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.

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In DMSO USD 98 In stock
USD 70 In stock
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USD 470 In stock
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7 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.

  • Effects of antagonists for RAGE (FPS-ZM), TLR-4 (TAK-242) and FGFR1 (PD and BGJ) on the S100B-induced alterations in glucose metabolism in L6 cells treated for 6 h. (A) Effects of FPS-ZM, (B) TAK-242 and (C) PD and BGJ on the S100B inhibition of glucose consumption.

    Am J Physiol Endocrinol Metab, 2017. PD173074 purchased from Selleck.

Purity & Quality Control

Choose Selective FGFR Inhibitors

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)
~25 nM 100 nM-200 nM
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 MlXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTpfnlNUUN3ME2wMlAyOjJ3IN88US=> NXrseHppW0GQR1XS
KG-1 NVyyfZhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWG2[oI{UUN3ME2wMlA2OTJ7IN88US=> NUPvcVJrW0GQR1XS
MFM-223 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfUToRKSzVyPUCuNlE2PzZizszN Mon2V2FPT0WU
EoL-1-cell NEn0e49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVO0NJVxUUN3ME2wMlMzQTh2IN88US=> MoLaV2FPT0WU
ECC10 M2n0NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rrfGlEPTB;MD6zN|g6QCEQvF2= MnnEV2FPT0WU
H-EMC-SS NEP4RmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwM{S3NVUh|ryP NEnuUpBUSU6JRWK=
AN3-CA MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{m3OmlEPTB;MD60NFE{OyEQvF2= M2e5O3NCVkeHUh?=
HuO-3N1 NGflNYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFn4U45KSzVyPUCuOVQ3PTNizszN NXTCdHQ3W0GQR1XS
RT-112 M2jZUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[wTWM2OD1yLkW0O|AyKM7:TR?= M4r0XXNCVkeHUh?=
NEC8 NHLGW3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NImwU5JKSzVyPUCuOVYzQDlizszN NIHRe5ZUSU6JRWK=
D-263MG MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TPO2lEPTB;MD63NVE2QSEQvF2= Ml\JV2FPT0WU
SW962 NWi1VGhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUn6b4loUUN3ME2wMlc5QTh6IN88US=> M2f0TXNCVkeHUh?=
BV-173 Mn;MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDkTWM2OD1yLki0OlI{KM7:TR?= M4fZeHNCVkeHUh?=
MFE-280 M{DaPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfyXZdKSzVyPUCuPFU5PzJizszN NFXaXZBUSU6JRWK=
HuH-7 NUSwcnBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fnVGlEPTB;MT6yOFQ3PCEQvF2= M3TUVXNCVkeHUh?=
RS4-11 Ml3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTFwM{O4PFYh|ryP NIXmcVFUSU6JRWK=
DMS-114 NELxeWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPD[4tKSzVyPUGuN|Y4OzdizszN MYHTRW5ITVJ?
MSTO-211H NWjNO21OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPGTWM2OD1zLkS3N|c5KM7:TR?= NXvjW3JDW0GQR1XS
DU-145 NHXuUIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUftOZN4UUN3ME2xMlU5OjF5IN88US=> MWTTRW5ITVJ?
A172 MmjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTFwN{CzOVUh|ryP MoPsV2FPT0WU
SBC-1 Mlz3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFL2VIlKSzVyPUKuNFk1KM7:TR?= NHvJT4RUSU6JRWK=
H9 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrWTWM2OD1{LkG0N|A3KM7:TR?= NYrZcGNkW0GQR1XS
NCI-SNU-1 M{Locmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jKeWlEPTB;Mj6xPFM6PCEQvF2= M1KzS3NCVkeHUh?=
NCI-H720 NWLQcIFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzLemFKSzVyPUKuNlEzQDNizszN M2LXV3NCVkeHUh?=
HCC2218 NYDTelRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHGxd2NKSzVyPUKuN|c6OzlizszN NEXyNFBUSU6JRWK=
G-401 M{\YSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfSSotYUUN3ME2yMlQ4OTh7IN88US=> MkXjV2FPT0WU
MPP-89 NX;YZo9NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTJwNEizOlQh|ryP Mn;0V2FPT0WU
697 NGTSPGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzTWo1KSzVyPUKuOlU{OzFizszN Mmm3V2FPT0WU
KARPAS-45 M4j2dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlKzTWM2OD1{LkewO|Q4KM7:TR?= M3\IPXNCVkeHUh?=
MG-63 NUTQVYJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnG2TWM2OD1{Lkm0NlYzKM7:TR?= M1mwd3NCVkeHUh?=
NTERA-S-cl-D1 NUjycGppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3K3RmlEPTB;Mz6wN|Q4OiEQvF2= NE\zSJBUSU6JRWK=
G-402 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHricIZKSzVyPUOuNVI4OjdizszN MoG1V2FPT0WU
NKM-1 M4T5fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moj2TWM2OD1|LkGzOVY1KM7:TR?= NHnmflBUSU6JRWK=
RH-18 Ml3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGq5WY9KSzVyPUOuNVk2QThizszN M17ZWnNCVkeHUh?=
NCI-H1092 NG\ISZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTNwMUm2PUDPxE1? MYPTRW5ITVJ?
RPMI-8226 NFTCcmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTNwMkO0OFch|ryP NIH4SlNUSU6JRWK=
GAMG NGGwZWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlq2TWM2OD1|LkS2OVc3KM7:TR?= NGj4VmFUSU6JRWK=
HH M1jOTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2T0[2lEPTB;Mz60O|Y4PiEQvF2= NHizcVdUSU6JRWK=
RO82-W-1 NHjTXmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjWUZBHUUN3ME2zMlQ6QDV3IN88US=> MUjTRW5ITVJ?
CCRF-CEM MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\ZXGdKSzVyPUOuOVA1QDhizszN NFflNIFUSU6JRWK=
NBsusSR NFG2UYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzFTWM2OD1|Lk[zPVY6KM7:TR?= M4ric3NCVkeHUh?=
CHL-1 M{fldGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LHTWlEPTB;Mz62OVc6QSEQvF2= Mle1V2FPT0WU
LK-2 NH;udmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3yzc2lEPTB;Mz62O|E{OyEQvF2= MmPvV2FPT0WU
Hs-578-T NEnaPYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkj3TWM2OD1|Lk[3PFc{KM7:TR?= NV3rWFBFW0GQR1XS
CTB-1 NXrlcWFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGG3NI9KSzVyPUOuPFAxPTFizszN Ml3SV2FPT0WU
ES5 NIPM[mVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYj0enltUUN3ME2zMlg{PjN5IN88US=> NH3wR|lUSU6JRWK=
A204 M2PVNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrEPJRKSzVyPUOuPVIxPzVizszN M3TDPHNCVkeHUh?=
SW780 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTNwOUKyOFUh|ryP NUT3XYg6W0GQR1XS
EW-3 MmnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETvdXNKSzVyPUOuPVg6OjNizszN MmW4V2FPT0WU
A704 M{\lTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTRwMki3NlMh|ryP MmfBV2FPT0WU
LU-139 M1;wN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXQTWM2OD12LkOxOVM1KM7:TR?= M{LG[nNCVkeHUh?=
CAL-72 NUX3UIR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTRwNEG3OFYh|ryP MmXDV2FPT0WU
D-336MG MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGS4NZhKSzVyPUSuOFY5OTdizszN NHroR4RUSU6JRWK=
LAMA-84 MlrES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPa[VlKSzVyPUSuOVM{OSEQvF2= NEXDdYVUSU6JRWK=
GI-ME-N M{XQN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;6TWM2OD12LkW0PFEh|ryP NF\Gd2NUSU6JRWK=
KM-H2 M3zpVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHpTWM2OD12LkW1NlIzKM7:TR?= NXvuS4Q6W0GQR1XS
NCI-H209 NG\jXIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7VPFBKSzVyPUSuOVgzQDNizszN MXPTRW5ITVJ?
IGROV-1 NEC3cWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTRwOEexOlgh|ryP MVjTRW5ITVJ?
L-363 MmPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzjOGlKSzVyPUSuPVY3PjVizszN Mn3DV2FPT0WU
SK-MEL-3 NXjjS5V1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLCR4dKSzVyPUWuNlQxPiEQvF2= NXOzV4QyW0GQR1XS
HuO9 NWPmd2hkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TTSmlEPTB;NT6zPFg1OyEQvF2= MmHuV2FPT0WU
NOS-1 NIPQXVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPFUXZMUUN3ME21MlczQTJ5IN88US=> MmrMV2FPT0WU
NCI-H1770 MmrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvrXVVwUUN3ME21Mlk2ODN{IN88US=> M{\mNXNCVkeHUh?=
SF126 MnnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlG1TWM2OD14LkKxOFA3KM7:TR?= MYLTRW5ITVJ?
ML-2 M{fLcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jEc2lEPTB;Nj6yOFk4PyEQvF2= NUjLXFBHW0GQR1XS
CHP-134 NYPXeldOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjjfWRKSzVyPU[uNlUyQDJizszN M{e1SHNCVkeHUh?=
NCI-H1355 NIThOmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTZwNEG3N|Mh|ryP MV7TRW5ITVJ?
TE-12 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTZwN{K2O|Eh|ryP NE\jcIVUSU6JRWK=
A4-Fuk M125emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrs[|VsUUN3ME22Mlc{OTR{IN88US=> M{HnNHNCVkeHUh?=
MV-4-11 MmPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTZwN{[2NlYh|ryP NW\4[oFnW0GQR1XS
SK-UT-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGD3fGdKSzVyPU[uPVE4QDRizszN M4fFfXNCVkeHUh?=
J-RT3-T3-5 NF7qfFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGi4WWpKSzVyPUeuNFc4PjRizszN MnjsV2FPT0WU
ME-180 NYjD[HZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2i2bmlEPTB;Nz6xNFQxPCEQvF2= NWH5[pN1W0GQR1XS
SK-MEL-28 MkTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTdwM{e4NVkh|ryP NV;qdXU5W0GQR1XS
HAL-01 NXW2OFVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvwTWM2OD15LkS4N|QyKM7:TR?= MmTYV2FPT0WU
ES8 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{T5emlEPTB;Nz62PVYzPiEQvF2= NX\JfHBsW0GQR1XS
DB MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVH5[|dTUUN3ME24MlEyPTB2IN88US=> MmHVV2FPT0WU
SK-NEP-1 NVfFeY0zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRThwNEixOFkh|ryP NV:4OmppW0GQR1XS
COR-L88 MmfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XOVWlEPTB;OD61NFk5OSEQvF2= NYDnXHhFW0GQR1XS
LB1047-RCC NVXScmdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPrOHA1UUN3ME24MlUzOjF{IN88US=> MmnDV2FPT0WU
NCI-H520 NXyxRW9rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRThwNkKxOVch|ryP NH\ISJRUSU6JRWK=
SW954 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGi1coJKSzVyPUiuOlk4QDZizszN MkTPV2FPT0WU
TE-6 MkiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVe4UogxUUN3ME24Mlc2OTR|IN88US=> NHv6UHVUSU6JRWK=
D-283MED MoD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4raS2lEPTB;OT6wOlU{PCEQvF2= NXzYSG1EW0GQR1XS
DBTRG-05MG MmLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HH[2lEPTB;OT6wPVYxPyEQvF2= NW[4epJlW0GQR1XS
NCI-H446 MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTlwMkm1NlYh|ryP NWfGd5drW0GQR1XS
HOS M{\aN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnu4TWM2OD17LkO1NVM1KM7:TR?= NGjh[HpUSU6JRWK=
ES4 Mnu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3:2UmlEPTB;OT61NFU6PSEQvF2= M{XURXNCVkeHUh?=
EW-13 MoLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1[2eWlEPTB;OT64PVA2PSEQvF2= MUfTRW5ITVJ?
IST-MES1 NWD5TYNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITXOFVKSzVyPUmuPVQ2OzRizszN M4SwXXNCVkeHUh?=
CAS-1 M4Xt[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jzS2lEPTB;OT65O|Y2QSEQvF2= Mn7GV2FPT0WU
EM-2 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnLPFJ4UUN3ME2xNE4yOzl|IN88US=> MlzGV2FPT0WU
SW948 NVXxUlVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rBXGlEPTB;MUCuNVg5OiEQvF2= MmPXV2FPT0WU
OAW-42 NXHlc5NLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXryXVNCUUN3ME2xNE42OjZ5IN88US=> NFXMU5VUSU6JRWK=
BE-13 M{nC[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTFyLk[1O|Yh|ryP MVvTRW5ITVJ?
KU812 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPhUmlKSzVyPUGwMlc{QTFizszN MWPTRW5ITVJ?
SK-MEL-30 NHHqNm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTFyLki5NFEh|ryP NWPPZWVqW0GQR1XS
A2780 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXq4NYNpUUN3ME2xNU4xOzB6IN88US=> MWHTRW5ITVJ?
TGBC24TKB NHnLNFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fvemlEPTB;MUGuNFc{PyEQvF2= Mn;nV2FPT0WU
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RPMI-2650 MnX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jXSWlEPTB;NEOuO|gyPiEQvF2= MoGzV2FPT0WU
SAS NYHlNYVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTR|Lkm1N|Qh|ryP M2r0RXNCVkeHUh?=
MDA-MB-231 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXrTWM2OD12Mz65OlA6KM7:TR?= MV3TRW5ITVJ?
JVM-3 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWj1fZl4UUN3ME20OE4xPTN|IN88US=> M4jNNnNCVkeHUh?=
COLO-320-HSR MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLzVJRKSzVyPUS0MlU3OzNizszN M3nmXXNCVkeHUh?=
SNB75 NX\HUpdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHQTWM2OD12ND62NVA2KM7:TR?= NU[wfXVvW0GQR1XS
NCI-H441 NEHWdolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TwXmlEPTB;NESuPVMzQCEQvF2= M1q2WnNCVkeHUh?=
HCT-116 M2LuUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTR2Lkm4Olgh|ryP NVTMTYtmW0GQR1XS
NCI-H226 NW\TeGxZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LYdGlEPTB;NEWuOlM3QCEQvF2= MlviV2FPT0WU
CAL-33 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTR3LkmyNVch|ryP M3yyenNCVkeHUh?=
NCI-H1437 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7sSlZKSzVyPUS2MlMzOSEQvF2= NFfTfWNUSU6JRWK=
HCC1187 NUTtfpFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnyTWM2OD12Nj60NlU2KM7:TR?= MlnXV2FPT0WU
NUGC-3 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mle5TWM2OD12Nj61O|A6KM7:TR?= MXTTRW5ITVJ?
T98G MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTR5LkW0O{DPxE1? MnXiV2FPT0WU
OVCAR-8 NUH4W2V[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTR5Lk[4N{DPxE1? M1jzeHNCVkeHUh?=
LB2241-RCC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXqSm9KSzVyPUS3MlczPyEQvF2= MoixV2FPT0WU
NCI-H358 NEPWOnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXlTWM2OD12OD6xNVUzKM7:TR?= Ml\ZV2FPT0WU
PANC-08-13 M1raR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DnO2lEPTB;NEiuNVg2OyEQvF2= NImwcnhUSU6JRWK=
KP-N-YN MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTR6LkKxNFIh|ryP Mn\HV2FPT0WU
NCI-H1755 NVfJbmJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTR6LkK3NlYh|ryP NXPue3luW0GQR1XS
NCI-N87 NWDN[IROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\zPGNLUUN3ME20PE4zQTlzIN88US=> MUnTRW5ITVJ?

... 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]
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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:[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 Insoluble
In vivo Add solvents individually and in order:
5% DMSO+corn oil
15mg/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 523.67
Formula

C28H41N7O3

CAS No. 219580-11-7
Storage powder
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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* 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

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

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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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