Palbociclib (PD-0332991) HCl

For research use only.

Licensed by Pfizer Catalog No.S1116

241 publications

Palbociclib (PD-0332991) HCl Chemical Structure

CAS No. 827022-32-2

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

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Selleck's Palbociclib (PD-0332991) HCl has been cited by 241 publications

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Choose Selective CDK Inhibitors

Biological Activity

Description Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.
Features Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).
Targets
CDK4/CyclinD3 [1]
(Cell-free assay)
CDK4/CyclinD1 [1]
(Cell-free assay)
CDK6/CyclinD2 [1]
(Cell-free assay)
9 nM 11 nM 15 nM
In vitro

PD 0332991 has little effect on other protein kinases including EGFR, FGFR, PGFR, IR. PD 0332991 is a non-ATP competitive inhibitor of Cdk4. PD 0332991 inhibits MDA-MB-435 breast carcinoma cells with IC50 of 66 nM, which is due to reduced Rb phosphorylation at Ser780. PD 0332991 inhibits thymidine incorporation into the DNA of Rb-positive human breast, colon, and lung carcinomas as well as human leukemias, with IC50 values ranging from 0.04-0.17 μM. PD 0332991 shows no activity in Rb-negative cells. PD 0332991 causes an accumulation of cells in G1 in MDA-MB-453 breast and Colo-205 carcinoma cells. [1] PD 0332991 also shows activity in 5T33MM myeloma cells (immunocompetent model) and sensitizes the cells to killing by bortezomib. [2] PD 0332991 inhibits luminal ER-positive as well as HER2-amplified breast cancer cell lines including MDA-MB-175, ZR-75-30, CAMA-1, MDA-MB-134, HCC-202 and UACC-893. PD 0332991 enhances the activity of tamoxifen and trastuzumab in these cell lines. PD 0332991 enhances the sensitivity of tamoxifen in the MCF7 tamoxifen-resistant cells. [3] A recent study shows that PD 0332991 could suppress malignant rhabdoid tumor (MRT) cell lines including MP-MRT-AN, KP-MRT-RY, G401, KP-MRT-NS and the sensitivity of the MRT cell lines to PD 0332991 is inversely correlated with expression of p16. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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MOLM13 NUPKcHlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\3NFczKGh? MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2RTF2xN{Bk\WyuczDoZZJjd3KrbnegSmxVOyCLVFSgcZV1[W62IHHzd4V{e2WmIHHzJIlv[2:{cH;yZZRqd25ib3[gX|NJZXSqeX3p[Ilv\SCrboTvJGRPSSC5aYToJGlEPTBib3[gNE4xQTZizszN NGG1bnEzPDZ2MUGwNy=>
MOLM13 NXr3VVlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEK4eHI4OiCq MmThRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDzc5Ji\mWwaXKtdoV{cXO2YX70JIh2dWGwIF3PUG0yOyClZXzsd{Bie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG30bJlucWSrbnWgbY51dyCGTlGge4l1cCCLQ{WwJI9nKDBwMEm2JO69VQ>? NWL2VVlEOjR4NEGxNFM>
MDA-MB-435 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzLNlQhcA>? MmrUTWM2OD1yLkG2JO69VQ>? Mlq0NVU5ODF6M{G=
K562 MWnDfZRwfG:6aXOgRZN{[Xl? MUO5OkBp MVHEUXNQ NVn4e3o4UUN3ME2yJO69VQ>? MYCyOFQyPzV4Nh?=
DU145 MmP4R5l1d3SxeHnjJGF{e2G7 MofUPVYhcA>? MlTISG1UVw>? M4C0XWlEPTB;Nz61JO69VQ>? NWDPTHlrOjR2MUe1OlY>
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697 NH;WboZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnoUo1EUUN3ME2xOFgvOzhibl2= M4KxWHNCVkeHUh?=
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NCI-SNU-1 M2fkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnOTWM2OD1zLkG2N|U1KM7:TR?= NVX0cXpOW0GQR1XS
CGTH-W-1 M3Lpe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjpepB2UUN3ME2xMlE4OTh4IN88US=> MnnsV2FPT0WU
MHH-ES-1 NYTuRlFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTFwMUe5PFYh|ryP NH:5NmpUSU6JRWK=
LB2241-RCC MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFwMUi2NkDPxE1? MljNV2FPT0WU
ML-2 NE\DU4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjiOnNxUUN3ME2xMlIxPzN2IN88US=> MonXV2FPT0WU
COR-L23 MmnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{[xRWlEPTB;MT6yNlk{OyEQvF2= NGO0NoNUSU6JRWK=
BFTC-905 MlvFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnNTWM2OD1zLkK0NlY4KM7:TR?= M2f5PHNCVkeHUh?=
Hs-578-T MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTFwMkW4NVch|ryP NWq2NZV2W0GQR1XS
KG-1 NYDORmlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjtNWMzUUN3ME2xMlI3Pjh4IN88US=> NHTibohUSU6JRWK=
HEL M2G2Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTFwMkmzN|gh|ryP MlHXV2FPT0WU
A549 M2PLemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\hTmlEPTB;MT6yPVM6QSEQvF2= NVTJUGxGW0GQR1XS
COLO-741 NVe0R2hOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLFPGxKSzVyPUGuN|IxQDlizszN NX3TO2U6W0GQR1XS
PC-3 MoS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXryTYg4UUN3ME2xMlM2OjJzIN88US=> MV\TRW5ITVJ?
HOS MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmD3TWM2OD1zLkO1Nlk3KM7:TR?= Mm\FV2FPT0WU
HT-1080 NUDL[ndvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE[2e5lKSzVyPUGuN|c2OTlizszN NIHFSpBUSU6JRWK=
TE-8 NIDwN21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvCTWM2OD1zLkSxO|c1KM7:TR?= MonkV2FPT0WU
BHY M2nEWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLVTWM2OD1zLkS2PVI{KM7:TR?= MmTkV2FPT0WU
BB65-RCC NUC2N2tmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2X6R2lEPTB;MT61NFUzQCEQvF2= NVnReFlzW0GQR1XS
HN MkfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPQTWM2OD1zLkW0NFcyKM7:TR?= M1T6NnNCVkeHUh?=
NCI-H441 NEi4SGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDGcWt1UUN3ME2xMlU1QTB5IN88US=> NXy1UI9KW0GQR1XS
RPMI-8866 NULBXGpqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHGxTVhKSzVyPUGuOVg2ODdizszN MnLJV2FPT0WU
CAL-62 M4XhR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7LOINKSzVyPUGuOlA5PjJizszN MmXuV2FPT0WU
MG-63 M37aeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnncoExUUN3ME2xMlYyQDF|IN88US=> MmD3V2FPT0WU
SK-LU-1 Mny1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mle4TWM2OD1zLk[yNVUzKM7:TR?= MlHBV2FPT0WU
BCPAP MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTFwNk[0OVch|ryP NYnnXmZ7W0GQR1XS
22RV1 NViwUpZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFmxOYhKSzVyPUGuOlc5PDNizszN MmnaV2FPT0WU
T47D M4C4bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfM[IR{UUN3ME2xMlY5ODZzIN88US=> MlqyV2FPT0WU
MSTO-211H NIXXZllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTFwNkm2NFMh|ryP NIL1SIlUSU6JRWK=
DEL NFPSVXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrBZlltUUN3ME2xMlcxOjd|IN88US=> Ml7uV2FPT0WU
H4 NVLnZYFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NES5[npKSzVyPUGuO|MzOTJizszN MWXTRW5ITVJ?
CAL-51 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\VbpJLUUN3ME2xMlc1QDV3IN88US=> MU\TRW5ITVJ?
ABC-1 NVfRSJhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjnc4V[UUN3ME2xMlc5PTh{IN88US=> M37SVnNCVkeHUh?=
MZ2-MEL NI\Hd|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIe4XJZKSzVyPUGuO|k2PDJizszN MUDTRW5ITVJ?
YKG-1 NHjU[I5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFwOEGwOlEh|ryP Ml64V2FPT0WU
KM12 NGi3OGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTFwOEG2NFIh|ryP NYLQZ|Z{W0GQR1XS
L-363 NYnZXlVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTFwOEe0NVIh|ryP MXXTRW5ITVJ?
KU812 NWLJ[HdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWP2ZnJTUUN3ME2xMlg6Ojh{IN88US=> MXvTRW5ITVJ?
LOXIMVI NWDocI9NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfWNZVvUUN3ME2xMlkyOjJ6IN88US=> NWfid5F2W0GQR1XS
G-401 M{jCcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEX2U5NKSzVyPUGuPVI1OjhizszN M2TVZ3NCVkeHUh?=
SW780 Mk\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTld|hKSzVyPUGuPVYzPDZizszN Mm\VV2FPT0WU
SW872 M3jFfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3ETWM2OD1zLkm4N|Mh|ryP MXrTRW5ITVJ?
NB7 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIL6S|NKSzVyPUGuPVk{OjNizszN NYPpfVZzW0GQR1XS
T98G MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXj[ZBKSzVyPUKuNFA3PjZizszN MYDTRW5ITVJ?
SW1710 Ml;6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HEWGlEPTB;Mj6wOlk1PSEQvF2= NUnsfItpW0GQR1XS
