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PD173074 FGFR1 inhibitor

Name: PD173074
Brand: Selleck Chemicals
SKU: S1264
Availability: InStock
Rating: 5 (124 reviews)

Cat.No.S1264

PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.

Chemical Structure

Molecular Weight: 523.67

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Quality Control

Batch: Purity: 99.95%

99.95

Related Targets	EGFR VEGFR JAK PDGFR Src HIF FLT FLT3 HER2 Bcr-Abl
Other FGFR Inhibitors	AZD4547 (Fexagratinib) BLU9931 Futibatinib (TAS-120) LY2874455 PD-166866 H3B-6527 Zoligratinib (Debio-1347) Fisogatinib (BLU-554) SSR128129E Ferulic Acid

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
NCI-H1581	Growth Inhibition Assay			IC50=0.01225 μM	SANGER
KG-1	Growth Inhibition Assay			IC50=0.05129 μM	SANGER
MFM-223	Growth Inhibition Assay			IC50=0.21576 μM	SANGER
EoL-1-cell	Growth Inhibition Assay			IC50=0.32984 μM	SANGER
ECC10	Growth Inhibition Assay			IC50=0.33898 μM	SANGER
H-EMC-SS	Growth Inhibition Assay			IC50=0.34715 μM	SANGER
AN3-CA	Growth Inhibition Assay			IC50=0.40133 μM	SANGER
HuO-3N1	Growth Inhibition Assay			IC50=0.54653 μM	SANGER
RT-112	Growth Inhibition Assay			IC50=0.54701 μM	SANGER
NEC8	Growth Inhibition Assay			IC50=0.56289 μM	SANGER
D-263MG	Growth Inhibition Assay			IC50=0.71159 μM	SANGER
SW962	Growth Inhibition Assay			IC50=0.78988 μM	SANGER
BV-173	Growth Inhibition Assay			IC50=0.84623 μM	SANGER
MFE-280	Growth Inhibition Assay			IC50=0.85872 μM	SANGER
HuH-7	Growth Inhibition Assay			IC50=1.24464 μM	SANGER
RS4-11	Growth Inhibition Assay			IC50=1.33886 μM	SANGER
DMS-114	Growth Inhibition Assay			IC50=1.36737 μM	SANGER
MSTO-211H	Growth Inhibition Assay			IC50=1.47378 μM	SANGER
DU-145	Growth Inhibition Assay			IC50=1.58217 μM	SANGER
A172	Growth Inhibition Assay			IC50=1.70355 μM	SANGER
SBC-1	Growth Inhibition Assay			IC50=2.094 μM	SANGER
H9	Growth Inhibition Assay			IC50=2.14306 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay			IC50=2.18394 μM	SANGER
NCI-H720	Growth Inhibition Assay			IC50=2.21283 μM	SANGER
HCC2218	Growth Inhibition Assay			IC50=2.37939 μM	SANGER
G-401	Growth Inhibition Assay			IC50=2.47189 μM	SANGER
MPP-89	Growth Inhibition Assay			IC50=2.48364 μM	SANGER
697	Growth Inhibition Assay			IC50=2.65331 μM	SANGER
KARPAS-45	Growth Inhibition Assay			IC50=2.70747 μM	SANGER
MG-63	Growth Inhibition Assay			IC50=2.94262 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay			IC50=3.03472 μM	SANGER
G-402	Growth Inhibition Assay			IC50=3.12727 μM	SANGER
NKM-1	Growth Inhibition Assay			IC50=3.13564 μM	SANGER
RH-18	Growth Inhibition Assay			IC50=3.19598 μM	SANGER
NCI-H1092	Growth Inhibition Assay			IC50=3.1969 μM	SANGER
RPMI-8226	Growth Inhibition Assay			IC50=3.23447 μM	SANGER
GAMG	Growth Inhibition Assay			IC50=3.46576 μM	SANGER
HH	Growth Inhibition Assay			IC50=3.47676 μM	SANGER
RO82-W-1	Growth Inhibition Assay			IC50=3.49855 μM	SANGER
CCRF-CEM	Growth Inhibition Assay			IC50=3.50488 μM	SANGER
NBsusSR	Growth Inhibition Assay			IC50=3.63969 μM	SANGER
CHL-1	Growth Inhibition Assay			IC50=3.65799 μM	SANGER
LK-2	Growth Inhibition Assay			IC50=3.67133 μM	SANGER
Hs-578-T	Growth Inhibition Assay			IC50=3.67873 μM	SANGER
CTB-1	Growth Inhibition Assay			IC50=3.80051 μM	SANGER
ES5	Growth Inhibition Assay			IC50=3.83637 μM	SANGER
A204	Growth Inhibition Assay			IC50=3.92075 μM	SANGER
SW780	Growth Inhibition Assay			IC50=3.92245 μM	SANGER
EW-3	Growth Inhibition Assay			IC50=3.98923 μM	SANGER
A704	Growth Inhibition Assay			IC50=4.28723 μM	SANGER
LU-139	Growth Inhibition Assay			IC50=4.31534 μM	SANGER
CAL-72	Growth Inhibition Assay			IC50=4.41746 μM	SANGER
D-336MG	Growth Inhibition Assay			IC50=4.46817 μM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=4.5331 μM	SANGER
GI-ME-N	Growth Inhibition Assay			IC50=4.5481 μM	SANGER
KM-H2	Growth Inhibition Assay			IC50=4.55222 μM	SANGER
NCI-H209	Growth Inhibition Assay			IC50=4.58283 μM	SANGER
IGROV-1	Growth Inhibition Assay			IC50=4.87168 μM	SANGER
L-363	Growth Inhibition Assay			IC50=4.96665 μM	SANGER
SK-MEL-3	Growth Inhibition Assay			IC50=5.2406 μM	SANGER
HuO9	Growth Inhibition Assay			IC50=5.38843 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=5.72927 μM	SANGER
NCI-H1770	Growth Inhibition Assay			IC50=5.95032 μM	SANGER
SF126	Growth Inhibition Assay			IC50=6.21406 μM	SANGER
ML-2	Growth Inhibition Assay			IC50=6.24977 μM	SANGER
CHP-134	Growth Inhibition Assay			IC50=6.25182 μM	SANGER
NCI-H1355	Growth Inhibition Assay			IC50=6.41733 μM	SANGER
TE-12	Growth Inhibition Assay			IC50=6.72671 μM	SANGER
A4-Fuk	Growth Inhibition Assay			IC50=6.73142 μM	SANGER
MV-4-11	Growth Inhibition Assay			IC50=6.76626 μM	SANGER
SK-UT-1	Growth Inhibition Assay			IC50=6.91784 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay			IC50=7.07764 μM	SANGER
ME-180	Growth Inhibition Assay			IC50=7.10404 μM	SANGER
SK-MEL-28	Growth Inhibition Assay			IC50=7.37819 μM	SANGER
HAL-01	Growth Inhibition Assay			IC50=7.48341 μM	SANGER
ES8	Growth Inhibition Assay			IC50=7.69626 μM	SANGER
DB	Growth Inhibition Assay			IC50=8.11504 μM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=8.48149 μM	SANGER
COR-L88	Growth Inhibition Assay			IC50=8.50981 μM	SANGER
LB1047-RCC	Growth Inhibition Assay			IC50=8.52212 μM	SANGER
NCI-H520	Growth Inhibition Assay			IC50=8.62157 μM	SANGER
SW954	Growth Inhibition Assay			IC50=8.69786 μM	SANGER
TE-6	Growth Inhibition Assay			IC50=8.75143 μM	SANGER
D-283MED	Growth Inhibition Assay			IC50=9.06534 μM	SANGER
DBTRG-05MG	Growth Inhibition Assay			IC50=9.09607 μM	SANGER
NCI-H446	Growth Inhibition Assay			IC50=9.29526 μM	SANGER
HOS	Growth Inhibition Assay			IC50=9.35134 μM	SANGER
ES4	Growth Inhibition Assay			IC50=9.50595 μM	SANGER
EW-13	Growth Inhibition Assay			IC50=9.89055 μM	SANGER
IST-MES1	Growth Inhibition Assay			IC50=9.94534 μM	SANGER
CAS-1	Growth Inhibition Assay			IC50=9.97659 μM	SANGER
EM-2	Growth Inhibition Assay			IC50=10.1393 μM	SANGER
SW948	Growth Inhibition Assay			IC50=10.1882 μM	SANGER
OAW-42	Growth Inhibition Assay			IC50=10.5267 μM	SANGER
BE-13	Growth Inhibition Assay			IC50=10.6576 μM	SANGER
KU812	Growth Inhibition Assay			IC50=10.7391 μM	SANGER
SK-MEL-30	Growth Inhibition Assay			IC50=10.8901 μM	SANGER
A2780	Growth Inhibition Assay			IC50=11.0308 μM	SANGER
TGBC24TKB	Growth Inhibition Assay			IC50=11.0737 μM	SANGER
GOTO	Growth Inhibition Assay			IC50=11.2084 μM	SANGER
NCI-H526	Growth Inhibition Assay			IC50=11.3837 μM	SANGER
BHT-101	Growth Inhibition Assay			IC50=11.4456 μM	SANGER
NCI-H1155	Growth Inhibition Assay			IC50=11.4947 μM	SANGER
MCF7	Growth Inhibition Assay			IC50=11.6167 μM	SANGER
MKN45	Growth Inhibition Assay			IC50=11.7993 μM	SANGER
MOLT-16	Growth Inhibition Assay			IC50=11.9692 μM	SANGER
YH-13	Growth Inhibition Assay			IC50=12.0346 μM	SANGER
P12-ICHIKAWA	Growth Inhibition Assay			IC50=12.3845 μM	SANGER
GR-ST	Growth Inhibition Assay			IC50=12.5295 μM	SANGER
CAKI-1	Growth Inhibition Assay			IC50=12.791 μM	SANGER
LXF-289	Growth Inhibition Assay			IC50=13.0835 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay			IC50=13.2704 μM	SANGER
EW-16	Growth Inhibition Assay			IC50=13.3187 μM	SANGER
NCI-H82	Growth Inhibition Assay			IC50=13.4195 μM	SANGER
MMAC-SF	Growth Inhibition Assay			IC50=13.4547 μM	SANGER
COLO-684	Growth Inhibition Assay			IC50=13.5318 μM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=13.8109 μM	SANGER
NB69	Growth Inhibition Assay			IC50=13.9868 μM	SANGER
NCI-H2291	Growth Inhibition Assay			IC50=14.4453 μM	SANGER
MKN7	Growth Inhibition Assay			IC50=14.6676 μM	SANGER
HDLM-2	Growth Inhibition Assay			IC50=15.1286 μM	SANGER
A253	Growth Inhibition Assay			IC50=15.3869 μM	SANGER
SK-LU-1	Growth Inhibition Assay			IC50=15.9094 μM	SANGER
MEG-01	Growth Inhibition Assay			IC50=15.9107 μM	SANGER
SK-N-DZ	Growth Inhibition Assay			IC50=15.9376 μM	SANGER
H4	Growth Inhibition Assay			IC50=16.088 μM	SANGER
LU-65	Growth Inhibition Assay			IC50=16.3384 μM	SANGER
NCI-H1048	Growth Inhibition Assay			IC50=16.5165 μM	SANGER
LCLC-97TM1	Growth Inhibition Assay			IC50=16.5889 μM	SANGER
CAL-120	Growth Inhibition Assay			IC50=16.9879 μM	SANGER
LU-134-A	Growth Inhibition Assay			IC50=17.3391 μM	SANGER
SK-MEL-1	Growth Inhibition Assay			IC50=17.7127 μM	SANGER
NCI-H69	Growth Inhibition Assay			IC50=17.9307 μM	SANGER
MC116	Growth Inhibition Assay			IC50=17.975 μM	SANGER
UMC-11	Growth Inhibition Assay			IC50=18.1788 μM	SANGER
HCC1395	Growth Inhibition Assay			IC50=18.4301 μM	SANGER
no-10	Growth Inhibition Assay			IC50=18.6388 μM	SANGER
NY	Growth Inhibition Assay			IC50=19.0809 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=19.1252 μM	SANGER
D-423MG	Growth Inhibition Assay			IC50=19.3952 μM	SANGER
LC-2-ad	Growth Inhibition Assay			IC50=19.7612 μM	SANGER
DU-4475	Growth Inhibition Assay			IC50=19.8852 μM	SANGER
YKG-1	Growth Inhibition Assay			IC50=19.962 μM	SANGER
HCC1569	Growth Inhibition Assay			IC50=20.2624 μM	SANGER
TYK-nu	Growth Inhibition Assay			IC50=20.2847 μM	SANGER
DEL	Growth Inhibition Assay			IC50=20.9808 μM	SANGER
MHH-ES-1	Growth Inhibition Assay			IC50=21.3597 μM	SANGER
KARPAS-299	Growth Inhibition Assay			IC50=21.529 μM	SANGER
CTV-1	Growth Inhibition Assay			IC50=21.6172 μM	SANGER
NCI-H2452	Growth Inhibition Assay			IC50=22.6677 μM	SANGER
D-566MG	Growth Inhibition Assay			IC50=22.7601 μM	SANGER
EFO-27	Growth Inhibition Assay			IC50=23.0651 μM	SANGER
NCI-H596	Growth Inhibition Assay			IC50=23.8527 μM	SANGER
KS-1	Growth Inhibition Assay			IC50=24.2759 μM	SANGER
8305C	Growth Inhibition Assay			IC50=24.4045 μM	SANGER
A427	Growth Inhibition Assay			IC50=25.0323 μM	SANGER
COLO-800	Growth Inhibition Assay			IC50=25.1061 μM	SANGER
SJRH30	Growth Inhibition Assay			IC50=25.3908 μM	SANGER
MEL-HO	Growth Inhibition Assay			IC50=25.4319 μM	SANGER
FTC-133	Growth Inhibition Assay			IC50=25.8186 μM	SANGER
SF295	Growth Inhibition Assay			IC50=26.296 μM	SANGER
SW1710	Growth Inhibition Assay			IC50=26.4123 μM	SANGER
EFM-19	Growth Inhibition Assay			IC50=26.8145 μM	SANGER
NB10	Growth Inhibition Assay			IC50=28.2297 μM	SANGER
TK10	Growth Inhibition Assay			IC50=28.2399 μM	SANGER
D-502MG	Growth Inhibition Assay			IC50=28.4 μM	SANGER
EW-18	Growth Inhibition Assay			IC50=28.4386 μM	SANGER
VMRC-RCZ	Growth Inhibition Assay			IC50=28.941 μM	SANGER
Ca9-22	Growth Inhibition Assay			IC50=29.4557 μM	SANGER
KYSE-70	Growth Inhibition Assay			IC50=29.5786 μM	SANGER
A101D	Growth Inhibition Assay			IC50=29.6472 μM	SANGER
WM-115	Growth Inhibition Assay			IC50=29.7607 μM	SANGER
HCC2157	Growth Inhibition Assay			IC50=29.8807 μM	SANGER
TE-9	Growth Inhibition Assay			IC50=29.8865 μM	SANGER
K-562	Growth Inhibition Assay			IC50=30.0933 μM	SANGER
SN12C	Growth Inhibition Assay			IC50=30.1426 μM	SANGER
ESS-1	Growth Inhibition Assay			IC50=30.4759 μM	SANGER
K5	Growth Inhibition Assay			IC50=30.764 μM	SANGER
J82	Growth Inhibition Assay			IC50=31.0897 μM	SANGER
HOP-92	Growth Inhibition Assay			IC50=31.1111 μM	SANGER
NCI-H2228	Growth Inhibition Assay			IC50=31.3296 μM	SANGER
OCI-AML2	Growth Inhibition Assay			IC50=31.361 μM	SANGER
NCI-SNU-5	Growth Inhibition Assay			IC50=31.8137 μM	SANGER
A3-KAW	Growth Inhibition Assay			IC50=31.9243 μM	SANGER
LCLC-103H	Growth Inhibition Assay			IC50=32.0171 μM	SANGER
KY821	Growth Inhibition Assay			IC50=32.6884 μM	SANGER
JVM-2	Growth Inhibition Assay			IC50=32.9079 μM	SANGER
Mo-T	Growth Inhibition Assay			IC50=33.1005 μM	SANGER
IA-LM	Growth Inhibition Assay			IC50=33.275 μM	SANGER
C8166	Growth Inhibition Assay			IC50=33.3192 μM	SANGER
TCCSUP	Growth Inhibition Assay			IC50=33.4307 μM	SANGER
JEG-3	Growth Inhibition Assay			IC50=33.4768 μM	SANGER
MS-1	Growth Inhibition Assay			IC50=33.5551 μM	SANGER
NCI-H1304	Growth Inhibition Assay			IC50=33.5725 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=34.0335 μM	SANGER
MDA-MB-453	Growth Inhibition Assay			IC50=34.6395 μM	SANGER
KYSE-520	Growth Inhibition Assay			IC50=34.7181 μM	SANGER
SW900	Growth Inhibition Assay			IC50=34.8115 μM	SANGER
HCC2998	Growth Inhibition Assay			IC50=35.1529 μM	SANGER
A2058	Growth Inhibition Assay			IC50=35.6061 μM	SANGER
OVCAR-3	Growth Inhibition Assay			IC50=36.2045 μM	SANGER
MOLT-4	Growth Inhibition Assay			IC50=36.2294 μM	SANGER
CAPAN-1	Growth Inhibition Assay			IC50=36.4699 μM	SANGER
SCC-9	Growth Inhibition Assay			IC50=37.4027 μM	SANGER
SF268	Growth Inhibition Assay			IC50=38.3433 μM	SANGER
HGC-27	Growth Inhibition Assay			IC50=38.3711 μM	SANGER
DOHH-2	Growth Inhibition Assay			IC50=38.7158 μM	SANGER
KE-37	Growth Inhibition Assay			IC50=38.9828 μM	SANGER
MOLT-13	Growth Inhibition Assay			IC50=39.2502 μM	SANGER
ES1	Growth Inhibition Assay			IC50=39.385 μM	SANGER
SK-OV-3	Growth Inhibition Assay			IC50=39.9643 μM	SANGER
SNU-449	Growth Inhibition Assay			IC50=40.0764 μM	SANGER
KYSE-510	Growth Inhibition Assay			IC50=40.1295 μM	SANGER
HL-60	Growth Inhibition Assay			IC50=40.9783 μM	SANGER
DJM-1	Growth Inhibition Assay			IC50=40.9799 μM	SANGER
TGBC11TKB	Growth Inhibition Assay			IC50=41.0926 μM	SANGER
U-2-OS	Growth Inhibition Assay			IC50=42.2641 μM	SANGER
NCI-H2030	Growth Inhibition Assay			IC50=42.4368 μM	SANGER
LU-135	Growth Inhibition Assay			IC50=42.5447 μM	SANGER
ZR-75-30	Growth Inhibition Assay			IC50=43.0493 μM	SANGER
GT3TKB	Growth Inhibition Assay			IC50=43.2679 μM	SANGER
RPMI-2650	Growth Inhibition Assay			IC50=43.7816 μM	SANGER
SAS	Growth Inhibition Assay			IC50=43.9534 μM	SANGER
MDA-MB-231	Growth Inhibition Assay			IC50=43.9609 μM	SANGER
JVM-3	Growth Inhibition Assay			IC50=44.0533 μM	SANGER
COLO-320-HSR	Growth Inhibition Assay			IC50=44.5633 μM	SANGER
SNB75	Growth Inhibition Assay			IC50=44.6105 μM	SANGER
NCI-H441	Growth Inhibition Assay			IC50=44.9328 μM	SANGER
HCT-116	Growth Inhibition Assay			IC50=44.9868 μM	SANGER
NCI-H226	Growth Inhibition Assay			IC50=45.6368 μM	SANGER
CAL-33	Growth Inhibition Assay			IC50=45.9217 μM	SANGER
NCI-H1437	Growth Inhibition Assay			IC50=46.321 μM	SANGER
HCC1187	Growth Inhibition Assay			IC50=46.4255 μM	SANGER
NUGC-3	Growth Inhibition Assay			IC50=46.5709 μM	SANGER
T98G	Growth Inhibition Assay			IC50=47.547 μM	SANGER
OVCAR-8	Growth Inhibition Assay			IC50=47.683 μM	SANGER
LB2241-RCC	Growth Inhibition Assay			IC50=47.727 μM	SANGER
NCI-H358	Growth Inhibition Assay			IC50=48.1152 μM	SANGER
PANC-08-13	Growth Inhibition Assay			IC50=48.1853 μM	SANGER
KP-N-YN	Growth Inhibition Assay			IC50=48.2102 μM	SANGER
NCI-H1755	Growth Inhibition Assay			IC50=48.2726 μM	SANGER
NCI-N87	Growth Inhibition Assay			IC50=48.2991 μM	SANGER
SUM52	Antiproliferative assay		5 days	Antiproliferative activity against human FGFR2-amplified SUM52 cells after 5 days by SRB assay, IC50 = 0.0123 μM.	28521156
RT112	Antiproliferative assay		72 hrs	Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay, GI50 = 0.015 μM.	27599742
insect cells	Function assay		10 mins	Inhibition of recombinant full length human FGFR1 expressed in baculovirus infected insect cells in presence of [gamma-32P]ATP after 10 mins by scintillation counting based radioactive filter binding assay, IC50 = 0.0215 μM.	27914362
SW780	Antiproliferative assay		5 days	Antiproliferative activity against human FGFR3-amplified SW780 cells after 5 days by SRB assay, IC50 = 0.0843 μM.	28521156
NIH/ 3T3	Function assay		5 mins	Inhibition of VEGFR2 (unknown origin) overexpressed in mouse NIH/ 3T3 cells incubated for 5 mins followed by stimulation with VEGF for 5 mins by immunoblotting analysis, IC50 = 0.1 μM.	27326339
NCI-H520	Antiproliferative assay		7 days	Antiproliferative activity against human FGFR1-amplified NCI-H520 cells after 7 days by SRB assay, IC50 = 0.281 μM.	28521156
HUVEC	Function assay	10 nM	14 hrs	Inhibition of FGFR-mediated angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at 10 nM after 14 hrs	16474387
HUVEC	Function assay	100 nM	14 hrs	Inhibition of FGFR-mediated angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at 100 nM after 14 hrs	16474387
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 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
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
fibroblast cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 105 mg/mL (200.5 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 105 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 40%PEG300 2 5%Tween80 3 53%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (5.73mM)	Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	523.67	Formula	C₂₈H₄₁N₇O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	219580-11-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C

Mechanism of Action

Targets/IC₅₀/Ki	FGFR1 (Cell-free assay) ~25 nM VEGFR2 (Cell-free assay) 100 nM-200 nM
In vitro	PD173074 is an ATP-competitive inhibitor of FGFR1 with K_i of ~40 nM. This compound is also an effective inhibitor of VEGFR2. Compared to FGFR1, it weakly inhibits the activities of Src, InsR, EGFR, PDGFR, MEK, and PKC with 1000-fold or greater IC50 values. This inhibitor inhibits autophosphorylation of FGFR1 and VEGFR2 in a dose-dependent manner with IC50 of 1-5 nM and 100-200 nM, respectively. It inhibits FGF-2 promotion of granule neuron survival in a dose-dependent manner with IC50 of 12 nM, exhibiting 1,000-fold greater potency than that of SU 5402. This chemical specifically inhibits FGF-2-mediated effects on proliferation, differentiation, and MAPK activation in oligodendrocyte (OL) lineage cells. It is active against the WT receptor and FGFR3 mutations in multiple myeloma (MM) cell lines. This compound also potently inhibits autophosphorylation of FGFR3 in a dose-dependent manner with IC50 of ~5 nM. Its treatment potently reduces viability of FGFR3-expressing KMS11 and KMS18 cells with IC50 of <20 nM. Inhibition of aFGF-stimulated MM cell growth by this agent is highly correlated with the expression of FGFR3. Its treatment completely abolishes NIH 3T3 transformation mediated by Y373C FGFR3 but not by Ras V12, demonstrating that it specifically targets FGFR3-mediated cell transformation and lacks nonspecific cytotoxic effect. This chemical also induces functional maturation of KMS11 and KMS18 cells.
Kinase Assay	In vitro kinase inhibition assays
Kinase Assay	Assays using the full-length FGFR-1 kinase are performed in a total volume of 100 μL containing 25 mM HEPES buffer (pH 7.4), 150 mM NaCl, 10 mM MnCl₂, 0.2 mM sodium orthovanadate, 750 μg/mL concentration of a random copolymer of glutamic acid and tyrosine (4:1), various concentrations of PD173074 and 60 to 75 ng of enzyme. The reaction is initiated by the addition of [γ-³²P]ATP (5 μM ATP containing 0.4 μCi of [γ-³²P]ATP per incubation), and samples are incubated at 25°C for 10 minutes. The reaction is terminated by the addition of 30% trichloroacetic acid and the precipitation of material onto glass-fiber filter mats. Filters are washed three times with 15% trichloroacetic acid, and the incorporation of [³²P] into the glutamate tyrosine polymer substrate is determined by counting the radioactivity retained on the filters in a Wallac 1250 betaplate reader. Nonspecific activity is defined as radioactivity retained on the filters following incubation of samples without enzyme. Specific activity is determined as total activity (enzyme plus buffer) minus nonspecific activity. The concentration of this compound that inhibits FGFR-1 enzymatic activity by 50% (IC50) is determined graphically.
In vivo	Administration of PD173074 at 1 mg/kg/day or 2 mg/ka/day in mice can effectively block angiogenesis induced by either FGF or VEGF in a dose-dependent manner with no apparent toxicity. This compound inhibits in vivo growth of mutant FGFR3-transfected NIH 3T3 cells in nude mice. Inhibition of FGFR3 by this chemical delays tumor growth and increases survival of mice in a KMS11 xenograft myeloma model. In the H-510 xenograft, oral aministration of this compound blocks tumor growth similar to that seen with single-agent cisplatin administration, increasing median survival compared with control sham-treated animals. In H-69 xenografts, this chemical induces complete responses lasting >6 months in 50% of mice. These effects are correlated with increased apoptosis in excised tumors, but not a consequence of disrupted tumor vasculature.
References	[1] https://pubmed.ncbi.nlm.nih.gov/9774334/ [2] https://pubmed.ncbi.nlm.nih.gov/10987832/ [3] https://pubmed.ncbi.nlm.nih.gov/14598292/ [4] https://pubmed.ncbi.nlm.nih.gov/14715624/ [5] https://pubmed.ncbi.nlm.nih.gov/19903855/ [6] https://pubmed.ncbi.nlm.nih.gov/23060048/

Applications

Methods	Biomarkers	Images	PMID
Western blot	pFGFR2 / FGFR2 p-S6RP / p-PRAS40 / p-p105 NFKB / P105 NFKB / P50 NFKB / p-AMPK / p-CRK II / p-PDK1		24968263
Growth inhibition assay	Cell viability		24968263

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Handling Instructions

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Frequently Asked Questions

Question 1:
What is the half-life of this compound (S1264) in vivo?

Answer:
According to literature research, it is given twice daily because this compound has a short half-life in vivo, please refer to the following link for detailed pharmacokinetic information (Supplementary Figure 8B): http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3990281/#!po=50.0000.

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