PD173074

Licensed by Pfizer Catalog No.S1264

PD173074 Chemical Structure

Molecular Weight(MW): 523.67

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.

Size Price Stock Quantity  
In DMSO USD 98 In stock
USD 70 In stock
USD 120 In stock
USD 470 In stock

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6 Customer Reviews

  • The inhibitor PD173074 (A) or PD184352 (B) was administered to one uterine horn of Hand2d/d mice on day 3 of pregnancy (n = 5). The other horn served as vehicle-treated control. Uterine horns were collected on the morning of day 4, and sections were subjected to IHC to detect p-FRS2, p-ERK1/2, and Ki-67. (C) IHC of pERa and Muc-1 in uterine sections of Hand2d/d mice treated with PD173074 or PD184352.

    Science 2011 331(6019), 912-6. PD173074 purchased from Selleck.

    Inhibition of FGFR signaling pathway by FGFR inhibitor PD173074 in mouse xenograft tumors. Bladder cancer SW780 cells were implanted in mice and treated with PD173074 after tumor formation as shown in B. Protein lysates of tumor tissues were prepared and immunoblotted with antibodies against phospho-ERK1/2, pan-ERK1/2, and γ-tubulin.

    Cancer Discov 2013 3(6), 636-47. PD173074 purchased from Selleck.

  • FGFR inhibitors block signaling in FGFR2-fusion-expressing cells. Activation of FGFR2 and MAPK by FGFR2-AHCYL1 and its suppression by FGFR inhibitors. Lysates from NIH3T3 cells expressing FGFR2-AHCYL1 or EZR-ROS1 (control) treated with vehicle (DMSO), 0.2 and 1 uM BGJ398, and 0.2 and 1 uM PD173074 were immunoblotted with the relevant antibodies. β-Actin was used as a loading control.

    Hepatology 2014 59(4) ,1427-34. PD173074 purchased from Selleck.

    The level of p-FRS2 was examined in the uterine sections of Msx1f/fMsx2f/f (upper panel) and Msx1d/dMsx2d/d (lower panel) mice on day 4 of pregnancy by immunohistochemistry. Magnification: a and d: 10 x, b and e: 20 x, c and f: 40x. FGFR-specific inhibitor PD173074 was applied to one uterine horn of Msx1d/dMsx2d/d (n = 3) mice on day 3 of pregnancy. The other horn served as vehicle-treated control. Uterine horns were collected on day 4 morning and sections were subjected to immunohistochemistry to detect p-FRS2, Ki67, and Muc-1.

    PLoS Genet 2012 8(2), e1002500. PD173074 purchased from Selleck.

  • Effect of select kinase inhibitors on DF508-CFTR maturation analyzed by immunoblotting. 293MSR-GT cells stably expressing DF508-CFTR were treated with 15 uM kinase inhibitors or 0.3% DMSO (vehicle control), as indicated, grown at 37 ℃ for 48 h, and the appearance of the mature protein, band C, monitored by immunoblotting with anti-CFTR antibodies. Band B represents the immature protein. DMSO represents vehicle- alone control, 27℃ represents temperature rescue of F508-CFTR at 27℃, 37℃ represents untreated DF508-CFTR control, and WT represents WT-CFTR. Top panels depict the anti-CFTR immunoblot and bottom panels depict actin (loading) control. ** represents cellular toxicity.

    Biochem Bioph Res Co 2012 11(9), 745-57. PD173074 purchased from Selleck.

    Cells were incubated with DMSO control, 10 uM TGFBR inhibitor or 10 uM FGFR inhibitor PD173074 for 1 h. Cells were fixed, labeled with anti-GM130 (red) and analyzed by confocal microscopy. Images were analyzed using Image J (n = 3 experiments, >100 cells per condition). Scale bars, 10 uM.

    J Cell Sci 2014 10.1242/jcs.159608. PD173074 purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description 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.
Targets
FGFR1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
c-Src [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
Insulin Receptor [1]
(Cell-free assay)
~25 nM 100 nM-200 nM 19.8 μM >50 μM >50 μM
In vitro

PD173074 is an ATP-competitive inhibitor of FGFR1 with Ki of ~40 nM. PD173074 is also an effective inhibitor of VEGFR2. Compared to FGFR1, PD173074 weakly inhibits the activities of Src, InsR, EGFR, PDGFR, MEK, and PKC with 1000-fold or greater IC50 values. PD173074 inhibits autophosphorylation of FGFR1 and VEGFR2 in a dose-dependent manner with IC50 of 1-5 nM and 100-200 nM, respectively. [1] PD173074 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. [2] PD173074 specifically inhibits FGF-2-mediated effects on proliferation, differentiation, and MAPK activation in oligodendrocyte (OL) lineage cells. [3] PD173074 is active against the WT receptor and FGFR3 mutations in multiple myeloma (MM) cell lines. PD173074 also potently inhibits autophosphorylation of FGFR3 in a dose-dependent manner with IC50 of ~5 nM. PD173074 treatment potently reduces viability of FGFR3-expressing KMS11 and KMS18 cells with IC50 of <20 nM. Inhibition of aFGF-stimulated MM cell growth by PD173074 is highly correlated with the expression of FGFR3. PD173074 treatment completely abolishes NIH 3T3 transformation mediated by Y373C FGFR3 but not by Ras V12, demonstrating that PD173074 specifically targets FGFR3-mediated cell transformation and lacks nonspecific cytotoxic effect. PD173074 also induces functional maturation of KMS11 and KMS18 cells. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1581 NEW3[YtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\jTWM2OD1yLkCxNlI2KM7:TR?= NV72[YpEW0GQR1XS
KG-1 M1zUOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPITWM2OD1yLkC1NVI6KM7:TR?= MX3TRW5ITVJ?
MFM-223 NYLjT2FMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjqbW1LUUN3ME2wMlIyPTd4IN88US=> Mn3jV2FPT0WU
EoL-1-cell MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWH0[YNzUUN3ME2wMlMzQTh2IN88US=> MVPTRW5ITVJ?
ECC10 MnjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LHZmlEPTB;MD6zN|g6QCEQvF2= NVvoZ5Y2W0GQR1XS
H-EMC-SS MnrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTBwM{S3NVUh|ryP MojoV2FPT0WU
AN3-CA NWOwVnBpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLTepRoUUN3ME2wMlQxOTN|IN88US=> NEX4OJdUSU6JRWK=
HuO-3N1 NEDKWWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPYTWM2OD1yLkW0OlU{KM7:TR?= M{nvNXNCVkeHUh?=
RT-112 MmLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3OT4xwUUN3ME2wMlU1PzBzIN88US=> M1:xNHNCVkeHUh?=
NEC8 MkjRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTBwNU[yPFkh|ryP M3TUfXNCVkeHUh?=
D-263MG NEHSfHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXJTWM2OD1yLkexNVU6KM7:TR?= Mo\WV2FPT0WU
SW962 M37UOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLHTWM2OD1yLke4PVg5KM7:TR?= NXr2WZNLW0GQR1XS
BV-173 NF;kTZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnQRlRKSzVyPUCuPFQ3OjNizszN Moq1V2FPT0WU
MFE-280 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{n3fWlEPTB;MD64OVg4OiEQvF2= NX7URo9tW0GQR1XS
HuH-7 NX7xV3lnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;MZlVKSzVyPUGuNlQ1PjRizszN NW\4N2tqW0GQR1XS
RS4-11 MkTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrueGRqUUN3ME2xMlM{QDh4IN88US=> MoXUV2FPT0WU
DMS-114 NXPhOGRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn70TWM2OD1zLkO2O|M4KM7:TR?= M1PtSXNCVkeHUh?=
MSTO-211H MlqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGK5O2lKSzVyPUGuOFc{PzhizszN NGjVSZBUSU6JRWK=
DU-145 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;LcoFQUUN3ME2xMlU5OjF5IN88US=> MXLTRW5ITVJ?
A172 MkjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7jTWM2OD1zLkewN|U2KM7:TR?= M3TWZnNCVkeHUh?=
SBC-1 NWS5dJZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TxUWlEPTB;Mj6wPVQh|ryP MofRV2FPT0WU
H9 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTJwMUSzNFYh|ryP M1LVPHNCVkeHUh?=
NCI-SNU-1 NUnhc24xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjzdYVKSzVyPUKuNVg{QTRizszN MULTRW5ITVJ?
NCI-H720 MkLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTJwMkGyPFMh|ryP M1\S[nNCVkeHUh?=
HCC2218 NHHKU4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTJwM{e5N|kh|ryP MXPTRW5ITVJ?
G-401 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLjTWM2OD1{LkS3NVg6KM7:TR?= NInoXHVUSU6JRWK=
MPP-89 NIrEPYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTJwNEizOlQh|ryP NV;x[IY4W0GQR1XS
697 MkfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrJWJVKSzVyPUKuOlU{OzFizszN NHjHb21USU6JRWK=
KARPAS-45 MmroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTJwN{C3OFch|ryP NGLYbpFUSU6JRWK=
MG-63 MnnaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnO1TWM2OD1{Lkm0NlYzKM7:TR?= NVXzOWU2W0GQR1XS
NTERA-S-cl-D1 NXTJcopiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTNwMEO0O|Ih|ryP M{j4NnNCVkeHUh?=
G-402 M2TWPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnwTmlKSzVyPUOuNVI4OjdizszN MUPTRW5ITVJ?
NKM-1 NX3LOpFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PFOGlEPTB;Mz6xN|U3PCEQvF2= NIXqO2hUSU6JRWK=
RH-18 NXjZdHhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTNwMUm1PVgh|ryP M3zKVXNCVkeHUh?=
NCI-H1092 Mn\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfXTWM2OD1|LkG5Olkh|ryP MmjUV2FPT0WU
RPMI-8226 MnnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTNwMkO0OFch|ryP NIWyfJZUSU6JRWK=
GAMG MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrYSGVKSzVyPUOuOFY2PzZizszN NUXUNVV2W0GQR1XS
HH MnrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1S0[mlEPTB;Mz60O|Y4PiEQvF2= Mn7BV2FPT0WU
RO82-W-1 M1TLXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlftTWM2OD1|LkS5PFU2KM7:TR?= MXvTRW5ITVJ?
CCRF-CEM NVrEZYM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\ScFZKSzVyPUOuOVA1QDhizszN NFW4OpRUSU6JRWK=
NBsusSR MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fpSWlEPTB;Mz62N|k3QSEQvF2= M{LmOXNCVkeHUh?=
CHL-1 NFL1SItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTNwNkW3PVkh|ryP NGHaN|dUSU6JRWK=
LK-2 NWPXdot4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFn3UGxKSzVyPUOuOlcyOzNizszN NGexe|RUSU6JRWK=
Hs-578-T M3\KRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF2wWYFKSzVyPUOuOlc5PzNizszN NGe1bJVUSU6JRWK=
CTB-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTNwOECwOVEh|ryP MXnTRW5ITVJ?
ES5 NXHyb|NKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzpb5FKSzVyPUOuPFM3OzdizszN M{DXe3NCVkeHUh?=
A204 MoHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTNwOUKwO|Uh|ryP NH7CRXBUSU6JRWK=
SW780 M37VcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HkbmlEPTB;Mz65NlI1PSEQvF2= MoewV2FPT0WU
EW-3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTNwOUi5NlMh|ryP MmnqV2FPT0WU
A704 M2\6T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7Oe5pPUUN3ME20MlI5PzJ|IN88US=> NEDpdIVUSU6JRWK=
LU-139 MkjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGf5fWRKSzVyPUSuN|E2OzRizszN M3vGS3NCVkeHUh?=
CAL-72 MmHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTRwNEG3OFYh|ryP Ml\HV2FPT0WU
D-336MG NEnQeYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3GTWM2OD12LkS2PFE4KM7:TR?= NXrNW3VRW0GQR1XS
LAMA-84 M1jK[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDqTWM2OD12LkWzN|Eh|ryP Mn[3V2FPT0WU
GI-ME-N M{XrWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LyW2lEPTB;ND61OFgyKM7:TR?= NXq1NYZDW0GQR1XS
KM-H2 NHXGR|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVqyVXNwUUN3ME20MlU2OjJ{IN88US=> MYjTRW5ITVJ?
NCI-H209 NFKxWZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnETWM2OD12LkW4Nlg{KM7:TR?= NIruOI1USU6JRWK=
IGROV-1 MoH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XYSmlEPTB;ND64O|E3QCEQvF2= NEDMNmVUSU6JRWK=
L-363 NIe4Rm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTRwOU[2OlUh|ryP M4jJNXNCVkeHUh?=
SK-MEL-3 NGXZS21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPufZA4UUN3ME21MlI1ODZizszN NUTmTWdQW0GQR1XS
HuO9 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mny4TWM2OD13LkO4PFQ{KM7:TR?= M{nVZXNCVkeHUh?=
NOS-1 NGPIZZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrpXGxjUUN3ME21MlczQTJ5IN88US=> M2rjNXNCVkeHUh?=
NCI-H1770 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfQTWM2OD13Lkm1NFMzKM7:TR?= M120S3NCVkeHUh?=
SF126 M4LHc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rMOWlEPTB;Nj6yNVQxPiEQvF2= M{C0N3NCVkeHUh?=
ML-2 MorFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvoN3VKSzVyPU[uNlQ6PzdizszN NYfkXIFSW0GQR1XS
CHP-134 NEnnR4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3FW|ZpUUN3ME22MlI2OTh{IN88US=> NX\aeW9rW0GQR1XS
NCI-H1355 MnG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTZwNEG3N|Mh|ryP NWq0[4VOW0GQR1XS
TE-12 MofyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHYXIlnUUN3ME22MlczPjdzIN88US=> NYfEUIRUW0GQR1XS
A4-Fuk NUnVNokyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj5cXZKSzVyPU[uO|MyPDJizszN MX7TRW5ITVJ?
MV-4-11 NYfpRmhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnXTWM2OD14Lke2OlI3KM7:TR?= NV\ieodOW0GQR1XS
SK-UT-1 NWH5UYpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3S1dGlEPTB;Nj65NVc5PCEQvF2= M4fZUXNCVkeHUh?=
J-RT3-T3-5 NVf0U|RoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVeycIJrUUN3ME23MlA4PzZ2IN88US=> MVTTRW5ITVJ?
ME-180 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLNSo9IUUN3ME23MlExPDB2IN88US=> M{HiWnNCVkeHUh?=
SK-MEL-28 M{CzVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzoSY9LUUN3ME23MlM4QDF7IN88US=> NF;0VYJUSU6JRWK=
HAL-01 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTdwNEizOFEh|ryP NXzJeIdIW0GQR1XS
ES8 M1jkO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTdwNkm2NlYh|ryP NFO3TIVUSU6JRWK=
DB NV22[Jc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LIU2lEPTB;OD6xNVUxPCEQvF2= NF;pfpdUSU6JRWK=
SK-NEP-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PweWlEPTB;OD60PFE1QSEQvF2= NUC1PZdOW0GQR1XS
COR-L88 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTJUW1KSzVyPUiuOVA6QDFizszN MkHUV2FPT0WU
LB1047-RCC M3LnZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHoTWM2OD16LkWyNlEzKM7:TR?= MU\TRW5ITVJ?
NCI-H520 MoizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDiS4xKSzVyPUiuOlIyPTdizszN NE\zR4VUSU6JRWK=
SW954 NVPuO2U4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\VNXFKSzVyPUiuOlk4QDZizszN NFvQZWVUSU6JRWK=
TE-6 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3iyW2lEPTB;OD63OVE1OyEQvF2= M{TuWHNCVkeHUh?=
D-283MED MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTlwME[1N|Qh|ryP NYXQbpVuW0GQR1XS
DBTRG-05MG MmS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXCTWM2OD17LkC5OlA4KM7:TR?= MYrTRW5ITVJ?
NCI-H446 MknyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzrPYVLUUN3ME25MlI6PTJ4IN88US=> MoDSV2FPT0WU
HOS M4ryWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PtfGlEPTB;OT6zOVE{PCEQvF2= NHHBNnpUSU6JRWK=
ES4 NHjLXZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnMXHdKSzVyPUmuOVA2QTVizszN MknXV2FPT0WU
EW-13 MkTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYf3bmpoUUN3ME25Mlg6ODV3IN88US=> NVfZboNpW0GQR1XS
IST-MES1 M3zFPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;5SJB3UUN3ME25Mlk1PTN2IN88US=> NGPkPWdUSU6JRWK=
CAS-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTHTWM2OD17Lkm3OlU6KM7:TR?= MnrsV2FPT0WU
EM-2 NV3JNHBlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\ITWM2OD1zMD6xN|k{KM7:TR?= M3m2VXNCVkeHUh?=
SW948 NF7tNmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTFyLkG4PFIh|ryP MlzvV2FPT0WU
OAW-42 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTFyLkWyOlch|ryP NXvNSXE4W0GQR1XS
BE-13 NWHr[4FYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DkS2lEPTB;MUCuOlU4PiEQvF2= MlTpV2FPT0WU
KU812 MkXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDGPYdKSzVyPUGwMlc{QTFizszN NUHCdXNSW0GQR1XS
SK-MEL-30 NUPhZlFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mly5TWM2OD1zMD64PVAyKM7:TR?= MnX6V2FPT0WU
A2780 M3K2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjnZlVKSzVyPUGxMlA{ODhizszN MnrRV2FPT0WU
TGBC24TKB NGjXd3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvMV|lXUUN3ME2xNU4xPzN5IN88US=> MlHXV2FPT0WU
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NCI-H1304 Mk\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLqfpJEUUN3ME2zN{42PzJ3IN88US=> M{XMTXNCVkeHUh?=
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NCI-H2030 M{W5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2O4VGlEPTB;NEKuOFM3QCEQvF2= M3PVVHNCVkeHUh?=
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ZR-75-30 NE\4TFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XNSWlEPTB;NEOuNFQ6OyEQvF2= M2nLdHNCVkeHUh?=
GT3TKB MlrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTR|LkK2O|kh|ryP NUHaZ21KW0GQR1XS
RPMI-2650 NFjYO29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvNdJc3UUN3ME20N{44QDF4IN88US=> MYLTRW5ITVJ?
SAS NHfET|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvXTWM2OD12Mz65OVM1KM7:TR?= M1LDNHNCVkeHUh?=
MDA-MB-231 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jW[mlEPTB;NEOuPVYxQSEQvF2= NFj3Z4pUSU6JRWK=
JVM-3 M{H2bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXsN|NQUUN3ME20OE4xPTN|IN88US=> MYTTRW5ITVJ?
COLO-320-HSR NHrBUm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTR2LkW2N|Mh|ryP MXzTRW5ITVJ?
SNB75 M3ftOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHMOXNKSzVyPUS0MlYyODVizszN NE\xUZhUSU6JRWK=
NCI-H441 MoXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUD1bm1ZUUN3ME20OE46OzJ6IN88US=> NY\vTIhUW0GQR1XS
HCT-116 MlHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHYTWM2OD12ND65PFY5KM7:TR?= M2Tz[3NCVkeHUh?=
NCI-H226 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTR3Lk[zOlgh|ryP MkK0V2FPT0WU
CAL-33 M1\Pb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPGcpBIUUN3ME20OU46OjF5IN88US=> MnKxV2FPT0WU
NCI-H1437 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWq5R4RmUUN3ME20Ok4{OjFizszN Ml32V2FPT0WU
HCC1187 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWW5fmoyUUN3ME20Ok41OjV3IN88US=> M{D3VnNCVkeHUh?=
NUGC-3 NEPNPXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPxe4hIUUN3ME20Ok42PzB7IN88US=> MWXTRW5ITVJ?
T98G NGPkOoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrtTWM2OD12Nz61OFch|ryP MoflV2FPT0WU
OVCAR-8 NIDHVWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\BTWM2OD12Nz62PFMh|ryP NWHufHNNW0GQR1XS
LB2241-RCC NUTQRVF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3H5Z2lEPTB;NEeuO|I4KM7:TR?= NF3F[3lUSU6JRWK=
NCI-H358 NUHacYxWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTR6LkGxOVIh|ryP M3r5PHNCVkeHUh?=
PANC-08-13 Mn25S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTR6LkG4OVMh|ryP NHvCUpZUSU6JRWK=
KP-N-YN NGrNdVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXaTWM2OD12OD6yNVAzKM7:TR?= NEHFW29USU6JRWK=
NCI-H1755 Mn:4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjSR25KSzVyPUS4MlI4OjZizszN MW\TRW5ITVJ?
NCI-N87 NX\KSolYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;4VHVqUUN3ME20PE4zQTlzIN88US=> MW\TRW5ITVJ?

... Click to View More Cell Line Experimental Data

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. [1] PD173074 inhibits in vivo growth of mutant FGFR3-transfected NIH 3T3 cells in nude mice. Inhibition of FGFR3 by PD173074 delays tumor growth and increases survival of mice in a KMS11 xenograft myeloma model. [4] In the H-510 xenograft, oral aministration of PD173074 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, PD173074 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. [5]

Protocol

Kinase Assay:[1]
+ Expand

In vitro kinase inhibition assays:

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 PD173074 that inhibits FGFR-1 enzymatic activity by 50% (IC50) is determined graphically.
Cell Research:[4]
+ Expand
  • Cell lines: KMS11 and KMS18
  • Concentrations: Dissolved in DMSO, final concentrations ~100 nM
  • Incubation Time: 48 hours
  • Method: Cells are incubated with increasing concentrations of PD173074 in the presence of aFGF/heparin for 48 hours. The percentage of viable cells is determined by MTT.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Swiss Webster mice with induced corneal angiogenesis
  • Formulation: Prepared in sterile fashion
  • Dosages: ~2 mg/kg/day
  • Administration: Administered intraperitoneally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (190.95 mM)
Ethanol 100 mg/mL (190.95 mM)
Water <1 mg/mL
In vivo 5% DMSO+corn oil 15mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 523.67
Formula

C28H41N7O3

CAS No. 219580-11-7
Storage powder
in solvent
Synonyms N/A

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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*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 )

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* 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

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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

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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

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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