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.

  • 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.

  • 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.

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 MoT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfkOFduUUN3ME2wMlAyOjJ3IN88US=> M3v1ZnNCVkeHUh?=
KG-1 Mn;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjqSYJKSzVyPUCuNFUyOjlizszN M3jJbXNCVkeHUh?=
MFM-223 NIq1[FVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPh[3lKSzVyPUCuNlE2PzZizszN M3jY[XNCVkeHUh?=
EoL-1-cell MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDETWM2OD1yLkOyPVg1KM7:TR?= NYjtflB2W0GQR1XS
ECC10 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTBwM{O4PVgh|ryP M2joTnNCVkeHUh?=
H-EMC-SS M2jWbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjMTWM2OD1yLkO0O|E2KM7:TR?= NXe3R4FHW0GQR1XS
AN3-CA Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PDN2lEPTB;MD60NFE{OyEQvF2= NWrvUpRHW0GQR1XS
HuO-3N1 NH\IbZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TMbGlEPTB;MD61OFY2OyEQvF2= NVvjZVJJW0GQR1XS
RT-112 NXLu[oZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGj4UpdKSzVyPUCuOVQ4ODFizszN NFj0Z5dUSU6JRWK=
NEC8 Ml34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTBwNU[yPFkh|ryP MXXTRW5ITVJ?
D-263MG Mm\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;RTWM2OD1yLkexNVU6KM7:TR?= M{XaOHNCVkeHUh?=
SW962 MkGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4i5V2lEPTB;MD63PFk5QCEQvF2= NWfyOWdmW0GQR1XS
BV-173 M{TMOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTBwOES2NlMh|ryP NFu5cINUSU6JRWK=
MFE-280 NGHoOpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwOEW4O|Ih|ryP NWjkdnZMW0GQR1XS
HuH-7 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmL1TWM2OD1zLkK0OFY1KM7:TR?= MUHTRW5ITVJ?
RS4-11 MkC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXINow5UUN3ME2xMlM{QDh4IN88US=> MXjTRW5ITVJ?
DMS-114 NILPTG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTFwM{[3N|ch|ryP MVrTRW5ITVJ?
MSTO-211H M3Tubmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFwNEezO|gh|ryP MnPXV2FPT0WU
DU-145 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\wbGlEPTB;MT61PFIyPyEQvF2= MWPTRW5ITVJ?
A172 NGjafHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTFwN{CzOVUh|ryP M17YcnNCVkeHUh?=
SBC-1 MorRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXPTWM2OD1{LkC5OEDPxE1? NYPQRYdEW0GQR1XS
H9 MmDDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTJwMUSzNFYh|ryP M3jienNCVkeHUh?=
NCI-SNU-1 MoTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\LTXFQUUN3ME2yMlE5Ozl2IN88US=> NXLvSJVmW0GQR1XS
NCI-H720 M{TGNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTGNHlKSzVyPUKuNlEzQDNizszN NVm1XY1xW0GQR1XS
HCC2218 NILHfFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rqcGlEPTB;Mj6zO|k{QSEQvF2= NVHHUWlMW0GQR1XS
G-401 NH7h[41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV[2VYRPUUN3ME2yMlQ4OTh7IN88US=> M4PiU3NCVkeHUh?=
MPP-89 NFnoXYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLvXpFKSzVyPUKuOFg{PjRizszN NWT6WZBkW0GQR1XS
697 NHO5UZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTJwNkWzN|Eh|ryP M4Lhd3NCVkeHUh?=
KARPAS-45 NUTBNWpLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\tfHRDUUN3ME2yMlcxPzR5IN88US=> M1HsenNCVkeHUh?=
MG-63 NUTJ[21{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\sbZpKSzVyPUKuPVQzPjJizszN MWrTRW5ITVJ?
NTERA-S-cl-D1 M1npTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjCV4pKSzVyPUOuNFM1PzJizszN NUHlTIp4W0GQR1XS
G-402 NXK2OZZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHjTWM2OD1|LkGyO|I4KM7:TR?= MV7TRW5ITVJ?
NKM-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVflNYZDUUN3ME2zMlE{PTZ2IN88US=> NIPZUIRUSU6JRWK=
RH-18 M1zm[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTNwMUm1PVgh|ryP MnToV2FPT0WU
NCI-H1092 M1rVdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mny3TWM2OD1|LkG5Olkh|ryP MUfTRW5ITVJ?
RPMI-8226 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfsN2ZKSzVyPUOuNlM1PDdizszN M3nZWXNCVkeHUh?=
GAMG NF3pdnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXSTWM2OD1|LkS2OVc3KM7:TR?= MUTTRW5ITVJ?
HH NX;vdWF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkP4TWM2OD1|LkS3Olc3KM7:TR?= NE\FTVZUSU6JRWK=
RO82-W-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfNTJhKSzVyPUOuOFk5PTVizszN M1;ZfXNCVkeHUh?=
CCRF-CEM NHzjeo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTNwNUC0PFgh|ryP MV;TRW5ITVJ?
NBsusSR M163UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1L6T2lEPTB;Mz62N|k3QSEQvF2= NU[4R3ByW0GQR1XS
CHL-1 M3\rTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHNTWM2OD1|Lk[1O|k6KM7:TR?= MWfTRW5ITVJ?
LK-2 NVmybYxCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV76cGpkUUN3ME2zMlY4OTN|IN88US=> M2PLdHNCVkeHUh?=
Hs-578-T NW[5VXpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUT0NVYxUUN3ME2zMlY4QDd|IN88US=> M1rmUXNCVkeHUh?=
CTB-1 Ml7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDWUod2UUN3ME2zMlgxODVzIN88US=> MmDrV2FPT0WU
ES5 NHfZTHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHIc2oyUUN3ME2zMlg{PjN5IN88US=> M{fBOnNCVkeHUh?=
A204 NWj1XFZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYmyc5JxUUN3ME2zMlkzODd3IN88US=> M2CwVHNCVkeHUh?=
SW780 NIDRRYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLJOnVKSzVyPUOuPVIzPDVizszN NYjKRnBxW0GQR1XS
EW-3 NYrFVI5OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{P2bGlEPTB;Mz65PFkzOyEQvF2= NEezcoZUSU6JRWK=
A704 NHHxc2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Lo[mlEPTB;ND6yPFczOyEQvF2= NYfMfHFFW0GQR1XS
LU-139 NF;1fo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{mxTmlEPTB;ND6zNVU{PCEQvF2= NGTjVFVUSU6JRWK=
CAL-72 NEHRWZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTRwNEG3OFYh|ryP M{PPNXNCVkeHUh?=
D-336MG MofhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4O4b2lEPTB;ND60OlgyPyEQvF2= MnXuV2FPT0WU
LAMA-84 NXPBSItQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXxb3dKSzVyPUSuOVM{OSEQvF2= NFrscYlUSU6JRWK=
GI-ME-N M1fwS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfFXItXUUN3ME20MlU1QDFizszN MmHlV2FPT0WU
KM-H2 MlPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M136TWlEPTB;ND61OVIzOiEQvF2= M1vvUHNCVkeHUh?=
NCI-H209 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTRwNUiyPFMh|ryP NV3QendbW0GQR1XS
IGROV-1 M2DNNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkK1TWM2OD12Lki3NVY5KM7:TR?= NX3UdnFsW0GQR1XS
L-363 NXHC[5BWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLiTWM2OD12Lkm2OlY2KM7:TR?= NWL3dWJnW0GQR1XS
SK-MEL-3 NXjHPZd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Xwd2lEPTB;NT6yOFA3KM7:TR?= NXLGR3JHW0GQR1XS
HuO9 NX\vfJlET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnXTWM2OD13LkO4PFQ{KM7:TR?= NGfwS2tUSU6JRWK=
NOS-1 NGPjZ4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3i0XWlEPTB;NT63NlkzPyEQvF2= M{HxO3NCVkeHUh?=
NCI-H1770 NX7rZZlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPzdIVtUUN3ME21Mlk2ODN{IN88US=> NGPTVHNUSU6JRWK=
SF126 NVPCRnl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFe3R5JKSzVyPU[uNlE1ODZizszN MXjTRW5ITVJ?
ML-2 Mkn3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonETWM2OD14LkK0PVc4KM7:TR?= MkXNV2FPT0WU
CHP-134 M3X1emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rLd2lEPTB;Nj6yOVE5OiEQvF2= NYqxPJE5W0GQR1XS
NCI-H1355 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\EVGlEPTB;Nj60NVc{OyEQvF2= NF;ZOFZUSU6JRWK=
TE-12 M{eybWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILkXWdKSzVyPU[uO|I3PzFizszN M1HIOXNCVkeHUh?=
A4-Fuk MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTZwN{OxOFIh|ryP MYrTRW5ITVJ?
MV-4-11 NFT1XG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\J[4dzUUN3ME22Mlc3PjJ4IN88US=> MkK5V2FPT0WU
SK-UT-1 M4WxSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXRTZVGUUN3ME22MlkyPzh2IN88US=> M1Sx[XNCVkeHUh?=
J-RT3-T3-5 NGDMTnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\XS|FKSzVyPUeuNFc4PjRizszN NIW4Z41USU6JRWK=
ME-180 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTdwMUC0NFQh|ryP NU\XOFBlW0GQR1XS
SK-MEL-28 NWDjR4tVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTdwM{e4NVkh|ryP NHTM[oxUSU6JRWK=
HAL-01 M3XuXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnn6TWM2OD15LkS4N|QyKM7:TR?= MnvLV2FPT0WU
ES8 M{XmRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnezTWM2OD15Lk[5OlI3KM7:TR?= MoXlV2FPT0WU
DB MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTxTWM2OD16LkGxOVA1KM7:TR?= MkjaV2FPT0WU
SK-NEP-1 MlHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3THPWlEPTB;OD60PFE1QSEQvF2= NH3rNnVUSU6JRWK=
COR-L88 NGHBTHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnWdYJKSzVyPUiuOVA6QDFizszN MV;TRW5ITVJ?
LB1047-RCC M{TJSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Oxe2lEPTB;OD61NlIyOiEQvF2= NF\POJFUSU6JRWK=
NCI-H520 MlvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIC4fZhKSzVyPUiuOlIyPTdizszN M1y0OHNCVkeHUh?=
SW954 M1PPNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRThwNkm3PFYh|ryP Mm\xV2FPT0WU
TE-6 NYHGfHoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{L6WWlEPTB;OD63OVE1OyEQvF2= MkLoV2FPT0WU
D-283MED M3yzUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnBU2FKSzVyPUmuNFY2OzRizszN MY\TRW5ITVJ?
DBTRG-05MG NY\JWVcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2H5[2lEPTB;OT6wPVYxPyEQvF2= NGnZZ4dUSU6JRWK=
NCI-H446 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTlwMkm1NlYh|ryP MVfTRW5ITVJ?
HOS MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nGZ2lEPTB;OT6zOVE{PCEQvF2= MX;TRW5ITVJ?
ES4 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTlwNUC1PVUh|ryP MmHlV2FPT0WU
EW-13 M17Zd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PVe2lEPTB;OT64PVA2PSEQvF2= NI\mPVlUSU6JRWK=
IST-MES1 NYC2SI0zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTlwOUS1N|Qh|ryP NUXHNVRpW0GQR1XS
CAS-1 NHnycGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXSWZpCUUN3ME25Mlk4PjV7IN88US=> NGLlUHpUSU6JRWK=
EM-2 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TS[WlEPTB;MUCuNVM6OyEQvF2= NYHQO2VbW0GQR1XS
SW948 M37XfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLReGRwUUN3ME2xNE4yQDh{IN88US=> NHW5XGlUSU6JRWK=
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DJM-1 NV3iUFFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfufGp1UUN3ME20NE46Pzl7IN88US=> MXvTRW5ITVJ?
TGBC11TKB M1;qPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjBSYZKSzVyPUSxMlA6OjZizszN NV;oOZRiW0GQR1XS
U-2-OS NICyNYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE[yXZFKSzVyPUSyMlI3PDFizszN M4LGZ3NCVkeHUh?=
NCI-H2030 NXG1VlVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTR{LkSzOlgh|ryP M3;RRnNCVkeHUh?=
LU-135 M3zSfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHwWIdKSzVyPUSyMlU1PDdizszN NHvEOnFUSU6JRWK=
ZR-75-30 Mlj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHja[lVKSzVyPUSzMlA1QTNizszN MmnwV2FPT0WU
GT3TKB MkXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfjdWxKSzVyPUSzMlI3PzlizszN NXPQPYpvW0GQR1XS
RPMI-2650 M1Tqe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTR|Lke4NVYh|ryP NIT3N2xUSU6JRWK=
SAS MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEf3[GRKSzVyPUSzMlk2OzRizszN NEjsc4tUSU6JRWK=
MDA-MB-231 NV3TeYdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TITWlEPTB;NEOuPVYxQSEQvF2= NVXScYpjW0GQR1XS
JVM-3 NYHXSVAxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTR2LkC1N|Mh|ryP NILvSYpUSU6JRWK=
COLO-320-HSR M1LURmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPBfIdjUUN3ME20OE42PjN|IN88US=> NUPX[JJVW0GQR1XS
SNB75 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17Sc2lEPTB;NESuOlExPSEQvF2= MmG0V2FPT0WU
NCI-H441 MlnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTR2LkmzNlgh|ryP MXrTRW5ITVJ?
HCT-116 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWe1NW5KUUN3ME20OE46QDZ6IN88US=> Mm[yV2FPT0WU
NCI-H226 NYjOb5JGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfYS4NUUUN3ME20OU43OzZ6IN88US=> MXTTRW5ITVJ?
CAL-33 M2jlN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnDcWJKSzVyPUS1MlkzOTdizszN M1T3eHNCVkeHUh?=
NCI-H1437 MlHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHaeFBpUUN3ME20Ok4{OjFizszN MnjFV2FPT0WU
HCC1187 NFrDWmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HnfGlEPTB;NE[uOFI2PSEQvF2= MXXTRW5ITVJ?
NUGC-3 NWrCT5hYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrRdlkxUUN3ME20Ok42PzB7IN88US=> M4LPcnNCVkeHUh?=
T98G M4\Z[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTyRVZKSzVyPUS3MlU1PyEQvF2= MlHLV2FPT0WU
OVCAR-8 NEXHVFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fybWlEPTB;NEeuOlg{KM7:TR?= NFnuPXpUSU6JRWK=
LB2241-RCC M3fqeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk[xTWM2OD12Nz63Nlch|ryP NUm0[5JnW0GQR1XS
NCI-H358 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;aTWM2OD12OD6xNVUzKM7:TR?= M1\Id3NCVkeHUh?=
PANC-08-13 NIfqR4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTR6LkG4OVMh|ryP NFzLXWlUSU6JRWK=
KP-N-YN MnTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPyUYdKSzVyPUS4MlIyODJizszN MYTTRW5ITVJ?
NCI-H1755 NFjEWplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLsTWM2OD12OD6yO|I3KM7:TR?= NYnnTWZNW0GQR1XS
NCI-N87 NYOyVWJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LtbmlEPTB;NEiuNlk6OSEQvF2= M{nwNnNCVkeHUh?=

... 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(数据来自Selleck实验检测而非文献):
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