone Growth Inhibition Assay IC50=0.092 ± 0.008 μM 25487917
MOLM13-ITD/D835Y Growth Inhibition Assay IC50=0.114 ± 0.011 μM 25487917
MV4-11-ITD/D835V Growth Inhibition Assay IC50=0.116 ± 0.011 μM 25487917
MV4-11-ITD/D835V Growth Inhibition Assay IC50=0.102 ± 0.006 μM 25487917
MV4-11-ITD/F691L Growth Inhibition Assay IC50=0.112 ± 0.015 μM 25487917
MV4-11-ITD/N841K Growth Inhibition Assay IC50=0.113 ± 0.002 μM 25487917
U937-FLT3 WT Growth Inhibition Assay IC50=0.102 ± 0.013 μM 25487917
P12-ICHIKAWA Growth Inhibition assay IC50 = 0.09604 μM SANGER
697 Growth Inhibition assay IC50 = 0.14838 μM SANGER
NB69 Growth Inhibition assay IC50 = 0.1618 μM SANGER
EoL-1-cell Growth Inhibition assay IC50 = 0.18726 μM SANGER
BHT-101 Growth Inhibition assay IC50 = 0.19825 μM SANGER
SK-NEP-1 Growth Inhibition assay IC50 = 0.22002 μM SANGER
MHH-NB-11 Growth Inhibition assay IC50 = 0.22019 μM SANGER
AsPC-1 Growth Inhibition assay IC50 = 0.25253 μM SANGER
ES1 Growth Inhibition assay IC50 = 0.25625 μM SANGER
LAMA-84 Growth Inhibition assay IC50 = 0.25819 μM SANGER
MOLT-16 Growth Inhibition assay IC50 = 0.25849 μM SANGER
ES7 Growth Inhibition assay IC50 = 0.27309 μM SANGER
KY821 Growth Inhibition assay IC50 = 0.3141 μM SANGER
RT-112 Growth Inhibition assay IC50 = 0.32105 μM SANGER
HL-60 Growth Inhibition assay IC50 = 0.34066 μM SANGER
MOLT-4 Growth Inhibition assay IC50 = 0.34513 μM SANGER
KARPAS-45 Growth Inhibition assay IC50 = 0.37616 μM SANGER
SK-N-AS Growth Inhibition assay IC50 = 0.38783 μM SANGER
CTB-1 Growth Inhibition assay IC50 = 0.40502 μM SANGER
NKM-1 Growth Inhibition assay IC50 = 0.41189 μM SANGER
HTC-C3 Growth Inhibition assay IC50 = 0.43295 μM SANGER
BE-13 Growth Inhibition assay IC50 = 0.44427 μM SANGER
KOSC-2 Growth Inhibition assay IC50 = 0.4669 μM SANGER
NB14 Growth Inhibition assay IC50 = 0.48358 μM SANGER
CAL-27 Growth Inhibition assay IC50 = 0.49459 μM SANGER
H9 Growth Inhibition assay IC50 = 0.49543 μM SANGER
RS4-11 Growth Inhibition assay IC50 = 0.50473 μM SANGER
PA-1 Growth Inhibition assay IC50 = 0.50986 μM SANGER
MV-4-11 Growth Inhibition assay IC50 = 0.51385 μM SANGER
OS-RC-2 Growth Inhibition assay IC50 = 0.52162 μM SANGER
RPMI-8226 Growth Inhibition assay IC50 = 0.52686 μM SANGER
HGC-27 Growth Inhibition assay IC50 = 0.56499 μM SANGER
CHP-212 Growth Inhibition assay IC50 = 0.59359 μM SANGER
NB10 Growth Inhibition assay IC50 = 0.59918 μM SANGER
HH Growth Inhibition assay IC50 = 0.59943 μM SANGER
EW-16 Growth Inhibition assay IC50 = 0.60352 μM SANGER
ES8 Growth Inhibition assay IC50 = 0.60521 μM SANGER
HAL-01 Growth Inhibition assay IC50 = 0.60567 μM SANGER
A204 Growth Inhibition assay IC50 = 0.63391 μM SANGER
MHH-PREB-1 Growth Inhibition assay IC50 = 0.63699 μM SANGER
EM-2 Growth Inhibition assay IC50 = 0.65064 μM SANGER
BV-173 Growth Inhibition assay IC50 = 0.65248 μM SANGER
ONS-76 Growth Inhibition assay IC50 = 0.67782 μM SANGER
KM-H2 Growth Inhibition assay IC50 = 0.69554 μM SANGER
D-263MG Growth Inhibition assay IC50 = 0.71712 μM SANGER
ES3 Growth Inhibition assay IC50 = 0.72893 μM SANGER
VA-ES-BJ Growth Inhibition assay IC50 = 0.73227 μM SANGER
NBsusSR Growth Inhibition assay IC50 = 0.74299 μM SANGER
NCI-H520 Growth Inhibition assay IC50 = 0.74652 μM SANGER
ES5 Growth Inhibition assay IC50 = 0.7528 μM SANGER
T-24 Growth Inhibition assay IC50 = 0.77871 μM SANGER
SW962 Growth Inhibition assay IC50 = 0.80863 μM SANGER
EW-3 Growth Inhibition assay IC50 = 0.80876 μM SANGER
RXF393 Growth Inhibition assay IC50 = 0.81279 μM SANGER
U251 Growth Inhibition assay IC50 = 0.81388 μM SANGER
CAMA-1 Growth Inhibition assay IC50 = 0.83394 μM SANGER
JVM-3 Growth Inhibition assay IC50 = 0.85178 μM SANGER
COLO-800 Growth Inhibition assay IC50 = 0.89778 μM SANGER
OVCAR-5 Growth Inhibition assay IC50 = 0.9001 μM SANGER
LB1047-RCC Growth Inhibition assay IC50 = 0.92756 μM SANGER
SW954 Growth Inhibition assay IC50 = 0.92941 μM SANGER
J-RT3-T3-5 Growth Inhibition assay IC50 = 0.93606 μM SANGER
Mewo Growth Inhibition assay IC50 = 0.9366 μM SANGER
NCI-H1770 Growth Inhibition assay IC50 = 0.94055 μM SANGER
HO-1-N-1 Growth Inhibition assay IC50 = 0.96281 μM SANGER
HSC-3 Growth Inhibition assay IC50 = 0.96648 μM SANGER
TYK-nu Growth Inhibition assay IC50 = 0.99825 μM SANGER
KYSE-150 Growth Inhibition assay IC50 = 1.00076 μM SANGER
SN12C Growth Inhibition assay IC50 = 1.00875 μM SANGER
MOLT-13 Growth Inhibition assay IC50 = 1.01421 μM SANGER
TE-11 Growth Inhibition assay IC50 = 1.04812 μM SANGER
DB Growth Inhibition assay IC50 = 1.07273 μM SANGER
CAL-39 Growth Inhibition assay IC50 = 1.07522 μM SANGER
A3-KAW Growth Inhibition assay IC50 = 1.08408 μM SANGER
CHP-134 Growth Inhibition assay IC50 = 1.11807 μM SANGER
TGW Growth Inhibition assay IC50 = 1.12395 μM SANGER
QIMR-WIL Growth Inhibition assay IC50 = 1.13134 μM SANGER
NCI-SNU-1 Growth Inhibition assay IC50 = 1.16354 μM SANGER
CGTH-W-1 Growth Inhibition assay IC50 = 1.17186 μM SANGER
MHH-ES-1 Growth Inhibition assay IC50 = 1.17986 μM SANGER
LB2241-RCC Growth Inhibition assay IC50 = 1.1862 μM SANGER
ML-2 Growth Inhibition assay IC50 = 1.20734 μM SANGER
COR-L23 Growth Inhibition assay IC50 = 1.22933 μM SANGER
BFTC-905 Growth Inhibition assay IC50 = 1.24267 μM SANGER
Hs-578-T Growth Inhibition assay IC50 = 1.25817 μM SANGER
KG-1 Growth Inhibition assay IC50 = 1.26686 μM SANGER
HEL Growth Inhibition assay IC50 = 1.29338 μM SANGER
A549 Growth Inhibition assay IC50 = 1.29399 μM SANGER
COLO-741 Growth Inhibition assay IC50 = 1.32089 μM SANGER
PC-3 Growth Inhibition assay IC50 = 1.35221 μM SANGER
HOS Growth Inhibition assay IC50 = 1.35296 μM SANGER
HT-1080 Growth Inhibition assay IC50 = 1.37519 μM SANGER
TE-8 Growth Inhibition assay IC50 = 1.41774 μM SANGER
BHY Growth Inhibition assay IC50 = 1.46923 μM SANGER
BB65-RCC Growth Inhibition assay IC50 = 1.50528 μM SANGER
HN Growth Inhibition assay IC50 = 1.54071 μM SANGER
NCI-H441 Growth Inhibition assay IC50 = 1.54907 μM SANGER
RPMI-8866 Growth Inhibition assay IC50 = 1.58507 μM SANGER
CAL-62 Growth Inhibition assay IC50 = 1.60862 μM SANGER
MG-63 Growth Inhibition assay IC50 = 1.61813 μM SANGER
SK-LU-1 Growth Inhibition assay IC50 = 1.62152 μM SANGER
BCPAP Growth Inhibition assay IC50 = 1.66457 μM SANGER
22RV1 Growth Inhibition assay IC50 = 1.67843 μM SANGER
T47D Growth Inhibition assay IC50 = 1.68061 μM SANGER
MSTO-211H Growth Inhibition assay IC50 = 1.69603 μM SANGER
DEL Growth Inhibition assay IC50 = 1.70273 μM SANGER
H4 Growth Inhibition assay IC50 = 1.73212 μM SANGER
CAL-51 Growth Inhibition assay IC50 = 1.74855 μM SANGER
ABC-1 Growth Inhibition assay IC50 = 1.78582 μM SANGER
MZ2-MEL Growth Inhibition assay IC50 = 1.79542 μM SANGER
YKG-1 Growth Inhibition assay IC50 = 1.81061 μM SANGER
KM12 Growth Inhibition assay IC50 = 1.81602 μM SANGER
L-363 Growth Inhibition assay IC50 = 1.87412 μM SANGER
KU812 Growth Inhibition assay IC50 = 1.89282 μM SANGER
LOXIMVI Growth Inhibition assay IC50 = 1.91228 μM SANGER
G-401 Growth Inhibition assay IC50 = 1.92428 μM SANGER
SW780 Growth Inhibition assay IC50 = 1.96246 μM SANGER
SW872 Growth Inhibition assay IC50 = 1.9833 μM SANGER
NB7 Growth Inhibition assay IC50 = 1.99323 μM SANGER
T98G Growth Inhibition assay IC50 = 2.00666 μM SANGER
SW1710 Growth Inhibition assay IC50 = 2.06945 μM SANGER
NCI-H1573 Growth Inhibition assay IC50 = 2.07298 μM SANGER
KE-37 Growth Inhibition assay IC50 = 2.08951 μM SANGER
786-0 Growth Inhibition assay IC50 = 2.15439 μM SANGER
SAS Growth Inhibition assay IC50 = 2.20374 μM SANGER
CAL-54 Growth Inhibition assay IC50 = 2.20413 μM SANGER
SF268 Growth Inhibition assay IC50 = 2.23122 μM SANGER
SW620 Growth Inhibition assay IC50 = 2.26169 μM SANGER
MN-60 Growth Inhibition assay IC50 = 2.3106 μM SANGER
EFO-27 Growth Inhibition assay IC50 = 2.32058 μM SANGER
NCI-H747 Growth Inhibition assay IC50 = 2.32199 μM SANGER
HCC2218 Growth Inhibition assay IC50 = 2.35374 μM SANGER
MIA-PaCa-2 Growth Inhibition assay IC50 = 2.36437 μM SANGER
SJSA-1 Growth Inhibition assay IC50 = 2.37796 μM SANGER
RKO Growth Inhibition assay IC50 = 2.38496 μM SANGER
NB6 Growth Inhibition assay IC50 = 2.40374 μM SANGER
ES4 Growth Inhibition assay IC50 = 2.45422 μM SANGER
EGI-1 Growth Inhibition assay IC50 = 2.46883 μM SANGER
CTV-1 Growth Inhibition assay IC50 = 2.52773 μM SANGER
NCI-H1355 Growth Inhibition assay IC50 = 2.55951 μM SANGER
GT3TKB Growth Inhibition assay IC50 = 2.59199 μM SANGER
SK-HEP-1 Growth Inhibition assay IC50 = 2.59266 μM SANGER
GAMG Growth Inhibition assay IC50 = 2.59394 μM SANGER
SK-MES-1 Growth Inhibition assay IC50 = 2.61803 μM SANGER
RO82-W-1 Growth Inhibition assay IC50 = 2.62057 μM SANGER
ECC10 Growth Inhibition assay IC50 = 2.70206 μM SANGER
MCF7 Growth Inhibition assay IC50 = 2.71464 μM SANGER
D-283MED Growth Inhibition assay IC50 = 2.7243 μM SANGER
RPMI-7951 Growth Inhibition assay IC50 = 2.75694 μM SANGER
Ramos-2G6-4C10 Growth Inhibition assay IC50 = 2.77099 μM SANGER
KGN Growth Inhibition assay IC50 = 2.81884 μM SANGER
NUGC-3 Growth Inhibition assay IC50 = 2.82505 μM SANGER
NCI-H292 Growth Inhibition assay IC50 = 2.85053 μM SANGER
Becker Growth Inhibition assay IC50 = 2.95832 μM SANGER
NCI-H1299 Growth Inhibition assay IC50 = 3.05263 μM SANGER
ETK-1 Growth Inhibition assay IC50 = 3.0543 μM SANGER
TK10 Growth Inhibition assay IC50 = 3.20165 μM SANGER
VMRC-RCZ Growth Inhibition assay IC50 = 3.36488 μM SANGER
YH-13 Growth Inhibition assay IC50 = 3.44079 μM SANGER
DU-145 Growth Inhibition assay IC50 = 3.46269 μM SANGER
SW1088 Growth Inhibition assay IC50 = 3.4747 μM SANGER
HOP-92 Growth Inhibition assay IC50 = 3.50342 μM SANGER
KP-N-YS Growth Inhibition assay IC50 = 3.62139 μM SANGER
NCI-H460 Growth Inhibition assay IC50 = 3.6673 μM SANGER
U-2-OS Growth Inhibition assay IC50 = 3.72535 μM SANGER
A101D Growth Inhibition assay IC50 = 3.76936 μM SANGER
MDA-MB-231 Growth Inhibition assay IC50 = 3.81951 μM SANGER
IST-MES1 Growth Inhibition assay IC50 = 3.832 μM SANGER
COR-L105 Growth Inhibition assay IC50 = 4.018 μM SANGER
NCI-H1437 Growth Inhibition assay IC50 = 4.02302 μM SANGER
CAL-85-1 Growth Inhibition assay IC50 = 4.02461 μM SANGER
MZ1-PC Growth Inhibition assay IC50 = 4.18556 μM SANGER
VM-CUB-1 Growth Inhibition assay IC50 = 4.31284 μM SANGER
CHL-1 Growth Inhibition assay IC50 = 4.32169 μM SANGER
MDA-MB-361 Growth Inhibition assay IC50 = 4.33153 μM SANGER
NCI-H661 Growth Inhibition assay IC50 = 4.50092 μM SANGER
EW-11 Growth Inhibition assay IC50 = 4.52231 μM SANGER
BEN Growth Inhibition assay IC50 = 4.52815 μM SANGER
BFTC-909 Growth Inhibition assay IC50 = 4.56275 μM SANGER
NCI-H2087 Growth Inhibition assay IC50 = 4.58164 μM SANGER
RVH-421 Growth Inhibition assay IC50 = 4.6669 μM SANGER
P30-OHK Growth Inhibition assay IC50 = 4.68008 μM SANGER
NCI-H28 Growth Inhibition assay IC50 = 4.81661 μM SANGER
ES6 Growth Inhibition assay IC50 = 4.83016 μM SANGER
769-P Growth Inhibition assay IC50 = 4.85926 μM SANGER
OE33 Growth Inhibition assay IC50 = 4.88161 μM SANGER
SW982 Growth Inhibition assay IC50 = 4.95061 μM SANGER
A388 Growth Inhibition assay IC50 = 5.02983 μM SANGER
TI-73 Growth Inhibition assay IC50 = 5.06194 μM SANGER
HCT-116 Growth Inhibition assay IC50 = 5.09889 μM SANGER
HuP-T3 Growth Inhibition assay IC50 = 5.18709 μM SANGER
G-402 Growth Inhibition assay IC50 = 5.19416 μM SANGER
NCI-H1792 Growth Inhibition assay IC50 = 5.24622 μM SANGER
NCI-H209 Growth Inhibition assay IC50 = 5.25942 μM SANGER
NCI-H1650 Growth Inhibition assay IC50 = 5.30634 μM SANGER
LCLC-97TM1 Growth Inhibition assay IC50 = 5.31808 μM SANGER
S-117 Growth Inhibition assay IC50 = 5.36976 μM SANGER
GI-ME-N Growth Inhibition assay IC50 = 5.39681 μM SANGER
NCI-H2122 Growth Inhibition assay IC50 = 5.49397 μM SANGER
NCI-H1793 Growth Inhibition assay IC50 = 5.67593 μM SANGER
C2BBe1 Growth Inhibition assay IC50 = 5.70088 μM SANGER
TE-12 Growth Inhibition assay IC50 = 5.80556 μM SANGER
LCLC-103H Growth Inhibition assay IC50 = 5.917 μM SANGER
A673 Growth Inhibition assay IC50 = 5.91932 μM SANGER
BB30-HNC Growth Inhibition assay IC50 = 5.9836 μM SANGER
SF295 Growth Inhibition assay IC50 = 6.00422 μM SANGER
KU-19-19 Growth Inhibition assay IC50 = 6.01731 μM SANGER
CFPAC-1 Growth Inhibition assay IC50 = 6.04443 μM SANGER
LoVo Growth Inhibition assay IC50 = 6.05063 μM SANGER
8505C Growth Inhibition assay IC50 = 6.07573 μM SANGER
GMS-10 Growth Inhibition assay IC50 = 6.15002 μM SANGER
Ca9-22 Growth Inhibition assay IC50 = 6.1671 μM SANGER
DOK Growth Inhibition assay IC50 = 6.22072 μM SANGER
FADU Growth Inhibition assay IC50 = 6.26039 μM SANGER
BxPC-3 Growth Inhibition assay IC50 = 6.2732 μM SANGER
CAL-33 Growth Inhibition assay IC50 = 6.29201 μM SANGER
SHP-77 Growth Inhibition assay IC50 = 6.31512 μM SANGER
LXF-289 Growth Inhibition assay IC50 = 6.33455 μM SANGER
GB-1 Growth Inhibition assay IC50 = 6.382 μM SANGER
KS-1 Growth Inhibition assay IC50 = 6.38447 μM SANGER
D-502MG Growth Inhibition assay IC50 = 6.42376 μM SANGER
LAN-6 Growth Inhibition assay IC50 = 6.51023 μM SANGER
H-EMC-SS Growth Inhibition assay IC50 = 6.56147 μM SANGER
LC-2-ad Growth Inhibition assay IC50 = 6.60076 μM SANGER
NCI-H1693 Growth Inhibition assay IC50 = 6.62215 μM SANGER
SK-N-FI Growth Inhibition assay IC50 = 6.75044 μM SANGER
D-423MG Growth Inhibition assay IC50 = 6.76117 μM SANGER
KNS-42 Growth Inhibition assay IC50 = 6.78197 μM SANGER
GCT Growth Inhibition assay IC50 = 6.938 μM SANGER
DSH1 Growth Inhibition assay IC50 = 7.0633 μM SANGER
D-247MG Growth Inhibition assay IC50 = 7.07881 μM SANGER
NCI-SNU-5 Growth Inhibition assay IC50 = 7.18371 μM SANGER
TE-6 Growth Inhibition assay IC50 = 7.20601 μM SANGER
NOMO-1 Growth Inhibition assay IC50 = 7.22127 μM SANGER
NB17 Growth Inhibition assay IC50 = 7.30309 μM SANGER
EW-22 Growth Inhibition assay IC50 = 7.34348 μM SANGER
EW-13 Growth Inhibition assay IC50 = 7.35162 μM SANGER
DOHH-2 Growth Inhibition assay IC50 = 7.4402 μM SANGER
TGBC1TKB Growth Inhibition assay IC50 = 7.49899 μM SANGER
GR-ST Growth Inhibition assay IC50 = 7.52594 μM SANGER
KYSE-520 Growth Inhibition assay IC50 = 7.55515 μM SANGER
CAPAN-1 Growth Inhibition assay IC50 = 7.5951 μM SANGER
HCE-4 Growth Inhibition assay IC50 = 7.62279 μM SANGER
MLMA Growth Inhibition assay IC50 = 7.62957 μM SANGER
HT-144 Growth Inhibition assay IC50 = 7.65368 μM SANGER
KYSE-180 Growth Inhibition assay IC50 = 7.71169 μM SANGER
TE-5 Growth Inhibition assay IC50 = 7.95971 μM SANGER
IGROV-1 Growth Inhibition assay IC50 = 7.98551 μM SANGER
NCI-H1581 Growth Inhibition assay IC50 = 8.012 μM SANGER
SW1990 Growth Inhibition assay IC50 = 8.04659 μM SANGER
EFM-19 Growth Inhibition assay IC50 = 8.08545 μM SANGER
IGR-1 Growth Inhibition assay IC50 = 8.43023 μM SANGER
U-118-MG Growth Inhibition assay IC50 = 8.43463 μM SANGER
SK-OV-3 Growth Inhibition assay IC50 = 8.46765 μM SANGER
KNS-62 Growth Inhibition assay IC50 = 8.51761 μM SANGER
GOTO Growth Inhibition assay IC50 = 8.57635 μM SANGER
8305C Growth Inhibition assay IC50 = 8.70484 μM SANGER
RPMI-2650 Growth Inhibition assay IC50 = 8.71955 μM SANGER
NEC8 Growth Inhibition assay IC50 = 8.74307 μM SANGER
KYSE-450 Growth Inhibition assay IC50 = 8.86548 μM SANGER
RMG-I Growth Inhibition assay IC50 = 9.14058 μM SANGER
CAKI-1 Growth Inhibition assay IC50 = 9.31979 μM SANGER
KYSE-510 Growth Inhibition assay IC50 = 9.35778 μM SANGER
A4-Fuk Growth Inhibition assay IC50 = 9.36701 μM SANGER
AN3-CA Growth Inhibition assay IC50 = 9.45444 μM SANGER
SK-N-DZ Growth Inhibition assay IC50 = 9.72849 μM SANGER
HSC-2 Growth Inhibition assay IC50 = 9.76629 μM SANGER
EW-1 Growth Inhibition assay IC50 = 9.79369 μM SANGER
D-566MG Growth Inhibition assay IC50 = 9.83664 μM SANGER
COLO-792 Growth Inhibition assay IC50 = 9.98746 μM SANGER
TE-10 Growth Inhibition assay IC50 = 10.0396 μM SANGER
NCI-H650 Growth Inhibition assay IC50 = 10.4286 μM SANGER
U-266 Growth Inhibition assay IC50 = 10.455 μM SANGER
Detroit562 Growth Inhibition assay IC50 = 11.0515 μM SANGER
NH-12 Growth Inhibition assay IC50 = 11.1446 μM SANGER
OC-314 Growth Inhibition assay IC50 = 11.2842 μM SANGER
IST-MEL1 Growth Inhibition assay IC50 = 11.5323 μM SANGER
KNS-81-FD Growth Inhibition assay IC50 = 11.5527 μM SANGER
SW1463 Growth Inhibition assay IC50 = 11.5989 μM SANGER
NCI-H23 Growth Inhibition assay IC50 = 11.6553 μM SANGER
SK-MEL-2 Growth Inhibition assay IC50 = 11.7197 μM SANGER
NB13 Growth Inhibition assay IC50 = 12.1495 μM SANGER
Daoy Growth Inhibition assay IC50 = 12.2855 μM SANGER
NCI-H1623 Growth Inhibition assay IC50 = 12.3801 μM SANGER
NMC-G1 Growth Inhibition assay IC50 = 12.717 μM SANGER
DK-MG Growth Inhibition assay IC50 = 12.9482 μM SANGER
TCCSUP Growth Inhibition assay IC50 = 13.1284 μM SANGER
SCC-15 Growth Inhibition assay IC50 = 13.2651 μM SANGER
NOS-1 Growth Inhibition assay IC50 = 13.2893 μM SANGER
RH-1 Growth Inhibition assay IC50 = 13.3037 μM SANGER
SK-MEL-3 Growth Inhibition assay IC50 = 13.3728 μM SANGER
NB5 Growth Inhibition assay IC50 = 13.4067 μM SANGER
SNU-387 Growth Inhibition assay IC50 = 13.5072 μM SANGER
CAL-120 Growth Inhibition assay IC50 = 13.6718 μM SANGER
LNCaP-Clone-FGC Growth Inhibition assay IC50 = 13.7991 μM SANGER
ACN Growth Inhibition assay IC50 = 14.0288 μM SANGER
SK-MEL-30 Growth Inhibition assay IC50 = 14.063 μM SANGER
COLO-678 Growth Inhibition assay IC50 = 14.0822 μM SANGER
SCC-9 Growth Inhibition assay IC50 = 14.1021 μM SANGER
KINGS-1 Growth Inhibition assay IC50 = 14.1402 μM SANGER
LS-513 Growth Inhibition assay IC50 = 14.187 μM SANGER
HLE Growth Inhibition assay IC50 = 14.3852 μM SANGER
SW1573 Growth Inhibition assay IC50 = 14.4435 μM SANGER
KYSE-140 Growth Inhibition assay IC50 = 14.6327 μM SANGER
SK-PN-DW Growth Inhibition assay IC50 = 14.8001 μM SANGER
A253 Growth Inhibition assay IC50 = 15.0625 μM SANGER
CAL-12T Growth Inhibition assay IC50 = 15.4662 μM SANGER
COLO-679 Growth Inhibition assay IC50 = 15.7683 μM SANGER
UACC-257 Growth Inhibition assay IC50 = 16.1201 μM SANGER
U-87-MG Growth Inhibition assay IC50 = 16.3523 μM SANGER
HCC1806 Growth Inhibition assay IC50 = 16.7071 μM SANGER
NCI-H2170 Growth Inhibition assay IC50 = 17.2448 μM SANGER
AGS Growth Inhibition assay IC50 = 17.3808 μM SANGER
MEL-HO Growth Inhibition assay IC50 = 17.7503 μM SANGER
SW48 Growth Inhibition assay IC50 = 17.7716 μM SANGER
HuP-T4 Growth Inhibition assay IC50 = 18.0206 μM SANGER
NCI-H720 Growth Inhibition assay IC50 = 18.1402 μM SANGER
RCC10RGB Growth Inhibition assay IC50 = 18.1697 μM SANGER
HD-MY-Z Growth Inhibition assay IC50 = 18.2254 μM SANGER
A427 Growth Inhibition assay IC50 = 18.5094 μM SANGER
HCC2998 Growth Inhibition assay IC50 = 18.6051 μM SANGER
EPLC-272H Growth Inhibition assay IC50 = 19.0434 μM SANGER
C32 Growth Inhibition assay IC50 = 19.045 μM SANGER
UMC-11 Growth Inhibition assay IC50 = 19.2123 μM SANGER
CaR-1 Growth Inhibition assay IC50 = 19.6804 μM SANGER
KYSE-410 Growth Inhibition assay IC50 = 19.9139 μM SANGER
HuCCT1 Growth Inhibition assay IC50 = 20.6293 μM SANGER
LB996-RCC Growth Inhibition assay IC50 = 20.7168 μM SANGER
KYSE-70 Growth Inhibition assay IC50 = 20.8059 μM SANGER
CAL-72 Growth Inhibition assay IC50 = 20.915 μM SANGER
Capan-2 Growth Inhibition assay IC50 = 21.0413 μM SANGER
PANC-08-13 Growth Inhibition assay IC50 = 21.2515 μM SANGER
SBC-1 Growth Inhibition assay IC50 = 21.3081 μM SANGER
MFM-223 Growth Inhibition assay IC50 = 21.3342 μM SANGER
BB49-HNC Growth Inhibition assay IC50 = 21.5716 μM SANGER
SH-4 Growth Inhibition assay IC50 = 21.6618 μM SANGER
HuO9 Growth Inhibition assay IC50 = 21.9825 μM SANGER
AM-38 Growth Inhibition assay IC50 = 22.0485 μM SANGER
A431 Growth Inhibition assay IC50 = 23.2119 μM SANGER
YAPC Growth Inhibition assay IC50 = 23.2651 μM SANGER
LU-139 Growth Inhibition assay IC50 = 23.4809 μM SANGER
HEC-1 Growth Inhibition assay IC50 = 23.4937 μM SANGER
SCC-25 Growth Inhibition assay IC50 = 24.3006 μM SANGER
HT-29 Growth Inhibition assay IC50 = 24.3823 μM SANGER
PC-14 Growth Inhibition assay IC50 = 24.6571 μM SANGER
Calu-6 Growth Inhibition assay IC50 = 25.5071 μM SANGER
SJRH30 Growth Inhibition assay IC50 = 25.6496 μM SANGER
ChaGo-K-1 Growth Inhibition assay IC50 = 26.1629 μM SANGER
IA-LM Growth Inhibition assay IC50 = 26.3645 μM SANGER
GP5d Growth Inhibition assay IC50 = 26.4491 μM SANGER
NCI-H2291 Growth Inhibition assay IC50 = 26.6541 μM SANGER
BALL-1 Growth Inhibition assay IC50 = 26.9397 μM SANGER
HCC1954 Growth Inhibition assay IC50 = 26.9808 μM SANGER
NCI-H2452 Growth Inhibition assay IC50 = 27.4163 μM SANGER
LU-99A Growth Inhibition assay IC50 = 27.5582 μM SANGER
NTERA-S-cl-D1 Growth Inhibition assay IC50 = 27.7299 μM SANGER
PANC-10-05 Growth Inhibition assay IC50 = 27.7775 μM SANGER
NCI-H2405 Growth Inhibition assay IC50 = 27.9387 μM SANGER
MDA-MB-415 Growth Inhibition assay IC50 = 28.4137 μM SANGER
NCI-H2342 Growth Inhibition assay IC50 = 28.5281 μM SANGER
TGBC24TKB Growth Inhibition assay IC50 = 28.7117 μM SANGER
LU-134-A Growth Inhibition assay IC50 = 28.9261 μM SANGER
SCC-4 Growth Inhibition assay IC50 = 31.0495 μM SANGER
Saos-2 Growth Inhibition assay IC50 = 31.9306 μM SANGER
RERF-LC-MS Growth Inhibition assay IC50 = 32.8231 μM SANGER
M14 Growth Inhibition assay IC50 = 32.9764 μM SANGER
HPAF-II Growth Inhibition assay IC50 = 33.5011 μM SANGER
NCI-H1755 Growth Inhibition assay IC50 = 34.3305 μM SANGER
D-392MG Growth Inhibition assay IC50 = 35.8674 μM SANGER
A704 Growth Inhibition assay IC50 = 36.0427 μM SANGER
CP50-MEL-B Growth Inhibition assay IC50 = 36.1911 μM SANGER
EW-18 Growth Inhibition assay IC50 = 36.452 μM SANGER
WM-115 Growth Inhibition assay IC50 = 36.8099 μM SANGER
LU-65 Growth Inhibition assay IC50 = 37.1417 μM SANGER
NCI-H1563 Growth Inhibition assay IC50 = 37.2484 μM SANGER
DBTRG-05MG Growth Inhibition assay IC50 = 38.0691 μM SANGER
NCI-H630 Growth Inhibition assay IC50 = 38.4714 μM SANGER
NCI-H1155 Growth Inhibition assay IC50 = 39.242 μM SANGER
OVCAR-3 Growth Inhibition assay IC50 = 39.9195 μM SANGER
OAW-42 Growth Inhibition assay IC50 = 40.4258 μM SANGER
JVM-2 Growth Inhibition assay IC50 = 41.2415 μM SANGER
C3A Growth Inhibition assay IC50 = 41.3447 μM SANGER
HT55 Growth Inhibition assay IC50 = 42.2841 μM SANGER
OVCAR-4 Growth Inhibition assay IC50 = 42.2974 μM SANGER
MEG-01 Growth Inhibition assay IC50 = 42.4616 μM SANGER
NCI-H82 Growth Inhibition assay IC50 = 43.9892 μM SANGER
JEG-3 Growth Inhibition assay IC50 = 44.947 μM SANGER
BPH-1 Growth Inhibition assay IC50 = 46.3998 μM SANGER
MPP-89 Growth Inhibition assay IC50 = 47.2898 μM SANGER
ALL-PO Growth Inhibition assay IC50 = 47.4188 μM SANGER
HT Growth Inhibition assay IC50 = 47.492 μM SANGER
NCI-H2347 Growth Inhibition assay IC50 = 48.0715 μM SANGER
A2780 Growth Inhibition assay IC50 = 49.4228 μM SANGER
KARPAS-299 Growth Inhibition assay IC50 = 49.5119 μM SANGER
NCI-H1651 Growth Inhibition assay IC50 = 49.8821 μM SANGER
OCI-AML2 Growth Inhibition assay IC50 = 50.2084 μM SANGER
OCUB-M Growth Inhibition assay IC50 = 50.3047 μM SANGER
HuH-7 Growth Inhibition assay IC50 = 50.5943 μM SANGER
RCM-1 Growth Inhibition assay IC50 = 50.9133 μM SANGER
FTC-133 Growth Inhibition assay IC50 = 51.322 μM SANGER
PSN1 Growth Inhibition assay IC50 = 51.4335 μM SANGER
A498 Growth Inhibition assay IC50 = 52.0995 μM SANGER
SF126 Growth Inhibition assay IC50 = 52.6568 μM SANGER
UACC-62 Growth Inhibition assay IC50 = 55.2224 μM SANGER
PANC-03-27 Growth Inhibition assay IC50 = 56.6788 μM SANGER
NCI-H727 Growth Inhibition assay IC50 = 56.8127 μM SANGER
SNU-423 Growth Inhibition assay IC50 = 57.2859 μM SANGER
LB771-HNC Growth Inhibition assay IC50 = 57.8405 μM SANGER
HCC1395 Growth Inhibition assay IC50 = 58.0464 μM SANGER
OAW-28 Growth Inhibition assay IC50 = 58.2785 μM SANGER
NB12 Growth Inhibition assay IC50 = 60.6696 μM SANGER
DJM-1 Growth Inhibition assay IC50 = 60.7331 μM SANGER
MDA-MB-157 Growth Inhibition assay IC50 = 61.1649 μM SANGER
DU-4475 Growth Inhibition assay IC50 = 62.5495 μM SANGER
RD Growth Inhibition assay IC50 = 62.7387 μM SANGER
LS-123 Growth Inhibition assay IC50 = 63.2618 μM SANGER
NCI-H226 Growth Inhibition assay IC50 = 64.22 μM SANGER
MS-1 Growth Inhibition assay IC50 = 64.8358 μM SANGER
no-10 Growth Inhibition assay IC50 = 65.7473 μM SANGER
SW626 Growth Inhibition assay IC50 = 65.7579 μM SANGER
DMS-273 Growth Inhibition assay IC50 = 66.2296 μM SANGER
ESS-1 Growth Inhibition assay IC50 = 66.5096 μM SANGER
TE-9 Growth Inhibition assay IC50 = 66.6316 μM SANGER
CAS-1 Growth Inhibition assay IC50 = 67.7954 μM SANGER
639-V Growth Inhibition assay IC50 = 69.4198 μM SANGER
GAK Growth Inhibition assay IC50 = 70.2031 μM SANGER
NCI-H526 Growth Inhibition assay IC50 = 71.0913 μM SANGER
DoTc2-4510 Growth Inhibition assay IC50 = 71.443 μM SANGER
647-V Growth Inhibition assay IC50 = 73.2118 μM SANGER
OVCAR-8 Growth Inhibition assay IC50 = 73.2367 μM SANGER
COLO-680N Growth Inhibition assay IC50 = 75.2497 μM SANGER
HDLM-2 Growth Inhibition assay IC50 = 75.7806 μM SANGER
TGBC11TKB Growth Inhibition assay IC50 = 79.0192 μM SANGER
DMS-114 Growth Inhibition assay IC50 = 81.9577 μM SANGER
CW-2 Growth Inhibition assay IC50 = 82.6818 μM SANGER
MDA-MB-175-VII Growth Inhibition assay IC50 = 85.3135 μM SANGER
HT-1376 Growth Inhibition assay IC50 = 85.846 μM SANGER
SW1417 Growth Inhibition assay IC50 = 88.2906 μM SANGER
HCE-T Growth Inhibition assay IC50 = 91.7205 μM SANGER
OE19 Growth Inhibition assay IC50 = 92.7944 μM SANGER
NCI-N87 Growth Inhibition assay IC50 = 92.8881 μM SANGER
SNU-449 Growth Inhibition assay IC50 = 93.584 μM SANGER
NCI-H1092 Growth Inhibition assay IC50 = 96.5851 μM SANGER
COLO-684 Growth Inhibition assay IC50 = 99.0686 μM SANGER
HCC1937 Growth Inhibition assay IC50 = 99.9315 μM SANGER
EFO-21 Growth Inhibition assay IC50 = 110.988 μM SANGER
ZR-75-30 Growth Inhibition assay IC50 = 114.117 μM SANGER
HCC1187 Growth Inhibition assay IC50 = 114.179 μM SANGER
SW684 Growth Inhibition assay IC50 = 114.655 μM SANGER
AU565 Growth Inhibition assay IC50 = 115.892 μM SANGER
HCC38 Growth Inhibition assay IC50 = 116.559 μM SANGER
LK-2 Growth Inhibition assay IC50 = 119.652 μM SANGER
LB2518-MEL Growth Inhibition assay IC50 = 122.428 μM SANGER
COLO-320-HSR Growth Inhibition assay IC50 = 126.212 μM SANGER
HCC1419 Growth Inhibition assay IC50 = 129.227 μM SANGER
NCI-H2228 Growth Inhibition assay IC50 = 129.321 μM SANGER
NCI-H2052 Growth Inhibition assay IC50 = 130.358 μM SANGER
HCC2157 Growth Inhibition assay IC50 = 133.973 μM SANGER
HCC1569 Growth Inhibition assay IC50 = 135.05 μM SANGER
HuO-3N1 Growth Inhibition assay IC50 = 135.366 μM SANGER
MZ7-mel Growth Inhibition assay IC50 = 145.604 μM SANGER
SW756 Growth Inhibition assay IC50 = 147.143 μM SANGER
NCI-H1304 Growth Inhibition assay IC50 = 149.222 μM SANGER
LN-405 Growth Inhibition assay IC50 = 149.732 μM SANGER
BT-474 Growth Inhibition assay IC50 = 150.969 μM SANGER
LS-411N Growth Inhibition assay IC50 = 152.319 μM SANGER
ATN-1 Growth Inhibition assay IC50 = 152.458 μM SANGER
SNU-C2B Growth Inhibition assay IC50 = 153.444 μM SANGER
KYSE-270 Growth Inhibition assay IC50 = 155.75 μM SANGER
NCI-H1395 Growth Inhibition assay IC50 = 156.493 μM SANGER
EKVX Growth Inhibition assay IC50 = 156.981 μM SANGER
HCC70 Growth Inhibition assay IC50 = 157.989 μM SANGER
NCI-H522 Growth Inhibition assay IC50 = 161.368 μM SANGER
Ca-Ski Growth Inhibition assay IC50 = 161.86 μM SANGER
SW1116 Growth Inhibition assay IC50 = 163.382 μM SANGER
8-MG-BA Growth Inhibition assay IC50 = 165.797 μM SANGER
NCI-H1048 Growth Inhibition assay IC50 = 172.374 μM SANGER
RH-18 Growth Inhibition assay IC50 = 172.601 μM SANGER
LU-135 Growth Inhibition assay IC50 = 173.259 μM SANGER
SW948 Growth Inhibition assay IC50 = 174.6 μM SANGER
LS-1034 Growth Inhibition assay IC50 = 183.742 μM SANGER
SCH Growth Inhibition assay IC50 = 187.022 μM SANGER
KP-N-YN Growth Inhibition assay IC50 = 192.971 μM SANGER
NCI-H69 Growth Inhibition assay IC50 = 210.925 μM SANGER
SBC-5 Growth Inhibition assay IC50 = 211.162 μM SANGER
MFE-280 Growth Inhibition assay IC50 = 212.067 μM SANGER
MC116 Growth Inhibition assay IC50 = 212.736 μM SANGER
BT-20 Growth Inhibition assay IC50 = 216.38 μM SANGER
NCI-H1993 Growth Inhibition assay IC50 = 217.295 μM SANGER
Calu-3 Growth Inhibition assay IC50 = 217.37 μM SANGER
GCIY Growth Inhibition assay IC50 = 221.332 μM SANGER
HT-3 Growth Inhibition assay IC50 = 222.173 μM SANGER
MC-IXC Growth Inhibition assay IC50 = 227.215 μM SANGER
COR-L88 Growth Inhibition assay IC50 = 234.259 μM SANGER
SK-MEL-1 Growth Inhibition assay IC50 = 235.59 μM SANGER
MDA-MB-453 Growth Inhibition assay IC50 = 236.33 μM SANGER
SiHa Growth Inhibition assay IC50 = 247.22 μM SANGER
C8166 Growth Inhibition assay IC50 = 251.341 μM SANGER
SKG-IIIa Growth Inhibition assay IC50 = 251.504 μM SANGER
HT-1197 Growth Inhibition assay IC50 = 268.492 μM SANGER
no-11 Growth Inhibition assay IC50 = 291.357 μM SANGER
ME-180 Growth Inhibition assay IC50 = 296.912 μM SANGER
NY Growth Inhibition assay IC50 = 320.632 μM SANGER
C-33-A Growth Inhibition assay IC50 = 325.06 μM SANGER
NCI-H2029 Growth Inhibition assay IC50 = 338.305 μM SANGER
IST-SL1 Growth Inhibition assay IC50 = 342.105 μM SANGER
KLE Growth Inhibition assay IC50 = 347.29 μM SANGER
SF539 Growth Inhibition assay IC50 = 348.01 μM SANGER
5637 Growth Inhibition assay IC50 = 360.37 μM SANGER
COLO-824 Growth Inhibition assay IC50 = 363.58 μM SANGER
NCI-H810 Growth Inhibition assay IC50 = 363.938 μM SANGER
JAR Growth Inhibition assay IC50 = 365.01 μM SANGER
L-428 Growth Inhibition assay IC50 = 369.277 μM SANGER
COLO-668 Growth Inhibition assay IC50 = 387.033 μM SANGER
GI-1 Growth Inhibition assay IC50 = 398.59 μM SANGER
NCI-H446 Growth Inhibition assay IC50 = 399.497 μM SANGER
CCRF-CEM Growth Inhibition assay IC50 = 403.587 μM SANGER
T84 Growth Inhibition assay IC50 = 403.686 μM SANGER
K-562 Growth Inhibition assay IC50 = 432.947 μM SANGER
OMC-1 Growth Inhibition assay IC50 = 433.814 μM SANGER
LB831-BLC Growth Inhibition assay IC50 = 434.556 μM SANGER
BT-549 Growth Inhibition assay IC50 = 435.102 μM SANGER
MKN7 Growth Inhibition assay IC50 = 439.822 μM SANGER
SW1783 Growth Inhibition assay IC50 = 449.251 μM SANGER
SNB75 Growth Inhibition assay IC50 = 486.478 μM SANGER
M059J Growth Inhibition assay IC50 = 492.923 μM SANGER
KURAMOCHI Growth Inhibition assay IC50 = 498.612 μM SANGER
TE-1 Growth Inhibition assay IC50 = 502.729 μM SANGER
NCI-H596 Growth Inhibition assay IC50 = 530.805 μM SANGER
PFSK-1 Growth Inhibition assay IC50 = 532.941 μM SANGER
MOLM13 Function assay 24 hrs Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs, IC50 = 0.011 μM. 24641103
COLO205 Antiproliferative assay 72 hrs Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.036 μM. 24641103
MOLM13 Antiproliferative assay 72 hrs Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.096 μM. 24641103
MOLM13 Antiproliferative assay 72 hrs Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.096 μM. 24641103
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.14 μM. 24641103
insect cell Function assay 2 mins Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.009 μM. 26115571
insect cell Function assay 2 mins Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.009 μM. 26115571
insect cell Function assay 2 mins Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.011 μM. 26115571
insect cell Function assay 2 mins Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.011 μM. 26115571
MDA-MB-435 Antiproliferative assay 24 hrs Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis, IC50 = 0.16 μM. 26115571
sf9 Function assay Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP, IC50 = 9.2 μM. 26851505
sf9 Function assay Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP, IC50 = 9.2 μM. 26851505
insect cell Function assay 2 mins Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.011 μM. 27171036
insect cell Function assay 2 mins Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.011 μM. 27171036
insect cell Function assay 2 mins Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.015 μM. 27171036
insect cell Function assay 2 mins Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.015 μM. 27171036
MDA-MB-453 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.137 μM. 27448913
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.24 μM. 27448913
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.58 μM. 27448913
MCF7 Antitumor assay 100 mg/kg/day 14 days Antitumor activity against human estrogen-independent human MCF7 cells xenografted in RNU rat assessed as tumor growth inhibition at 100 mg/kg/day, ig administered for 14 days measured on day 15 27448913
A2780 Growth inhibition assay 72 hrs Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.032 μM. 28156111
MV4-11 Growth inhibition assay 72 hrs Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay, GI50 = 0.05 μM. 28156111
MOLM13 Growth inhibition assay 72 hrs Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.062 μM. 28156111
NB4 Growth inhibition assay 72 hrs Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.066 μM. 28156111
PC3 Growth inhibition assay 72 hrs Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.071 μM. 28156111
MDA-MB-453 Growth inhibition assay 72 hrs Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay, GI50 = 0.326 μM. 28156111
MCF7 Growth inhibition assay 72 hrs Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.557 μM. 28156111
M229 Growth inhibition assay 72 hrs Growth inhibition of human M229 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.22 μM. 28156111
M238 Growth inhibition assay 72 hrs Growth inhibition of human M238 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.97 μM. 28156111
M249 Growth inhibition assay 72 hrs Growth inhibition of human M249 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.99 μM. 28156111
M249R Growth inhibition assay 72 hrs Growth inhibition of human M249R cells after 72 hrs by resazurin or MTT assay, GI50 = 2.96 μM. 28156111
C4-2B Growth inhibition assay 72 hrs Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay, GI50 = 4.15 μM. 28156111
DU145 Growth inhibition assay 72 hrs Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay, GI50 = 5.792 μM. 28156111
MDA-MB-468 Growth inhibition assay 72 hrs Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay, GI50 = 5.96 μM. 28156111
BPH1 Growth inhibition assay 72 hrs Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay, GI50 = 7.442 μM. 28156111
K562 Cytotoxicity assay 96 hrs Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay, IC50 = 2 μM. 24417566
DU145 Cytotoxicity assay 96 hrs Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay, IC50 = 7.5 μM. 24417566
MDA-MB-231 Cell cycle arrest assay 0.5 to 1 uM 24 hrs Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1 phase at 0.5 to 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis 24417566
MCF7 Cell cycle arrest assay 0.5 to 1 uM 24 hrs Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 0.5 to 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis 24417566
MDA-MB-231 Function assay 0.5 to 5 uM 24 hrs Inhibition of recombinant CDK4/cyclinD1 in human MDA-MB-231 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis 24417566
MDA-MB-231 Function assay 0.5 to 5 uM 24 hrs Inhibition of recombinant CDK4/cyclinD1 in human MDA-MB-231 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis 24417566
MCF7 Function assay 0.5 to 5 uM 24 hrs Inhibition of recombinant CDK4/cyclinD1 in human MCF7 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis 24417566
MCF7 Function assay 0.5 to 5 uM 24 hrs Inhibition of recombinant CDK4/cyclinD1 in human MCF7 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis 24417566
MV4-11 Function assay 12 to 24 hrs Inhibition of CDK4/6 in human MV4-11 cells assessed as reduction in Rb phosphorylation at Ser780 at GI50 after 12 to 24 hrs by Western blot analysis 28156111
MV4-11 Function assay 12 to 24 hrs Inhibition of CDK4/6 in human MV4-11 cells assessed as reduction in Rb phosphorylation at Ser780 at GI50 after 12 to 24 hrs by Western blot analysis 28156111
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

Water : 100 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

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In vivo
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In vivo Formulation Calculator (Clear solution)

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Chemical Information, Storage & Stability

Molecular Weight 573.66 Formula

C24H29N7O2.C2H6O4S

 Storage (From the date of receipt)
CAS No. 827022-33-3 Download SDF Storage of Stock Solutions

Synonyms PD0332991 Isethionate Smiles CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.C(CS(=O)(=O)O)O

Mechanism of Action

Features
The 1st specific inhibitor for CDK4/6 to show promise in multiple cancers.
Targets/IC50/Ki
CDK4/CyclinD3
(Cell-free assay)
9 nM
CDK4/CyclinD1
(Cell-free assay)
11 nM
CDK6/CyclinD2
(Cell-free assay)
15 nM
In vitro
PD 0332991 exhibits absolute selectivity for CDK4/6 with little or no activity against other CDKs. PD 0332991 is effective at reducing Rb phosphorylation at Ser780 and Ser795 in MDA-MB-435 breast carcinoma cells with IC50 of 66 nM and 63 nM, respectively. PD 0332991 is a potent inhibitor of cell growth and suppresses DNA replication by preventing cells from entering S phase. PD 0332991 inhibits thymidine incorporation into the DNA of Rb-positive human breast (such as MDA-MB-435, MCF-7), colon (H1299), and lung carcinomas (Colo-205) as well as human leukemias (CRRF-CEM and K562), with IC50 values ranging from 0.04-0.17 μM. PD 0332991 significant increases the percentage of MDA-MB-453 in G1 period. PD 0332991 inhibits phosphorylation of Rb in cycling CD138+ primary bone marrow myeloma cells, nontransformed primary B cells, MM1.S and CAG HMCLs cells line with IC50 of <0.1 μM, 0.05 μM, and 60-70 nM, respectively. PD 0332991 treatment also induces G1 arrest of CD138+ primary bone marrow myeloma and nontransformed primary B cells. PD 0332991 induces G1 arrest in MM1.S with IC50 of ~0.05 μM. PD 0332991 preferentially inhibits proliferation of luminal estrogen receptor-positive (including HER2-positive) human breast cancer cell lines. PD 0332991 increases gene expression of pRb and cyclin D1 and decreases gene expression of CDKN2A (p16) in most sensitive lines. PD 0332991 enhances sensitivity to tamoxifen in cell lines with conditioned resistance to ER blockade.
Kinase Assay
CDK activity assays
CDK assays for IC50 determinations and kinetic evaluation are performed in 96-well filter plates. All CDK-cyclin kinase complexes are expressed in insect cells through baculovirus infection and purified. The substrate for the assays is a fragment (amino acids 792–928) of pRb fused to GST (GST•RB-Cterm). The total reaction volume is 0.1 mL containing a final concentration of 20 mM Tris-HCl, pH 7.4, 50 mM NaCl, 1 mM dithiothreitol, 10 mM MgCl2 25 μM ATP (for CDK4-cyclin D1, CDK6-cyclin D2, and CDK6-cyclin D3) containing 0.25 μCi of [γ-32P]ATP, 20 ng of enzyme, 1 μg of GST•RB-Cterm, and appropriate dilutions of inhibitor. All components except the [γ-32P]ATP are added to the wells, and placed on a plate mixer for 2 min. The reaction is started by adding the [γ-32P]ATP, and incubated at 25℃ for 15 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid, and the plate is kept at 4 ℃ for at least 1 hr to allow the substrate to precipitate. The wells are then washed five times with 0.2 mL of 10% trichloroacetic acid, and radioactive incorporation is determined with a β plate counter.
In vivo
PD 0332991(150 mg/kg) produces rapid Colo-205 colon carcinoma xenografts regressions and a corresponding tumor growth delay. PD 0332991 (150 mg/kg) induces complete tumor stasis and cell kill in MDA-MB-435 breast carcinoma. PD 0332991 (150 mg/kg) also induces significant tumor regression in mice bearing the SF-295 glioblastoma xenografts, and in ZR-75-1 breast and PC-3 prostate tumor models (complete suppression of tumor growth). PD 0332991 (150 mg/kg) suppresses Rb Ser780 phosphorylation in MDA-MB-435 breast carcinoma over the full 24-hour period. PD 0332991 (150 mg/kg) down-regulates expression of four E2F-regulated genes CDC2, CCNE2, TK1, and TOP2A in Colo-205 carcinoma xenografts. PD 0332991 also rapidly inhibits myeloma tumor growth.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11278443/

Applications

Methods Biomarkers Images PMID
Western blot RB1 (pT821) / RB1 (pS780) pAMPKα(T172) / AMPKα pULK1(S317) / ULK1 c-Jun / p-c-Jun / NFκB(p50) p38 / p-P38 / JNK / p-JNK
S1579-WB1
30300583
Growth inhibition assay Cell viability IC50
S1579-viability1
28453226
Immunofluorescence γH2AX(Ser139) LC3B
S1579-IF2
29669860
ELISA PGE2
S1579-ELISA1
26540629

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05665361 Recruiting
Advanced Clear Cell Renal Carcinoma (Ccrcc)|Papillary Renal Cell Carcinoma (Prcc)
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 April 24 2024 Phase 1|Phase 2
NCT06307457 Completed
Breast Cancer
Pfizer
 March 11 2024 --
NCT05709158 Not yet recruiting
Breast Cancer
Pfizer
 March 1 2024 --
NCT05912933 Not yet recruiting
Breast Cancer
Pfizer
 March 1 2024 --

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
What is the best vehicle for it for in vitro and in vivo?

Answer:
It can be used with water for vitro use and saline for vivo use.

Signaling Pathway Map