NCI-H1573 NVjuSIpsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\OV2lEPTB;Mj6wO|I6QCEQvF2= MnnFV2FPT0WU
KE-37 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFj5VYdKSzVyPUKuNFg6PTFizszN MlLzV2FPT0WU
786-0 M1PnU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXvNYhnUUN3ME2yMlE2PDN7IN88US=> MkD2V2FPT0WU
SAS Mof2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnv2TWM2OD1{LkKwN|c1KM7:TR?= MVzTRW5ITVJ?
CAL-54 M1fsXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\uTWM2OD1{LkKwOFE{KM7:TR?= M17hVHNCVkeHUh?=
SF268 NHToTpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTJwMkOxNlIh|ryP MnXIV2FPT0WU
SW620 MlfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PBU2lEPTB;Mj6yOlE3QSEQvF2= NH3BOWNUSU6JRWK=
MN-60 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTJwM{GwOkDPxE1? NW\6eppLW0GQR1XS
EFO-27 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LVTmlEPTB;Mj6zNlA2QCEQvF2= MoT5V2FPT0WU
NCI-H747 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\sTWM2OD1{LkOyNVk6KM7:TR?= NWDPUI1MW0GQR1XS
HCC2218 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTJwM{WzO|Qh|ryP M3PQTXNCVkeHUh?=
MIA-PaCa-2 MnviS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjr[oxKSzVyPUKuN|Y1OzdizszN NWnpc2tXW0GQR1XS
SJSA-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTJwM{e3PVYh|ryP M1;N[HNCVkeHUh?=
RKO NXPGbW51T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrFTWM2OD1{LkO4OFk3KM7:TR?= NYH1UpZtW0GQR1XS
NB6 Mn\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M374T2lEPTB;Mj60NFM4PCEQvF2= MkjuV2FPT0WU
ES4 NWLacIw3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTQTWM2OD1{LkS1OFIzKM7:TR?= MmD0V2FPT0WU
EGI-1 MmW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnSN29[UUN3ME2yMlQ3QDh|IN88US=> NEL1[4tUSU6JRWK=
CTV-1 M1Gzfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3wTWM2OD1{LkWyO|c{KM7:TR?= MorvV2FPT0WU
NCI-H1355 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33YPWlEPTB;Mj61OVk2OSEQvF2= NF\CUmdUSU6JRWK=
GT3TKB MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTJwNUmxPVkh|ryP Ml2yV2FPT0WU
SK-HEP-1 M1rIfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPZdIxKSzVyPUKuOVkzPjZizszN NXezZY52W0GQR1XS
GAMG NHjhe25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\nd2lEPTB;Mj61PVM6PCEQvF2= MoO1V2FPT0WU
SK-MES-1 NHX1Um9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvzdnBJUUN3ME2yMlYyQDB|IN88US=> NGqyNGxUSU6JRWK=
RO82-W-1 NVvnOnhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\xVGlEPTB;Mj62NlA2PyEQvF2= MVTTRW5ITVJ?
ECC10 MnHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrRXnBKSzVyPUKuO|AzODZizszN Mn\mV2FPT0WU
MCF7 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mof1TWM2OD1{LkexOFY1KM7:TR?= NF;acmZUSU6JRWK=
D-283MED MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HOR2lEPTB;Mj63NlQ{KM7:TR?= NGG2cJRUSU6JRWK=
RPMI-7951 NH3sWFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmi4TWM2OD1{Lke1Olk1KM7:TR?= NVXjV3NIW0GQR1XS
Ramos-2G6-4C10 NUWzNGVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTJwN{ewPVkh|ryP NE\ESm5USU6JRWK=
KGN MljCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHf1cmxKSzVyPUKuPFE5QDRizszN MljxV2FPT0WU
NUGC-3 MmfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rpdGlEPTB;Mj64NlUxPSEQvF2= MnfXV2FPT0WU
NCI-H292 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELPWXlKSzVyPUKuPFUxPTNizszN M1O3NnNCVkeHUh?=
Becker MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HKUGlEPTB;Mj65OVg{OiEQvF2= M{C0TnNCVkeHUh?=
NCI-H1299 MkXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljYTWM2OD1|LkC1NlY{KM7:TR?= NHfscYlUSU6JRWK=
ETK-1 NHXMSIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TmUmlEPTB;Mz6wOVQ{KM7:TR?= MXnTRW5ITVJ?
TK10 NEizS25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTNwMkCxOlUh|ryP MVzTRW5ITVJ?
VMRC-RCZ M4W5XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFq3XVFKSzVyPUOuN|Y1QDhizszN MYfTRW5ITVJ?
YH-13 MlLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXTdVN3UUN3ME2zMlQ1ODd7IN88US=> MnXFV2FPT0WU
DU-145 MnTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTNwNE[yOlkh|ryP MlLSV2FPT0WU
SW1088 NHrQWphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTNwNEe0O{DPxE1? NY\3ZXNzW0GQR1XS
HOP-92 M{DRd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnhOFV[UUN3ME2zMlUxOzR{IN88US=> MoLxV2FPT0WU
KP-N-YS NHvROplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4m0RWlEPTB;Mz62NlE{QSEQvF2= Mn2yV2FPT0WU
NCI-H460 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\GVmJ1UUN3ME2zMlY3PzNizszN M{PESHNCVkeHUh?=
U-2-OS MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXFXo9MUUN3ME2zMlczPTN3IN88US=> MnnCV2FPT0WU
A101D MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4S2NmlEPTB;Mz63Olk{PiEQvF2= M{\0NHNCVkeHUh?=
MDA-MB-231 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTNwOEG5OVEh|ryP MlzFV2FPT0WU
IST-MES1 MmnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrSTWM2OD1|LkizNkDPxE1? NF3kd4ZUSU6JRWK=
COR-L105 M13xU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTRwMEG4JO69VQ>? MoLkV2FPT0WU
NCI-H1437 M3jCemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL5NndrUUN3ME20MlAzOzB{IN88US=> MVTTRW5ITVJ?
CAL-85-1 NGG0XnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTF[ml3UUN3ME20MlAzPDZzIN88US=> Mn\WV2FPT0WU
MZ1-PC NGjIPZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzlTWM2OD12LkG4OVU3KM7:TR?= M{D4[3NCVkeHUh?=
VM-CUB-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfKWYc2UUN3ME20MlMyOjh2IN88US=> M3fWW3NCVkeHUh?=
CHL-1 M1\Tb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vwSWlEPTB;ND6zNlE3QSEQvF2= MlX4V2FPT0WU
MDA-MB-361 NVv1WpBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEGxblhKSzVyPUSuN|MyPTNizszN M4rlR3NCVkeHUh?=
NCI-H661 NFr2XoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWftfGE5UUN3ME20MlUxODl{IN88US=> Mo\mV2FPT0WU
EW-11 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmeyTWM2OD12LkWyNlMyKM7:TR?= MmriV2FPT0WU
BEN NEGx[llIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PsU2lEPTB;ND61NlgyPSEQvF2= NHjFbG1USU6JRWK=
BFTC-909 NHSyR3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPETWM2OD12LkW2Nlc2KM7:TR?= M3mzWHNCVkeHUh?=
NCI-H2087 MmLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jXdGlEPTB;ND61PFE3PCEQvF2= MWjTRW5ITVJ?
RVH-421 M{DTO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[yUmtKSzVyPUSuOlY3QSEQvF2= NHvZZZFUSU6JRWK=
P30-OHK MkjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHVfYhGUUN3ME20MlY5ODB6IN88US=> NXL2XllGW0GQR1XS
NCI-H28 MmrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTRwOEG2OlEh|ryP MWXTRW5ITVJ?
ES6 MmfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2ThdmlEPTB;ND64N|AyPiEQvF2= M1PpNnNCVkeHUh?=
769-P NXvVTYpoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUO3b4VpUUN3ME20Mlg2QTJ4IN88US=> M3LTUHNCVkeHUh?=
OE33 M1TWb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTRwOEixOlEh|ryP MYXTRW5ITVJ?
SW982 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrIVJZKSzVyPUSuPVUxPjFizszN M{Xx[HNCVkeHUh?=
A388 NWjJfnloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTVwMEK5PFMh|ryP NFjNVXJUSU6JRWK=
TI-73 NHHxeIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7UfWpKSzVyPUWuNFYyQTRizszN NYjzfWVDW0GQR1XS
HCT-116 M37iNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWf4d5Z5UUN3ME21MlA6QDh7IN88US=> NVfhOpRRW0GQR1XS
HuP-T3 NH3QXo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDqVm9KSzVyPUWuNVg4ODlizszN MV\TRW5ITVJ?
G-402 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHGzcZFKSzVyPUWuNVk1OTZizszN Ml;uV2FPT0WU
NCI-H1792 NYDQdINwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DWR2lEPTB;NT6yOFYzOiEQvF2= NGm5cpBUSU6JRWK=
NCI-H209 M2X4bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTVwMkW5OFIh|ryP NXzsTHZDW0GQR1XS
NCI-H1650 NXrESZhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTVwM{C2N|Qh|ryP MXrTRW5ITVJ?
LCLC-97TM1 MnniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTVwM{G4NFgh|ryP NYnld5dqW0GQR1XS
S-117 NWTYblZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV35O4wzUUN3ME21MlM3QTd4IN88US=> M33M[nNCVkeHUh?=
GI-ME-N MoK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XVZWlEPTB;NT6zPVY5OSEQvF2= MUTTRW5ITVJ?
NCI-H2122 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFP2WIhKSzVyPUWuOFk{QTdizszN NVXnWWxTW0GQR1XS
NCI-H1793 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGra[WJKSzVyPUWuOlc2QTNizszN MW\TRW5ITVJ?
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CaR-1 M{XScGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPyZmhKSzVyPUG5MlY5ODRizszN MnPoV2FPT0WU
KYSE-410 NXfodVdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHUSJhKSzVyPUG5MlkyOzlizszN M3rY[3NCVkeHUh?=
HuCCT1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHz3eYhKSzVyPUKwMlYzQTRizszN MVvTRW5ITVJ?
LB996-RCC NGSzRZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2j4eWlEPTB;MkCuO|E3QCEQvF2= NXnVWlBlW0GQR1XS
KYSE-70 NW\GdWRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPjU2JKSzVyPUKwMlgxPTlizszN MYrTRW5ITVJ?
CAL-72 NXKyfpVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLsXIh1UUN3ME2yNE46OTVizszN NUGxfZlsW0GQR1XS
Capan-2 MnXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnGZoNKSzVyPUKxMlA1OTNizszN M4WyZnNCVkeHUh?=
PANC-08-13 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTKdFZWUUN3ME2yNU4zPTF3IN88US=> MVXTRW5ITVJ?
SBC-1 M4\mOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH:3ZYZKSzVyPUKxMlMxQDFizszN MV7TRW5ITVJ?
MFM-223 MmOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXXTWM2OD1{MT6zN|QzKM7:TR?= M4P4TnNCVkeHUh?=
BB49-HNC M2j6O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTuSJNKSzVyPUKxMlU4OTZizszN M2XFe3NCVkeHUh?=
SH-4 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HtNWlEPTB;MkGuOlYyQCEQvF2= NFH6bIpUSU6JRWK=
HuO9 Mnz6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTJzLkm4NlUh|ryP MlnmV2FPT0WU
AM-38 M13tRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTJ{LkC0PFUh|ryP MonOV2FPT0WU
A431 MkLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHWS2RKSzVyPUKzMlIyOTlizszN MVzTRW5ITVJ?
YAPC NYTvOoxNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;rTWM2OD1{Mz6yOlUyKM7:TR?= MkTWV2FPT0WU
LU-139 NFLZZ2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLDXJAxUUN3ME2yN{41QDB7IN88US=> NFTJ[4xUSU6JRWK=
HEC-1 NFvOUHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;WOGlEPTB;MkOuOFk{PyEQvF2= MV7TRW5ITVJ?
SCC-25 NVnxdmcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDReIJKSzVyPUK0MlMxODZizszN MkC3V2FPT0WU
HT-29 M3TDR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTJ2LkO4NlMh|ryP NWrxb5hZW0GQR1XS
PC-14 M{[wOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTJ2Lk[1O|Eh|ryP MUjTRW5ITVJ?
Calu-6 MmHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIruNm1KSzVyPUK1MlUxPzFizszN MV3TRW5ITVJ?
SJRH30 NVHXdXRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkn0TWM2OD1{NT62OFk3KM7:TR?= MV;TRW5ITVJ?
ChaGo-K-1 NIrTRVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jUdGlEPTB;Mk[uNVYzQSEQvF2= MnHJV2FPT0WU
IA-LM NFiyeHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTJ4LkO2OFUh|ryP MnfTV2FPT0WU
GP5d NILHWoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTKfpFKSzVyPUK2MlQ1QTFizszN M4XI[HNCVkeHUh?=
NCI-H2291 M{C3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2q3TWlEPTB;Mk[uOlU1OSEQvF2= M{TrUXNCVkeHUh?=
BALL-1 MmrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PCVGlEPTB;Mk[uPVM6PyEQvF2= M1PI[nNCVkeHUh?=
HCC1954 NWXB[Hg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DTc2lEPTB;Mk[uPVgxQCEQvF2= MmLsV2FPT0WU
NCI-H2452 NGHmdJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfRbmxDUUN3ME2yO{41OTZ|IN88US=> MV\TRW5ITVJ?
LU-99A NEjEfXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{Dv[WlEPTB;MkeuOVU5OiEQvF2= NGPWSZVUSU6JRWK=
NTERA-S-cl-D1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTJ5LkeyPVkh|ryP NYDxVZRCW0GQR1XS
PANC-10-05 MoTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTJ5Lke3O|Uh|ryP M1\GT3NCVkeHUh?=
NCI-H2405 NXH6OlJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTJ5LkmzPFch|ryP NIqzWWJUSU6JRWK=
MDA-MB-415 M4\QeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTJ6LkSxN|ch|ryP MV7TRW5ITVJ?
NCI-H2342 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PrVGlEPTB;MkiuOVI5OSEQvF2= MWTTRW5ITVJ?
TGBC24TKB MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7JZodKSzVyPUK4MlcyOTdizszN M2LoOHNCVkeHUh?=
LU-134-A M4rGPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTJ6LkmyOlEh|ryP MWLTRW5ITVJ?
SCC-4 MlfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rYVGlEPTB;M{GuNFQ6PCEQvF2= NVLocZNpW0GQR1XS
Saos-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLncZpSUUN3ME2zNU46OzB4IN88US=> NGLsTGpUSU6JRWK=
RERF-LC-MS NXi5[2hIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTN{LkiyN|Eh|ryP M{C3ZXNCVkeHUh?=
M14 MlLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvBTWM2OD1|Mj65O|Y1KM7:TR?= NHzjWYNUSU6JRWK=
HPAF-II NWTSZmJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVv1OHFNUUN3ME2zN{42ODFzIN88US=> MkfGV2FPT0WU
NCI-H1755 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLYTWM2OD1|ND6zN|A2KM7:TR?= MXHTRW5ITVJ?
D-392MG NU\MTJhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTN3Lki2O|Qh|ryP M2fPSnNCVkeHUh?=
A704 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPJZXZ7UUN3ME2zOk4xPDJ5IN88US=> M3X1enNCVkeHUh?=
CP50-MEL-B MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;vTWM2OD1|Nj6xPVEyKM7:TR?= M3PFOXNCVkeHUh?=
EW-18 NY[wVXpLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;qTWM2OD1|Nj60OVIh|ryP NH\2UoJUSU6JRWK=
WM-115 MoTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXFS3lrUUN3ME2zOk45ODl7IN88US=> NFXsPGtUSU6JRWK=
LU-65 MmXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTN5LkG0NVch|ryP NW\MemtlW0GQR1XS
NCI-H1563 NYrmfVl5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPwN2NKSzVyPUO3MlI1QDRizszN Mk\PV2FPT0WU
DBTRG-05MG M3X1Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3npTmlEPTB;M{iuNFY6OSEQvF2= NHizeFdUSU6JRWK=
NCI-H630 NEHU[npIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3aV5dMUUN3ME2zPE41PzF2IN88US=> MnHqV2FPT0WU
NCI-H1155 MkPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFO0UJVKSzVyPUO5MlI1OiEQvF2= MUDTRW5ITVJ?
OVACR-3 NIXNb2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPUOIpKSzVyPUO5MlkyQTVizszN NVvKRWY3W0GQR1XS
OAW-42 M{jZd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rCTGlEPTB;NECuOFI2QCEQvF2= NHfSR41USU6JRWK=
JVM-2 MlniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTRzLkK0NVUh|ryP MWXTRW5ITVJ?
C3A MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PndWlEPTB;NEGuN|Q1PyEQvF2= MVzTRW5ITVJ?
HT55 M2i0U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHZTYNPUUN3ME20Nk4zQDRzIN88US=> NFnSZYJUSU6JRWK=
OVCAR-4 MmnWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPFWXNKSzVyPUSyMlI6PzRizszN MXzTRW5ITVJ?
MEG-01 MmL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTR{LkS2NVYh|ryP NIToTlJUSU6JRWK=
NCI-H82 M3;BcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjVemtKSzVyPUSzMlk5QTJizszN MlLjV2FPT0WU
JEG-3 MoLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;PW|JrUUN3ME20OE46PDdizszN M1vwVnNCVkeHUh?=
BPH-1 NHLFeWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLSTWM2OD12Nj6zPVk5KM7:TR?= Moi1V2FPT0WU
MPP-89 NIXNdWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTR5LkK4PVgh|ryP MVzTRW5ITVJ?
ALL-PO M{LIbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILuXFRKSzVyPUS3MlQyQDhizszN M1jaXHNCVkeHUh?=
HT NU\ESGt6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPV[lRqUUN3ME20O{41QTJizszN MlT6V2FPT0WU
NCI-H2347 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\INGlEPTB;NEiuNFcyPSEQvF2= NE\6TI1USU6JRWK=
A2780 M{m3N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3K3[2lEPTB;NEmuOFIzQCEQvF2= NILJSXVUSU6JRWK=
KARPAS-299 MmXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXL3XJlTUUN3ME20PU42OTF7IN88US=> MmjpV2FPT0WU
NCI-H1651 NFfYTlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTR7Lki4NlEh|ryP MYDTRW5ITVJ?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
RB1 (pT821) / RB1 (pS780) / RB1 / CDK6 / CCND2 / RUNX1 / ETO; 

PubMed: 30300583     


Immunoblots showing dose-dependent impact of 72 hr palbociclib treatment on indicated protein levels in Kasumi-1 and SKNO-1 cells.

pRb(S807, 811) / CDK4 / CDK6 / PARP; 

PubMed: 28453226     


Effects of palbociclib on CDK4/6-Rb pathway. HCC cells were treated with different doses of palbociclib for 24 h, and then, the cells were subjected to western blot analysis. CF, cleaved fragment. 

LC3-I / LC3-II; 

PubMed: 28453226     


Palbociclib increases LC3-II amount in a dose-dependent manner in HCC cell lines. 

pAMPKα(T172) / pULK1(S317); 

PubMed: 28453226     


Dose-dependent response of palbociclib on AMPK-related molecules. HCC cells were treated with different concentrations of palbociclib for 24 h. The phosphorylation of the indicated proteins was determined by western blotting. 

SMAD2 (pS255); 

PubMed: 30343527     


T47D cells were treated with indicated concentrations of palbociclib for 24 h to evaluate substrate phosphorylation.

30300583 28453226 30343527
Growth inhibition assay
Cell viability; 

PubMed: 29670090     


Cell viability was determined by MTT assays after palbociclib exposure for 2, 4, and 6 days. The cell cycle of SYO-1 and Fuji cells was assessed after exposure to palbociclib (1 µM) for 24 h by flow cytometry analysis.

29670090
Immunofluorescence
SAHF/ATRX; 

PubMed: 26988987     


DAPI staining for senescence-associated heterochromatic foci (SAHF, left panel) and ATRX staining (right panel) in 1205Lu cells +/− palbociclib for 8 days. 

LC3B; 

PubMed: 28453226     


LC3B immunofluorescence in palbociclib‐treated Hep3B cells. Arrowheads indicate LC3-positive autophagosomes. Nuclei were counterstained with DAPI (blue).

26988987 28453226
ELISA
PGE2; 

PubMed: 26540629     


The supernatant of control and 7.5 μM palbociclib-treated cells was collected and stored at −80°C. PGE2 secretion was detected using ELISA.

26540629
In vivo PD 0332991 indicates complete tumor stasis in a MDA-MB-435 xenograft at 150 mg/kg. PD 0332991 also shows broad-spectrum antitumor activity in multiple human tumor xenografts by eliminating phospho-Rb and the proliferative marker Ki-67 from tumor tissue and down-regulation of genes under the transcriptional control of E2F. [1]

Protocol

Kinase Assay:

[1]

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Cdk Assays:

A stock solution of PD0332991 is prepared in DMSO. CDK assays 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 volume in each well 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) or 12 μM ATP (for CDK2-cyclin E, CDK2-cyclin A, and CDC2-cyclin B) containing 0.25 μCi of [γ-32P]ATP, 20 ng of enzyme, 1 μg of GST·RB-Cterm, and PD 0332991 (0.001-0.1μM). All components except the [γ-32P]ATP are added to the wells, and the plate is placed on a plate mixer for 2 min. The reaction is started by adding the [γ-32P]ATP and the plate is incubated at 25 °C for 15 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid and the plate is kept at 4  °C for at least 1 hour to allow the substrate to precipitate. The wells are then washed 5 times with 0.2 mL of 10% trichloroacetic acid and radioactive incorporation is determined with a β plate counter.
Cell Research:

[1]

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  • Cell lines: Tumor cell lines including MDA-MB-435, ZR-75-1, T-47D, MCF-7, H1299, Colo-205, MDA-MB-468, H2009, CRRF-CEM and K562
  • Concentrations: 0.01-1 μM
  • Incubation Time: 24 hours
  • Method:

    Cells are seeded at 2 × 104 per well in a 96-well plate and incubated overnight. PD 0332991 (0.01-1 μM) is added to the wells and incubated at 37 °C for another 24 hours. [14C]Thymidine (0.1 μCi) is added to each well and incorporation of the radiolabel is allowed to proceed for 72 hours. Incorporated radioactivity is determined with a β plate counter.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Advanced stage human tumor xenografts including Colo-205, MDA-MB-435 breast, SF-295 glioblastoma, ZR-75-1 breast, PC-3 prostate, H125 lung, SW-620 colon, H23 lung and MDA-MB-468 breast (Rb negative) are established in severe combined immunodeficient mice.
  • Dosages: 0-150 mg/kg
  • Administration: Given by gavage
    (Only for Reference)

Solubility (25°C)

In vitro Water 30 mg/mL (61.98 mM)
DMSO 3 mg/mL warmed (6.19 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.
6 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 483.99
Formula

C24H29N7O2.HCl

CAS No. 827022-32-2
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04483505 Not yet recruiting Drug: Combination Rogaratinib + palbociclib + fulvestrant Breast Cancer Metastatic|Hormone Receptor Positive Malignant Neoplasm of Breast Fundacion CRIS de Investigación para Vencer el Cáncer|Bayer|Pfizer|Apices Soluciones S.L. October 1 2020 Phase 1
NCT04360941 Recruiting Drug: Palbociclib|Drug: Avelumab Triple Negative Breast Cancer|Locally Advanced Breast Cancer|Recurrent Breast Cancer|Metastatic Breast Cancer|ER+ Breast Cancer|HER2-positive Breast Cancer Royal Marsden NHS Foundation Trust|Pfizer|Breast Cancer Now August 11 2020 Phase 1
NCT03870919 Suspended Drug: Palbociclib|Other: locoregional treatment Breast Cancer Stage IV|Radiotherapy|Surgery UNICANCER|Pfizer October 23 2019 Not Applicable

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID