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 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPRUYpKSzVyPUCuNFEzOjVizszN M2DNPHNCVkeHUh?=
KG-1 NIPIdYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjybWl6UUN3ME2wMlA2OTJ7IN88US=> NHniWolUSU6JRWK=
MFM-223 NEPxeWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTBwMkG1O|Yh|ryP M4jqdXNCVkeHUh?=
EoL-1-cell M1e3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDjflRKSzVyPUCuN|I6QDRizszN Mn7SV2FPT0WU
ECC10 NX;pOpMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDTNXRiUUN3ME2wMlM{QDl6IN88US=> NGfndYJUSU6JRWK=
H-EMC-SS NGDRUoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHUWHBIUUN3ME2wMlM1PzF3IN88US=> M3PidHNCVkeHUh?=
AN3-CA MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYCxVWpFUUN3ME2wMlQxOTN|IN88US=> M2fFenNCVkeHUh?=
HuO-3N1 M4Xx[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LwPGlEPTB;MD61OFY2OyEQvF2= NWLjTWJLW0GQR1XS
RT-112 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonYTWM2OD1yLkW0O|AyKM7:TR?= MX7TRW5ITVJ?
NEC8 NIH6dlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV6xVI5JUUN3ME2wMlU3Ojh7IN88US=> MoDsV2FPT0WU
D-263MG M1nRc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vT[mlEPTB;MD63NVE2QSEQvF2= NG\UTldUSU6JRWK=
SW962 MkHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nkc2lEPTB;MD63PFk5QCEQvF2= MnvCV2FPT0WU
BV-173 NXnDdXhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PsfWlEPTB;MD64OFYzOyEQvF2= MUDTRW5ITVJ?
MFE-280 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HGeWlEPTB;MD64OVg4OiEQvF2= MonxV2FPT0WU
HuH-7 NGLzWmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LwXmlEPTB;MT6yOFQ3PCEQvF2= NYjrO|BbW0GQR1XS
RS4-11 NXzobIw2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTGOXdKSzVyPUGuN|M5QDZizszN NW\3d41pW0GQR1XS
DMS-114 M3LP[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[0NlJKSzVyPUGuN|Y4OzdizszN NEHYd4tUSU6JRWK=
MSTO-211H MoWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTFwNEezO|gh|ryP MWXTRW5ITVJ?
DU-145 M1HKVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnnTWM2OD1zLkW4NlE4KM7:TR?= M1e2ZXNCVkeHUh?=
A172 Ml7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXQTWM2OD1zLkewN|U2KM7:TR?= MYrTRW5ITVJ?
SBC-1 NUf1dWJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjHSG5KSzVyPUKuNFk1KM7:TR?= MYHTRW5ITVJ?
H9 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnUTWM2OD1{LkG0N|A3KM7:TR?= M1K4UXNCVkeHUh?=
NCI-SNU-1 Mn3YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPMNm5IUUN3ME2yMlE5Ozl2IN88US=> NUDZU|NRW0GQR1XS
NCI-H720 NFHiRoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTPUllSUUN3ME2yMlIyOjh|IN88US=> NVK2bVNuW0GQR1XS
HCC2218 NH:0e|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vWS2lEPTB;Mj6zO|k{QSEQvF2= NF\Eb4NUSU6JRWK=
G-401 NIro[WhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTJwNEexPFkh|ryP NUe3XmxwW0GQR1XS
MPP-89 NVvSRploT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHxTWM2OD1{LkS4N|Y1KM7:TR?= Ml;3V2FPT0WU
697 NWHM[IxFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\NTWM2OD1{Lk[1N|MyKM7:TR?= MVrTRW5ITVJ?
KARPAS-45 MnL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXW2S3U2UUN3ME2yMlcxPzR5IN88US=> MXnTRW5ITVJ?
MG-63 M3PhPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HqPWlEPTB;Mj65OFI3OiEQvF2= M3G0SXNCVkeHUh?=
NTERA-S-cl-D1 M3P5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjScGNKSzVyPUOuNFM1PzJizszN MXnTRW5ITVJ?
G-402 NFrYcnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13sfmlEPTB;Mz6xNlczPyEQvF2= MWHTRW5ITVJ?
NKM-1 NHu4No5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFOzWWpKSzVyPUOuNVM2PjRizszN MnezV2FPT0WU
RH-18 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PJe2lEPTB;Mz6xPVU6QCEQvF2= NHL1O5BUSU6JRWK=
NCI-H1092 Ml;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\0Um1KSzVyPUOuNVk3QSEQvF2= NUXqclJbW0GQR1XS
RPMI-8226 M2\0Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1naZmlEPTB;Mz6yN|Q1PyEQvF2= NFrxZXJUSU6JRWK=
GAMG MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLtTWM2OD1|LkS2OVc3KM7:TR?= NVrJO5l2W0GQR1XS
HH NIHtVGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDhTWM2OD1|LkS3Olc3KM7:TR?= NUnnfIJYW0GQR1XS
RO82-W-1 MkK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHK5U4dKSzVyPUOuOFk5PTVizszN NXjqeldqW0GQR1XS
CCRF-CEM NInlUo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXNVpFKSzVyPUOuOVA1QDhizszN NUXLRVJ2W0GQR1XS
NBsusSR NFfNNnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTNwNkO5Olkh|ryP M{PkdnNCVkeHUh?=
CHL-1 MlXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHjTWM2OD1|Lk[1O|k6KM7:TR?= Mk\TV2FPT0WU
LK-2 NFTBclVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\LVnNKSzVyPUOuOlcyOzNizszN M3:0SHNCVkeHUh?=
Hs-578-T NIXnVo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnuyTWM2OD1|Lk[3PFc{KM7:TR?= NFfLeWpUSU6JRWK=
CTB-1 NInJbYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWP3WmQyUUN3ME2zMlgxODVzIN88US=> NWPMb4syW0GQR1XS
ES5 NUjNRYZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\UTWM2OD1|LkizOlM4KM7:TR?= Mk[2V2FPT0WU
A204 NGDSd5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\D[2lEPTB;Mz65NlA4PSEQvF2= MUjTRW5ITVJ?
SW780 MmHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrzTWM2OD1|LkmyNlQ2KM7:TR?= MmXMV2FPT0WU
EW-3 M{m3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHf6dnNKSzVyPUOuPVg6OjNizszN MWHTRW5ITVJ?
A704 M3qwTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{P5OGlEPTB;ND6yPFczOyEQvF2= MkLmV2FPT0WU
LU-139 Mn22S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELB[Y5KSzVyPUSuN|E2OzRizszN Ml3hV2FPT0WU
CAL-72 NUT0TWJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG[1TGVKSzVyPUSuOFE4PDZizszN NYfEUolZW0GQR1XS
D-336MG MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTJ[HlKSzVyPUSuOFY5OTdizszN NGf0PIlUSU6JRWK=
LAMA-84 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTFOFFYUUN3ME20MlU{OzFizszN M{LFXXNCVkeHUh?=
GI-ME-N NIm3dlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LIT2lEPTB;ND61OFgyKM7:TR?= NFPyW4hUSU6JRWK=
KM-H2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LEOmlEPTB;ND61OVIzOiEQvF2= M4eyV3NCVkeHUh?=
NCI-H209 NF\NZ2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zVPGlEPTB;ND61PFI5OyEQvF2= NGrqPFdUSU6JRWK=
IGROV-1 Mnj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HFTGlEPTB;ND64O|E3QCEQvF2= MmXLV2FPT0WU
L-363 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTRwOU[2OlUh|ryP NWfuUYcyW0GQR1XS
SK-MEL-3 NGe1VJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ezNWlEPTB;NT6yOFA3KM7:TR?= MnvaV2FPT0WU
HuO9 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrETWM2OD13LkO4PFQ{KM7:TR?= MXjTRW5ITVJ?
NOS-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoewTWM2OD13LkeyPVI4KM7:TR?= Mk\uV2FPT0WU
NCI-H1770 Mm\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXNU3VKSzVyPUWuPVUxOzJizszN MUTTRW5ITVJ?
SF126 M{\1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;2SpNKSzVyPU[uNlE1ODZizszN NIrzfI1USU6JRWK=
ML-2 Mo[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jkPWlEPTB;Nj6yOFk4PyEQvF2= MoG0V2FPT0WU
CHP-134 NGjFVJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV:3Ump7UUN3ME22MlI2OTh{IN88US=> NH3xV4lUSU6JRWK=
NCI-H1355 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTGTWM2OD14LkSxO|M{KM7:TR?= MojKV2FPT0WU
TE-12 NXTNXVJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\LTWM2OD14LkeyOlcyKM7:TR?= NHnw[IhUSU6JRWK=
A4-Fuk NVnwO5FwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;zTWM2OD14LkezNVQzKM7:TR?= NVjrW2trW0GQR1XS
MV-4-11 NXiyWodoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jkPWlEPTB;Nj63OlYzPiEQvF2= NUe3NIQzW0GQR1XS
SK-UT-1 M2fremdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TJNGlEPTB;Nj65NVc5PCEQvF2= MUTTRW5ITVJ?
J-RT3-T3-5 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHq5foNKSzVyPUeuNFc4PjRizszN MYPTRW5ITVJ?
ME-180 NGmyRpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfPOVhKSzVyPUeuNVA1ODRizszN M2q4SHNCVkeHUh?=
SK-MEL-28 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojyTWM2OD15LkO3PFE6KM7:TR?= NE\qT3FUSU6JRWK=
HAL-01 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLWcVI6UUN3ME23MlQ5OzRzIN88US=> MVvTRW5ITVJ?
ES8 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2i5S2lEPTB;Nz62PVYzPiEQvF2= M3u0TXNCVkeHUh?=
DB Ml23S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnyXVdpUUN3ME24MlEyPTB2IN88US=> NXTm[2JkW0GQR1XS
SK-NEP-1 NWnuXXlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3ObJdXUUN3ME24MlQ5OTR7IN88US=> NXLofZp1W0GQR1XS
COR-L88 NXzCdGtVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jiO2lEPTB;OD61NFk5OSEQvF2= MnO5V2FPT0WU
LB1047-RCC MmjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrx[XFKSzVyPUiuOVIzOTJizszN MWDTRW5ITVJ?
NCI-H520 M1z5XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRThwNkKxOVch|ryP NWX1dWQ6W0GQR1XS
SW954 NEjRbmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{CzeGlEPTB;OD62PVc5PiEQvF2= MnfBV2FPT0WU
TE-6 NX7BSIxLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPsTHZ[UUN3ME24Mlc2OTR|IN88US=> NHLtdVBUSU6JRWK=
D-283MED M2DrZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUm5d3Z3UUN3ME25MlA3PTN2IN88US=> MYPTRW5ITVJ?
DBTRG-05MG MojTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7EcpFKSzVyPUmuNFk3ODdizszN MnnhV2FPT0WU
NCI-H446 MmDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3GTWM2OD17LkK5OVI3KM7:TR?= MmL6V2FPT0WU
HOS NEHDNJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTlwM{WxN|Qh|ryP M3uxPHNCVkeHUh?=
ES4 NH3LO|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTlwNUC1PVUh|ryP NYC4PZRyW0GQR1XS
EW-13 NIe5ZW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3T1[WlEPTB;OT64PVA2PSEQvF2= M2DScXNCVkeHUh?=
IST-MES1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnuwTWM2OD17Lkm0OVM1KM7:TR?= NYDzPZl1W0GQR1XS
CAS-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTlwOUe2OVkh|ryP NH;Db3VUSU6JRWK=
EM-2 NWHMNIExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFSwNoZKSzVyPUGwMlE{QTNizszN NX\xXIplW0GQR1XS
SW948 NX7QWGhzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\1fmlEPTB;MUCuNVg5OiEQvF2= M4LUfHNCVkeHUh?=
OAW-42 NX7ON|lxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTFyLkWyOlch|ryP NXz0N|htW0GQR1XS
BE-13 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHqeGhKUUN3ME2xNE43PTd4IN88US=> MoHCV2FPT0WU
KU812 NIOyV2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HUd2lEPTB;MUCuO|M6OSEQvF2= MYLTRW5ITVJ?
SK-MEL-30 M3jr[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2K0U2lEPTB;MUCuPFkxOSEQvF2= NInGRpdUSU6JRWK=
A2780 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rNZmlEPTB;MUGuNFMxQCEQvF2= M4THXHNCVkeHUh?=
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ZR-75-30 NIq1[HpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTXVJpKSzVyPUSzMlA1QTNizszN MWfTRW5ITVJ?
GT3TKB MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHRe4dKSzVyPUSzMlI3PzlizszN NEXId2FUSU6JRWK=
RPMI-2650 NVTIU5BlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzoTWM2OD12Mz63PFE3KM7:TR?= NWPKZlV1W0GQR1XS
SAS NIjZOXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTR|Lkm1N|Qh|ryP M3\N[HNCVkeHUh?=
MDA-MB-231 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2njd2lEPTB;NEOuPVYxQSEQvF2= MmDjV2FPT0WU
JVM-3 M4Lrb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3n3WGlEPTB;NESuNFU{OyEQvF2= NHTsUVlUSU6JRWK=
COLO-320-HSR NXPnTlFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTaTWM2OD12ND61OlM{KM7:TR?= MWrTRW5ITVJ?
SNB75 Mn3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIr4S2lKSzVyPUS0MlYyODVizszN MU\TRW5ITVJ?
NCI-H441 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInl[YxKSzVyPUS0Mlk{OjhizszN NXy4Z|d1W0GQR1XS
HCT-116 NUDm[|dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTBTZZKSzVyPUS0Mlk5PjhizszN NF;ISY9USU6JRWK=
NCI-H226 Ml\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLjTWM2OD12NT62N|Y5KM7:TR?= MlXLV2FPT0WU
CAL-33 M4C0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\LUmt2UUN3ME20OU46OjF5IN88US=> M134[XNCVkeHUh?=
NCI-H1437 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVe3ZXRvUUN3ME20Ok4{OjFizszN MnXoV2FPT0WU
HCC1187 NX\mTlk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHCTWM2OD12Nj60NlU2KM7:TR?= MVfTRW5ITVJ?
NUGC-3 NX7VdnYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEn4RoVKSzVyPUS2MlU4ODlizszN NXf1[olVW0GQR1XS
T98G NFL0UnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTR5LkW0O{DPxE1? MnXKV2FPT0WU
OVCAR-8 MnfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTR5Lk[4N{DPxE1? M1f4eHNCVkeHUh?=
LB2241-RCC NVP1dWJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XrbmlEPTB;NEeuO|I4KM7:TR?= NFuzUlJUSU6JRWK=
NCI-H358 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTR6LkGxOVIh|ryP Ml23V2FPT0WU
PANC-08-13 NGjMc4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTR6LkG4OVMh|ryP MkLXV2FPT0WU
KP-N-YN NV;FSFV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\RdHBKSzVyPUS4MlIyODJizszN MV3TRW5ITVJ?
NCI-H1755 NGPOV4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHKdY1KSzVyPUS4MlI4OjZizszN NEPKS3FUSU6JRWK=
NCI-N87 MnXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jx[GlEPTB;NEiuNlk6OSEQvF2= MoewV2FPT0WU

... 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
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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
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  • 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
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  • 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).

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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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Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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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Frequently Asked Questions

  • Question 1:

    What is the half-life of PD173074(S1264) in vivo?

  • Answer:

    According to literature research, PD173074 is given twice daily because it 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.

FGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID