PD173074

Pfizer辉瑞授权 目录号:S1264

PD173074 Chemical Structure

Molecular Weight(MW): 523.67

PD173074是一种有效的FGFR1抑制剂,在无细胞试验中IC50约为25 nM,也能抑制VEGFR2,IC50为100-200 nM,作用于FGFR1比作用于PDGFR和c-Src选择性高1000倍左右。

规格 价格 库存 购买数量  
RMB 802.11 现货
RMB 575.36 现货
RMB 985.04 现货
RMB 3867.14 现货
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客户使用该产品的7个实验数据:

  • 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, 312(6):E471-E481. PD173074 purchased from Selleck.

产品安全说明书

FGFR抑制剂选择性比较

生物活性

产品描述 PD173074是一种有效的FGFR1抑制剂,在无细胞试验中IC50约为25 nM,也能抑制VEGFR2,IC50为100-200 nM,作用于FGFR1比作用于PDGFR和c-Src选择性高1000倍左右。
靶点
FGFR1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
~25 nM 100 nM-200 nM
体外研究

PD173074是FGFR1的ATP竞争性抑制剂, Ki约为40 nM。PD173074也是VEGFR2的有效抑制剂。相比FGFR1,PD173074弱抑制Src,INSR,EGFR,PDGFR,MEK和PKC的活性,IC 50值大1000倍以上。PD173074剂量依赖性地抑制FGFR1和VEGFR2的自身磷酸化,IC50 分别为1-5 nM和100-200 nM。[1] PD173074以剂量依赖的方式抑制FGF-2促进的颗粒神经元存活,IC50是12 nM,活性是SU 5402的1,000倍以上。[2] D173074特异性地抑制FGF-2-介导的少突胶质细胞(OL)谱系细胞的细胞增殖,分化和MAPK激活。[3] 在多发性骨髓瘤(MM)细胞系中,PD173074对野生受体和FGFR3突变有活性。PD173074还以剂量依赖的方式有效地抑制FGFR3的自磷酸化,IC50约为5 nM。PD173074有力地降低了表达FGFR3的KMS11细胞和KMS18细胞的活力,IC50小于20 nM。aFGF刺激的MM细胞生长受PD173074抑制是和FGFR3的表达高度相关的。PD173074完全抑制由Y373C FGFR3介导而不是的Ras介导的NIH 3T3转化,这表明PD173074专门针对FGFR3基因介导的细胞转化和缺乏非特异性的细胞毒性作用。PD173074也诱导KMS11和KMS18细胞功能成熟。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1581 M2XrXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvrbVNKSzVyPUCuNFEzOjVizszN NWTRUI5mW0GQR1XS
KG-1 NHz2VFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlKwTWM2OD1yLkC1NVI6KM7:TR?= NYDYTI85W0GQR1XS
MFM-223 NXPUWmVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPzclhKSzVyPUCuNlE2PzZizszN NWrMdHloW0GQR1XS
EoL-1-cell MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zSSWlEPTB;MD6zNlk5PCEQvF2= NHzJOpBUSU6JRWK=
ECC10 NVe2[5lRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vBdWlEPTB;MD6zN|g6QCEQvF2= MWTTRW5ITVJ?
H-EMC-SS NHHaNlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPLcI9KSzVyPUCuN|Q4OTVizszN MXrTRW5ITVJ?
AN3-CA NInvUmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknWTWM2OD1yLkSwNVM{KM7:TR?= M17QXnNCVkeHUh?=
HuO-3N1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvwVVRFUUN3ME2wMlU1PjV|IN88US=> M2XIXXNCVkeHUh?=
RT-112 NWjsdpViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXz6O2MxUUN3ME2wMlU1PzBzIN88US=> MVnTRW5ITVJ?
NEC8 MnqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWG0cIc5UUN3ME2wMlU3Ojh7IN88US=> MU\TRW5ITVJ?
D-263MG NGTtUlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzMTWM2OD1yLkexNVU6KM7:TR?= MoXSV2FPT0WU
SW962 NHvRdXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTWTWM2OD1yLke4PVg5KM7:TR?= M13CbXNCVkeHUh?=
BV-173 MlnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHH5XW9KSzVyPUCuPFQ3OjNizszN MlL5V2FPT0WU
MFE-280 M2PxPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PW[mlEPTB;MD64OVg4OiEQvF2= Mmi4V2FPT0WU
HuH-7 NUjDbZRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnz3TWM2OD1zLkK0OFY1KM7:TR?= NV3sWFI4W0GQR1XS
RS4-11 NFPTVoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7UWHZWUUN3ME2xMlM{QDh4IN88US=> NWnjeo9VW0GQR1XS
DMS-114 M37VcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFwM{[3N|ch|ryP MWrTRW5ITVJ?
MSTO-211H MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DWTGlEPTB;MT60O|M4QCEQvF2= M1XT[3NCVkeHUh?=
DU-145 M3TydWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\4WYRKSzVyPUGuOVgzOTdizszN M4T0fXNCVkeHUh?=
A172 MmfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDPTWM2OD1zLkewN|U2KM7:TR?= M3XvfXNCVkeHUh?=
SBC-1 NFjhOFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUL0bY1PUUN3ME2yMlA6PCEQvF2= M2j2cHNCVkeHUh?=
H9 M3njbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlr6TWM2OD1{LkG0N|A3KM7:TR?= M{XsT3NCVkeHUh?=
NCI-SNU-1 NUHLSVdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTJwMUizPVQh|ryP NVLGZoo3W0GQR1XS
NCI-H720 NXm1PHh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTJwMkGyPFMh|ryP M{LIPXNCVkeHUh?=
HCC2218 M4n0S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37PTGlEPTB;Mj6zO|k{QSEQvF2= NHu1dGVUSU6JRWK=
G-401 MoC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTJwNEexPFkh|ryP MnzuV2FPT0WU
MPP-89 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITQOGRKSzVyPUKuOFg{PjRizszN NW\VUHVCW0GQR1XS
697 MkHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnzTWM2OD1{Lk[1N|MyKM7:TR?= Ml3jV2FPT0WU
KARPAS-45 NWHjT2ljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfOOlM5UUN3ME2yMlcxPzR5IN88US=> Mo\oV2FPT0WU
MG-63 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33xZWlEPTB;Mj65OFI3OiEQvF2= MULTRW5ITVJ?
NTERA-S-cl-D1 M{nr[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2r5PWlEPTB;Mz6wN|Q4OiEQvF2= MnXJV2FPT0WU
G-402 NX7nOmtZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3u3OWlEPTB;Mz6xNlczPyEQvF2= M{XqWnNCVkeHUh?=
NKM-1 MlHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnDb2ZIUUN3ME2zMlE{PTZ2IN88US=> MorTV2FPT0WU
RH-18 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzUTWM2OD1|LkG5OVk5KM7:TR?= MXPTRW5ITVJ?
NCI-H1092 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHmTWM2OD1|LkG5Olkh|ryP NYnsW|ZDW0GQR1XS
RPMI-8226 M{S4Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmP4TWM2OD1|LkKzOFQ4KM7:TR?= M1vPZXNCVkeHUh?=
GAMG M4fHNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTNwNE[1O|Yh|ryP MWrTRW5ITVJ?
HH NYnL[XlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTNwNEe2O|Yh|ryP NGjaNZpUSU6JRWK=
RO82-W-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTNwNEm4OVUh|ryP MmHlV2FPT0WU
CCRF-CEM MlrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTqeGxzUUN3ME2zMlUxPDh6IN88US=> Mmr4V2FPT0WU
NBsusSR NX7SZYJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rnZ2lEPTB;Mz62N|k3QSEQvF2= Mkn2V2FPT0WU
CHL-1 NVWxcIZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3wTWM2OD1|Lk[1O|k6KM7:TR?= M3H4TXNCVkeHUh?=
LK-2 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF72SWNKSzVyPUOuOlcyOzNizszN NIr2XmpUSU6JRWK=
Hs-578-T NXf0UI5RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlexTWM2OD1|Lk[3PFc{KM7:TR?= M4\ITHNCVkeHUh?=
CTB-1 MlnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPmTWM2OD1|LkiwNFUyKM7:TR?= MXXTRW5ITVJ?
ES5 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PqdmlEPTB;Mz64N|Y{PyEQvF2= Mln1V2FPT0WU
A204 M4K3bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTNwOUKwO|Uh|ryP MVLTRW5ITVJ?
SW780 NF\3TWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHJTWM2OD1|LkmyNlQ2KM7:TR?= M3r1eXNCVkeHUh?=
EW-3 NUfENFJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\iT|hKSzVyPUOuPVg6OjNizszN M4njTnNCVkeHUh?=
A704 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrZPYlvUUN3ME20MlI5PzJ|IN88US=> M4L6VnNCVkeHUh?=
LU-139 NEjDcGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGWwXWpKSzVyPUSuN|E2OzRizszN MWjTRW5ITVJ?
CAL-72 Mn[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVmyeFZUUUN3ME20MlQyPzR4IN88US=> MXLTRW5ITVJ?
D-336MG M3fXemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrTNohKSzVyPUSuOFY5OTdizszN NFe4bHJUSU6JRWK=
LAMA-84 NEHYW21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTKfmdzUUN3ME20MlU{OzFizszN NUPwbZBCW0GQR1XS
GI-ME-N NHvQfWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTRwNUS4NUDPxE1? MWLTRW5ITVJ?
KM-H2 NX30XFlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\jTWM2OD12LkW1NlIzKM7:TR?= NYPhTI1EW0GQR1XS
NCI-H209 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDSS|FDUUN3ME20MlU5Ojh|IN88US=> M{TkfXNCVkeHUh?=
IGROV-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELjfGtKSzVyPUSuPFcyPjhizszN M2To[XNCVkeHUh?=
L-363 NXTkXldlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\qVWlEPTB;ND65OlY3PSEQvF2= NIPCb2NUSU6JRWK=
SK-MEL-3 MnO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPwOlVKSzVyPUWuNlQxPiEQvF2= NVqzdWFFW0GQR1XS
HuO9 Ml3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnGyTWM2OD13LkO4PFQ{KM7:TR?= NXvUcIpFW0GQR1XS
NOS-1 NYrPZ3hkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfB[ZFKSzVyPUWuO|I6OjdizszN NEOyWINUSU6JRWK=
NCI-H1770 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFe0WIlKSzVyPUWuPVUxOzJizszN NXrkNm9xW0GQR1XS
SF126 NX;ONmFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jlb2lEPTB;Nj6yNVQxPiEQvF2= M4DOPXNCVkeHUh?=
ML-2 Mnj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7uR4dKSzVyPU[uNlQ6PzdizszN NGDIfYJUSU6JRWK=
CHP-134 NULROnl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTZwMkWxPFIh|ryP MkD4V2FPT0WU
NCI-H1355 NF3nNXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIf0[VBKSzVyPU[uOFE4OzNizszN MWnTRW5ITVJ?
TE-12 NYTBd3I1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjXeGh7UUN3ME22MlczPjdzIN88US=> MlvCV2FPT0WU
A4-Fuk MlvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1P3RmlEPTB;Nj63N|E1OiEQvF2= NHjOTIhUSU6JRWK=
MV-4-11 MkXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjQWJJEUUN3ME22Mlc3PjJ4IN88US=> MUjTRW5ITVJ?
SK-UT-1 M1f6cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1K0PWlEPTB;Nj65NVc5PCEQvF2= Mm\WV2FPT0WU
J-RT3-T3-5 M4D0Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTdwMEe3OlQh|ryP MWnTRW5ITVJ?
ME-180 M2rKOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;MR2lEPTB;Nz6xNFQxPCEQvF2= NYTFPZNzW0GQR1XS
SK-MEL-28 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDWTFFiUUN3ME23MlM4QDF7IN88US=> NU\odlZ7W0GQR1XS
HAL-01 M2DYTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nnUWlEPTB;Nz60PFM1OSEQvF2= NGW0U3BUSU6JRWK=
ES8 NGHxeI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTmXoJKSzVyPUeuOlk3OjZizszN MortV2FPT0WU
DB NFGzPWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvFcnlKSzVyPUiuNVE2ODRizszN MlO1V2FPT0WU
SK-NEP-1 NVTyVGNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRThwNEixOFkh|ryP NIHDZpFUSU6JRWK=
COR-L88 NWKxbI56T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRThwNUC5PFEh|ryP NX\WeXRxW0GQR1XS
LB1047-RCC NXS5VHJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRThwNUKyNVIh|ryP NVTYXoNzW0GQR1XS
NCI-H520 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfaTWM2OD16Lk[yNVU4KM7:TR?= MV7TRW5ITVJ?
SW954 NWf6UXU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRThwNkm3PFYh|ryP NGD2eHNUSU6JRWK=
TE-6 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XweWlEPTB;OD63OVE1OyEQvF2= MnfwV2FPT0WU
D-283MED MlLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\yVJBCUUN3ME25MlA3PTN2IN88US=> M{LDV3NCVkeHUh?=
DBTRG-05MG MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4K4XWlEPTB;OT6wPVYxPyEQvF2= MlT2V2FPT0WU
NCI-H446 NUO0[GJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnztTWM2OD17LkK5OVI3KM7:TR?= NXfLe5RKW0GQR1XS
HOS MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTlwM{WxN|Qh|ryP NGq4OHdUSU6JRWK=
ES4 M{XOWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVK4cHBHUUN3ME25MlUxPTl3IN88US=> M2fybnNCVkeHUh?=
EW-13 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3Jc|ZqUUN3ME25Mlg6ODV3IN88US=> NV7jTJVCW0GQR1XS
IST-MES1 NYHqNXg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYraWXNZUUN3ME25Mlk1PTN2IN88US=> NV21NVZmW0GQR1XS
CAS-1 NHPhTnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrzTWM2OD17Lkm3OlU6KM7:TR?= NYn6dGN1W0GQR1XS
EM-2 M1nDV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:0N3dWUUN3ME2xNE4yOzl|IN88US=> NWf6VHVRW0GQR1XS
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NCI-H2228 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mle5TWM2OD1|MT6zNlk3KM7:TR?= M2nNWHNCVkeHUh?=
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KYSE-510 NHj3PJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoC3TWM2OD12MD6xNlk2KM7:TR?= Mor6V2FPT0WU
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DJM-1 NWO4SpZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGn3WWVKSzVyPUSwMlk4QTlizszN MYPTRW5ITVJ?
TGBC11TKB MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTRzLkC5NlYh|ryP NFPDfZFUSU6JRWK=
U-2-OS M1nqfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnv4TWM2OD12Mj6yOlQyKM7:TR?= NXm4XWZ7W0GQR1XS
NCI-H2030 NH\OR4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV6zWmVyUUN3ME20Nk41OzZ6IN88US=> MUHTRW5ITVJ?
LU-135 NYG5bpNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTR{LkW0OFch|ryP M3\GN3NCVkeHUh?=
ZR-75-30 NGXN[nZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDBVIJUUUN3ME20N{4xPDl|IN88US=> NYrrXmx1W0GQR1XS
GT3TKB MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHOwZ2RKSzVyPUSzMlI3PzlizszN M3T6PHNCVkeHUh?=
RPMI-2650 M{TNb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\aNnpwUUN3ME20N{44QDF4IN88US=> NGjMV4xUSU6JRWK=
SAS MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HrW2lEPTB;NEOuPVU{PCEQvF2= MkH0V2FPT0WU
MDA-MB-231 NUjMd5lOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjLXVFKSzVyPUSzMlk3ODlizszN M4G5R3NCVkeHUh?=
JVM-3 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTR2LkC1N|Mh|ryP MnzpV2FPT0WU
COLO-320-HSR NXriXHBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTR2LkW2N|Mh|ryP MUDTRW5ITVJ?
SNB75 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTR2Lk[xNFUh|ryP NELsSFRUSU6JRWK=
NCI-H441 M1H3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTR2LkmzNlgh|ryP M1rldXNCVkeHUh?=
HCT-116 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfPTWM2OD12ND65PFY5KM7:TR?= NHz3d2FUSU6JRWK=
NCI-H226 NGm0ZVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LiSmlEPTB;NEWuOlM3QCEQvF2= NVPXbo9jW0GQR1XS
CAL-33 Mo\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLlRYJrUUN3ME20OU46OjF5IN88US=> NWO3ZZYyW0GQR1XS
NCI-H1437 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPnS|ZYUUN3ME20Ok4{OjFizszN NXHkXpV{W0GQR1XS
HCC1187 NGixWI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLFbZpKSzVyPUS2MlQzPTVizszN NXq3WmdYW0GQR1XS
NUGC-3 NXPoOmdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjNe2J5UUN3ME20Ok42PzB7IN88US=> NV;KU212W0GQR1XS
T98G MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTR5LkW0O{DPxE1? Mlv3V2FPT0WU
OVCAR-8 NHriW2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofYTWM2OD12Nz62PFMh|ryP NHrTbllUSU6JRWK=
LB2241-RCC MmrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHP4OXBKSzVyPUS3MlczPyEQvF2= NWm0fFAyW0GQR1XS
NCI-H358 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTR6LkGxOVIh|ryP M2nyS3NCVkeHUh?=
PANC-08-13 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmL3TWM2OD12OD6xPFU{KM7:TR?= NVfqUWo{W0GQR1XS
KP-N-YN NUPBRVl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTR6LkKxNFIh|ryP NG\KTnZUSU6JRWK=
NCI-H1755 NYXufIxVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LkXGlEPTB;NEiuNlczPiEQvF2= MX;TRW5ITVJ?
NCI-N87 NGDhSVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlf6TWM2OD12OD6yPVkyKM7:TR?= MkPaV2FPT0WU

... Click to View More Cell Line Experimental Data

体内研究 PD173074在1 mg/kg/day或2 mg/ka/day对小鼠给药可以剂量依赖性的方式有效阻止由FGF或VEGF诱导的血管生成,并没有明显的毒性。[1] PD173074抑制FGFR3突变体转染的NIH 3T3细胞在裸鼠体内生长。在KMS11异种移植瘤模型中,PD173074抑制FGFR3导致肿瘤生长延缓,小鼠的存活率提高。[4] 在H-510异种移植体中,PD173074阻断肿瘤生长和cisplatin相似,与对照假治疗的动物相比增加中位生存期。在H-69异种移植体中,PD173074在50%小鼠中的诱导作用长于6个月。这些效应是和切除肿瘤中增加的细胞凋亡相关的,而非破坏肿瘤血管。[5]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
+ 展开

体外激酶抑制试验:

检测是使用全长FGFR-1激酶在100微升含25 mM HEPES缓冲液(pH7.4),150 mM氯化钠,10 mM MnCl2,0.2 mM的原钒酸钠,750 μg/mL谷氨酸和酪氨酸(4:1)的无规共聚物,各种浓度的PD173074,和60至75 ng酶中进行的。该反应通过加入[γ-32P]ATP(含有0.4 μCi of [γ-32P]ATP的5 μM ATP)起始,样品在25°C孵育10分钟。反应通过加入30%三氯乙酸和材料的沉淀到玻璃纤维滤垫上终止。过滤器用15%三氯乙酸洗涤三次,掺入[32P]到谷氨酸酪氨酸聚合物衬底是通过计算保留在过滤器上的放射性来确定,通过WALLAC1250 betaplate阅读器读取。非特异性的活性被定义为温育不含酶的样品保留在过滤器上放射性。特异活性被确定为总活性(酶加缓冲液)减去非特异性活性。PD173074抑制FGFR-1的酶活性的IC50浓度用图解法测定。
细胞实验:[4]
+ 展开
  • Cell lines: KMS11和 KMS18
  • Concentrations: 溶解在DMSO中至终浓度~100 nM
  • Incubation Time: 48小时
  • Method: 在aFGF/肝素的存在下,细胞在PD173074浓度梯度中孵育48小时。活细胞的百分比由MTT法检测。
    (Only for Reference)
动物实验:[1]
+ 展开
  • Animal Models: 诱导角膜新生血管的瑞士韦伯斯特小鼠
  • Formulation: 无菌准备
  • Dosages: 约2 mg/kg/day
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (190.95 mM)
Ethanol 100 mg/mL (190.95 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用:
5% DMSO+corn oil
15mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 523.67
化学式

C28H41N7O3

CAS号 219580-11-7
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

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

  • 回答:

    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

FGFR Inhibitors with Unique Features

相关FGFR产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID