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。

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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 Ml;jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGn2RWNKSzVyPUCuNFEzOjVizszN NWOwOpI4W0GQR1XS
KG-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTBwMEWxNlkh|ryP MXjTRW5ITVJ?
MFM-223 NIjOVm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknPTWM2OD1yLkKxOVc3KM7:TR?= NEnBNINUSU6JRWK=
EoL-1-cell MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTBwM{K5PFQh|ryP M2rpTHNCVkeHUh?=
ECC10 Ml3yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTBwM{O4PVgh|ryP MVXTRW5ITVJ?
H-EMC-SS NH\uU4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTBwM{S3NVUh|ryP M4KxdHNCVkeHUh?=
AN3-CA MnjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGSyN4JKSzVyPUCuOFAyOzNizszN NVj4TmZvW0GQR1XS
HuO-3N1 M{XVfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfXNWppUUN3ME2wMlU1PjV|IN88US=> MUTTRW5ITVJ?
RT-112 NFXkXm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXP6fJduUUN3ME2wMlU1PzBzIN88US=> NY\POVFGW0GQR1XS
NEC8 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHVb4NKSzVyPUCuOVYzQDlizszN NHLjS2NUSU6JRWK=
D-263MG NUC4UZlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7R[|ZKUUN3ME2wMlcyOTV7IN88US=> Mn\jV2FPT0WU
SW962 MkLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXuwVFFqUUN3ME2wMlc5QTh6IN88US=> MYLTRW5ITVJ?
BV-173 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfrcGk2UUN3ME2wMlg1PjJ|IN88US=> NUDRNJVYW0GQR1XS
MFE-280 MlriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnqSWVKSzVyPUCuPFU5PzJizszN NXLJelh4W0GQR1XS
HuH-7 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTFwMkS0OlQh|ryP NUTkRZFSW0GQR1XS
RS4-11 NUnZcXVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTFwM{O4PFYh|ryP NH:1PYNUSU6JRWK=
DMS-114 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfzeHM3UUN3ME2xMlM3PzN5IN88US=> NIfnSHNUSU6JRWK=
MSTO-211H NWfXOGxYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVGyWW9wUUN3ME2xMlQ4Ozd6IN88US=> MmfaV2FPT0WU
DU-145 NXHs[oI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TRTWlEPTB;MT61PFIyPyEQvF2= MkSwV2FPT0WU
A172 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2n4d2lEPTB;MT63NFM2PSEQvF2= MWTTRW5ITVJ?
SBC-1 M{CyT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHYdIJKUUN3ME2yMlA6PCEQvF2= NU\VR|hpW0GQR1XS
H9 M2TBeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XFd2lEPTB;Mj6xOFMxPiEQvF2= M4T5SXNCVkeHUh?=
NCI-SNU-1 MoK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHwdpdiUUN3ME2yMlE5Ozl2IN88US=> Mnn3V2FPT0WU
NCI-H720 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnrO|BKSzVyPUKuNlEzQDNizszN NF;0WpVUSU6JRWK=
HCC2218 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7qb3RuUUN3ME2yMlM4QTN7IN88US=> NHXz[GFUSU6JRWK=
G-401 Mmf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDW[lFYUUN3ME2yMlQ4OTh7IN88US=> Mnn5V2FPT0WU
MPP-89 NX3t[GZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTJwNEizOlQh|ryP MYDTRW5ITVJ?
697 NU\Xc5RnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTLTWM2OD1{Lk[1N|MyKM7:TR?= MVnTRW5ITVJ?
KARPAS-45 M3TNOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfSTWsyUUN3ME2yMlcxPzR5IN88US=> NXfGbpJFW0GQR1XS
MG-63 NHrt[FlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUe4NmU6UUN3ME2yMlk1OjZ{IN88US=> Mo\pV2FPT0WU
NTERA-S-cl-D1 M4izXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Tl[mlEPTB;Mz6wN|Q4OiEQvF2= Ml7aV2FPT0WU
G-402 M2nDc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTNwMUK3Nlch|ryP MVXTRW5ITVJ?
NKM-1 NXrqdmVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTNwMUO1OlQh|ryP MV3TRW5ITVJ?
RH-18 NXnHZmpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTNwMUm1PVgh|ryP M2nBdnNCVkeHUh?=
NCI-H1092 NFTrPHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTNwMUm2PUDPxE1? MVXTRW5ITVJ?
RPMI-8226 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDxeXpRUUN3ME2zMlI{PDR5IN88US=> NFflRY5USU6JRWK=
GAMG MlX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTNwNE[1O|Yh|ryP NHi4RnZUSU6JRWK=
HH MkjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr3SoxVUUN3ME2zMlQ4Pjd4IN88US=> MlnwV2FPT0WU
RO82-W-1 MnSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3PTWM2OD1|LkS5PFU2KM7:TR?= NUDJRY9DW0GQR1XS
CCRF-CEM Mm\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWS2b2hTUUN3ME2zMlUxPDh6IN88US=> NHXVZ5lUSU6JRWK=
NBsusSR NIS1enZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3H2SWlEPTB;Mz62N|k3QSEQvF2= NHHscXZUSU6JRWK=
CHL-1 NH7ZeFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXVTWM2OD1|Lk[1O|k6KM7:TR?= NFTrSodUSU6JRWK=
LK-2 NV7vfnE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojiTWM2OD1|Lk[3NVM{KM7:TR?= NEPxZohUSU6JRWK=
Hs-578-T NVTtblFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PPOGlEPTB;Mz62O|g4OyEQvF2= M{G1UHNCVkeHUh?=
CTB-1 NX:0S2ViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfUTWM2OD1|LkiwNFUyKM7:TR?= M2XUSXNCVkeHUh?=
ES5 NIPTdWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWe1Vll1UUN3ME2zMlg{PjN5IN88US=> M4D5N3NCVkeHUh?=
A204 NG\SSpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTNwOUKwO|Uh|ryP NX32N5Q6W0GQR1XS
SW780 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XBUmlEPTB;Mz65NlI1PSEQvF2= Mn3jV2FPT0WU
EW-3 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTNwOUi5NlMh|ryP MnSzV2FPT0WU
A704 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[2bWlEPTB;ND6yPFczOyEQvF2= NFPMVVZUSU6JRWK=
LU-139 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\tNmlEPTB;ND6zNVU{PCEQvF2= NIHFWmhUSU6JRWK=
CAL-72 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPmN|RKSzVyPUSuOFE4PDZizszN M4jhWXNCVkeHUh?=
D-336MG M4C0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7UPXhGUUN3ME20MlQ3QDF5IN88US=> M{DNfnNCVkeHUh?=
LAMA-84 NEPvRZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTRwNUOzNUDPxE1? M4PTXnNCVkeHUh?=
GI-ME-N MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3kfo9vUUN3ME20MlU1QDFizszN NILIUYNUSU6JRWK=
KM-H2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTRwNUWyNlIh|ryP NEPYRZhUSU6JRWK=
NCI-H209 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTRwNUiyPFMh|ryP NGPafXFUSU6JRWK=
IGROV-1 NHjBRnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLTTWM2OD12Lki3NVY5KM7:TR?= NUnzcGkxW0GQR1XS
L-363 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTRwOU[2OlUh|ryP MnzzV2FPT0WU
SK-MEL-3 MoXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrsTWM2OD13LkK0NFYh|ryP MV3TRW5ITVJ?
HuO9 M1G1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTVwM{i4OFMh|ryP Mmr0V2FPT0WU
NOS-1 M{O1S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XYXmlEPTB;NT63NlkzPyEQvF2= NWX3fndFW0GQR1XS
NCI-H1770 NY\Le2NST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\1ZWlEPTB;NT65OVA{OiEQvF2= MofoV2FPT0WU
SF126 NWrMO|E{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfnTWM2OD14LkKxOFA3KM7:TR?= MmOzV2FPT0WU
ML-2 NUfTUGh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIq2cYZKSzVyPU[uNlQ6PzdizszN NGTyR2JUSU6JRWK=
CHP-134 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTZwMkWxPFIh|ryP NVz1dI9yW0GQR1XS
NCI-H1355 MnqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LCSGlEPTB;Nj60NVc{OyEQvF2= MXrTRW5ITVJ?
TE-12 MkC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\jbGVKSzVyPU[uO|I3PzFizszN NIKwWlRUSU6JRWK=
A4-Fuk MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPkXZNPUUN3ME22Mlc{OTR{IN88US=> MoSwV2FPT0WU
MV-4-11 Mn\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlG0TWM2OD14Lke2OlI3KM7:TR?= NV;ETmZ3W0GQR1XS
SK-UT-1 NWH3WFd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfuTWM2OD14LkmxO|g1KM7:TR?= MnvzV2FPT0WU
J-RT3-T3-5 MlP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnSOYlKSzVyPUeuNFc4PjRizszN NFHKNWRUSU6JRWK=
ME-180 NELQ[JZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELKbnVKSzVyPUeuNVA1ODRizszN MXfTRW5ITVJ?
SK-MEL-28 Mk\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vpXGlEPTB;Nz6zO|gyQSEQvF2= NWntc3FQW0GQR1XS
HAL-01 MmmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTdwNEizOFEh|ryP NH20enhUSU6JRWK=
ES8 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\5SHJuUUN3ME23MlY6PjJ4IN88US=> MlnMV2FPT0WU
DB NH7Eb2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEH0coJKSzVyPUiuNVE2ODRizszN MVPTRW5ITVJ?
SK-NEP-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4izcGlEPTB;OD60PFE1QSEQvF2= NEO0fIpUSU6JRWK=
COR-L88 NV\DTGVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjvNoxKSzVyPUiuOVA6QDFizszN NUjHUG1SW0GQR1XS
LB1047-RCC NHTreZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRThwNUKyNVIh|ryP Mk\RV2FPT0WU
NCI-H520 NGn6S5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvEeFVKSzVyPUiuOlIyPTdizszN NUizZZhEW0GQR1XS
SW954 NYj4XlkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2D4dGlEPTB;OD62PVc5PiEQvF2= Mm\IV2FPT0WU
TE-6 M4TMS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXixcI5LUUN3ME24Mlc2OTR|IN88US=> M4HrfXNCVkeHUh?=
D-283MED M3;hcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTlwME[1N|Qh|ryP Moe5V2FPT0WU
DBTRG-05MG MkfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEC3N5BKSzVyPUmuNFk3ODdizszN NIjSPHNUSU6JRWK=
NCI-H446 NYX1fm5CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTlwMkm1NlYh|ryP NF[zXZJUSU6JRWK=
HOS MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTVTWM2OD17LkO1NVM1KM7:TR?= NFXxU2lUSU6JRWK=
ES4 NH30WFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;MfGlEPTB;OT61NFU6PSEQvF2= NGjRXpJUSU6JRWK=
EW-13 MlLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTlwOEmwOVUh|ryP MXLTRW5ITVJ?
IST-MES1 M3P0d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTlwOUS1N|Qh|ryP MV3TRW5ITVJ?
CAS-1 MmPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTlwOUe2OVkh|ryP M4rQeHNCVkeHUh?=
EM-2 MkHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\hUWlEPTB;MUCuNVM6OyEQvF2= NIrYdFFUSU6JRWK=
SW948 M1PLWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{S2R2lEPTB;MUCuNVg5OiEQvF2= Ml;jV2FPT0WU
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DJM-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\B[WpKSzVyPUSwMlk4QTlizszN MnXPV2FPT0WU
TGBC11TKB MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzrTWM2OD12MT6wPVI3KM7:TR?= MkPJV2FPT0WU
U-2-OS NHLoU2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;xUnBDUUN3ME20Nk4zPjRzIN88US=> M2\YRnNCVkeHUh?=
NCI-H2030 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3vTWM2OD12Mj60N|Y5KM7:TR?= NF;WUYVUSU6JRWK=
LU-135 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnOcJRKSzVyPUSyMlU1PDdizszN NWjreVZWW0GQR1XS
ZR-75-30 Mlj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4ixO2lEPTB;NEOuNFQ6OyEQvF2= MYjTRW5ITVJ?
GT3TKB M2iwSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{X1R2lEPTB;NEOuNlY4QSEQvF2= MmG4V2FPT0WU
RPMI-2650 M3\4Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTR|Lke4NVYh|ryP MmH6V2FPT0WU
SAS NETKVJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTR|Lkm1N|Qh|ryP Mk\xV2FPT0WU
MDA-MB-231 MnHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XXdWlEPTB;NEOuPVYxQSEQvF2= M1\LWXNCVkeHUh?=
JVM-3 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTR2LkC1N|Mh|ryP M1HRSHNCVkeHUh?=
COLO-320-HSR NYHhcoZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDVeHNKSzVyPUS0MlU3OzNizszN M1XrXnNCVkeHUh?=
SNB75 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLCTWM2OD12ND62NVA2KM7:TR?= NXnGXYlwW0GQR1XS
NCI-H441 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVz5R5dsUUN3ME20OE46OzJ6IN88US=> Moe4V2FPT0WU
HCT-116 NFTJW5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37uVWlEPTB;NESuPVg3QCEQvF2= NWrReY15W0GQR1XS
NCI-H226 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfnRXpKSzVyPUS1MlY{PjhizszN NEXPe4lUSU6JRWK=
CAL-33 M2XUbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIi0UZRKSzVyPUS1MlkzOTdizszN M33nSnNCVkeHUh?=
NCI-H1437 NH;sVotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnPTWM2OD12Nj6zNlEh|ryP M{i3SHNCVkeHUh?=
HCC1187 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTlTWM2OD12Nj60NlU2KM7:TR?= MmmxV2FPT0WU
NUGC-3 M3ixPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofxTWM2OD12Nj61O|A6KM7:TR?= NF3qUWVUSU6JRWK=
T98G MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX75NFdHUUN3ME20O{42PDdizszN NG[5VpJUSU6JRWK=
OVCAR-8 MmPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzIenM2UUN3ME20O{43QDNizszN NXn6Vm5UW0GQR1XS
LB2241-RCC NFXFRoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHkTWM2OD12Nz63Nlch|ryP M2XhPHNCVkeHUh?=
NCI-H358 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTR6LkGxOVIh|ryP MXXTRW5ITVJ?
PANC-08-13 M{P3dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLVTWM2OD12OD6xPFU{KM7:TR?= MXXTRW5ITVJ?
KP-N-YN M4nLcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHOzXXBKSzVyPUS4MlIyODJizszN M3Pk[3NCVkeHUh?=
NCI-H1755 Ml65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYe5PVRyUUN3ME20PE4zPzJ4IN88US=> NHfGZmJUSU6JRWK=
NCI-N87 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHPTWM2OD12OD6yPVkyKM7:TR?= Mk[yV2FPT0WU

... 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