PD173074是一种有效的FGFR1抑制剂,IC50为25 nM。它还抑制VEGFR2的活性,IC50为100-200 nM,对FGFR1与PDGFR和c-Src的选择性超过1000倍。
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产品名称 | FGFR ↓ ↑ | FGFR1 ↓ ↑ | FGFR2 ↓ ↑ | FGFR3 ↓ ↑ | FGFR4 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tyrphostin AG1296 |
+
FGFR (Swiss 3T3), IC50: 12.3 μM |
PDGFR | 99%+ | ||||||||||||||||
Pazopanib |
+
FGFR, IC50: 140 nM |
99% | |||||||||||||||||
Erdafitinib | ✔ | RET | 99%+ | ||||||||||||||||
Gambogenic acid | ✔ | 98+% | |||||||||||||||||
Sulfatinib |
+++
FGFR1, IC50: 15 nM |
99+% | |||||||||||||||||
Nintedanib esylate |
+
FGFR1, IC50: 69 nM |
++
FGFR2, IC50: 37 nM |
+
FGFR3, IC50: 108 nM |
98% | |||||||||||||||
Zoligratinib |
+++
FGFR1, IC50: 9.3 nM |
+++
FGFR2, IC50: 7.6 nM |
++
FGFR3, IC50: 22 nM |
+
FGFR4, IC50: 290 nM |
99%+ | ||||||||||||||
MK-2461 |
+
FGFR1, IC50: 65 nM |
++
FGFR2, IC50: 39 nM |
++
FGFR3, IC50: 50 nM |
98%+ | |||||||||||||||
SU 5402 |
++
FGFR1, IC50: 30 nM |
98% | |||||||||||||||||
Brivanib |
+
FGFR1, IC50: 148 nM |
99%+ | |||||||||||||||||
Lucitanib |
++
FGFR1, IC50: 17.5 nM |
+
FGFR2, IC50: 82.5 nM |
99%+ | ||||||||||||||||
Ponatinib |
++++
FGFR1, IC50: 2.2 nM |
98% | |||||||||||||||||
PD-166866 |
+
FGFR1, IC50: 52.4 nM |
98% | |||||||||||||||||
Narazaciclib |
++
FGFR1, IC50: 26 nM |
RET | 99%+ | ||||||||||||||||
Lactate |
+++
FGFR1, IC50: 8 nM |
+++
FGFR3, IC50: 9 nM |
c-Kit,FLT3 | 85% | |||||||||||||||
Lenvatinib mesylate |
++
FGFR1, IC50: 46 nM |
c-RET | 99% | ||||||||||||||||
LY2874455 |
++++
FGFR1, IC50: 2.8 nM |
++++
FGFR2, IC50: 2.6 nM |
+++
FGFR3, IC50: 6.4 nM |
+++
FGFR4, IC50: 6 nM |
99%+ | ||||||||||||||
FIIN-2 |
+++
FGFR1, IC50: 3.09 nM |
+++
FGFR2, IC50: 4.3 nM |
++
FGFR3, IC50: 27 nM |
++
FGFR4, IC50: 45.3 nM |
98% | ||||||||||||||
FIIN-3 |
+++
FGFR1, IC50: 13.1 nM |
++
FGFR2, IC50: 21 nM |
++
FGFR3, IC50: 31.4 nM |
++
FGFR4, IC50: 35.3 nM |
98% | ||||||||||||||
Infigratinib |
++++
FGFR1, IC50: 0.9 nM |
++++
FGFR2, IC50: 1.4 nM |
++++
FGFR3, IC50: 1.0 nM FGFR3 (K650E), IC50: 4.9 nM |
+
FGFR4, IC50: 60 nM |
99%+ | ||||||||||||||
Danusertib |
++
FGFR1, IC50: 47 nM |
RET | 99%+ | ||||||||||||||||
R1530 |
++
FGFR1, IC50: 28 nM |
98% | |||||||||||||||||
ENMD-2076 |
+
FGFR1, IC50: 92.7 nM |
+
FGFR2, IC50: 70.8 nM |
RET,FLT3 | 98% | |||||||||||||||
Dovitinib |
+++
FGFR1, IC50: 8 nM |
+++
FGFR3, IC50: 9 nM |
c-Kit,FLT3 | 99%+ | |||||||||||||||
Sorafenib |
+
FGFR1, IC50: 580 nM |
99% | |||||||||||||||||
SSR128129E |
+
FGFR1, IC50: 1.9 μM |
99%+ | |||||||||||||||||
AZD-4547 |
++++
FGFR1, IC50: 0.2 nM |
++++
FGFR2, IC50: 2.5 nM |
++++
FGFR3, IC50: 1.8 nM |
98% | |||||||||||||||
Lenvatinib |
++
FGFR1, IC50: 46 nM |
RET | 98% | ||||||||||||||||
PD173074 |
++
FGFR1, IC50: ~25 nM |
99%+ | |||||||||||||||||
S49076 |
++
FGFR1, IC50: 18 nM |
+++
FGFR2, IC50: 17 nM |
+++
FGFR3, IC50: 15 nM |
98% | |||||||||||||||
Futibatinib |
++++
FGFR1, IC50: 1.8 nM |
++++
FGFR2, IC50: 1.4 nM |
++++
FGFR3, IC50: 1.6 nM |
+++
FGFR4, IC50: 3.7 nM |
99%+ | ||||||||||||||
Ferulic Acid |
+
FGFR1, IC50: 3.78 μM |
+
FGFR2, IC50: 12.5 μM |
98% | ||||||||||||||||
Nintedanib |
+
FGFR1, IC50: 69 nM |
++
FGFR2, IC50: 37 nM |
+
FGFR3, IC50: 108 nM |
+
FGFR4, IC50: 610 nM |
99+% | ||||||||||||||
ASP5878 |
++++
FGFR1, IC50: 0.47 nM |
++++
FGFR2, IC50: 0.6 nM |
++++
FGFR3, IC50: 0.74 nM |
+++
FGFR4, IC50: 3.5 nM |
98% | ||||||||||||||
PRN1371 |
++++
FGFR1, IC50: 0.6 nM |
++++
FGFR2, IC50: 1.3 nM |
+++
FGFR3, IC50: 4.1 nM |
++
FGFR4, IC50: 19.3 nM |
99% | ||||||||||||||
Derazantinib |
+++
FGFR1, IC50: 4.5 nM |
++++
FGFR2, IC50: 1.8 nM |
+++
FGFR3, IC50: 4.5 nM |
++
FGFR4, IC50: 34 nM |
RET | 99%+ | |||||||||||||
ODM-203 |
+++
FGFR1, IC50: 11 nM |
+++
FGFR2, IC50: 16 nM |
+++
FGFR3, IC50: 6 nM |
++
FGFR4, IC50: 35 nM |
99%+ | ||||||||||||||
Pemigatinib |
++++
FGFR1, IC50: 0.4 nM |
++++
FGFR2, IC50: 0.5 nM |
++++
FGFR3, IC50: 1.2 nM |
++
FGFR4, IC50: 30 nM |
99%+ | ||||||||||||||
SKLB 610 | ✔ | PDGFR | 99%+ | ||||||||||||||||
Alofanib | ✔ | 99%+ | |||||||||||||||||
Lirafugratinib | ✔ | 98% | |||||||||||||||||
Masitinib mesylate | ✔ | FAK | 99%+ | ||||||||||||||||
BLU9931 |
+
FGFR3, IC50: 150 nM |
+++
FGFR4, IC50: 3 nM |
99%+ | ||||||||||||||||
BO-264 | ✔ | 99%+ | |||||||||||||||||
Fisogatinib |
+++
FGFR4, IC50: 5 nM |
99%+ | |||||||||||||||||
H3B-6527 |
++++
FGFR4, IC50: <1.2 nM |
99%+ | |||||||||||||||||
Roblitinib |
++++
FGFR4, IC50: 1.9 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
产品名称 | VEGFR1 ↓ ↑ | VEGFR2 ↓ ↑ | VEGFR3 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Motesanib Diphosphate |
++++
VEGFR1, IC50: 2 nM |
++++
VEGFR2/Flk1, IC50: 3 nM VEGFR2, IC50: 3 nM |
+++
VEGFR3, IC50: 6 nM |
RET,PDGFR | 98% | ||||||||||||||
Tivozanib |
++
VEGFR1, IC50: 30 nM |
+++
VEGFR2, IC50: 6.5 nM |
++
VEGFR3, IC50: 15 nM |
99%+ | |||||||||||||||
Brivanib |
+
VEGFR1, IC50: 380 nM |
++
Flk1, IC50: 25 nM VEGFR2, IC50: 25 nM |
99%+ | ||||||||||||||||
Regorafenib |
+++
VEGFR1, IC50: 13 nM |
+++
VEGFR2, IC50: 4.2 nM |
+
VEGFR3, IC50: 46 nM |
RET | 98% | ||||||||||||||
Pazopanib |
+++
VEGFR1, IC50: 10 nM |
++
VEGFR2, IC50: 30 nM |
+
VEGFR3, IC50: 47 nM |
FGFR,c-Kit,PDGFR | 99% | ||||||||||||||
Sitravatinib |
+++
VEGFR1 (FLT1), IC50: 6 nM |
+++
VEGFR2 (KDR), IC50: 5 nM |
++++
VEGFR3 (FLT4), IC50: 2 nM |
99%+ | |||||||||||||||
Foretinib |
+++
VEGFR1/FLT1, IC50: 6.8 nM |
++++
KDR, IC50: 0.86 nM |
++++
VEGFR3/FLT4, IC50: 2.8 nM |
Tie-2 | 99%+ | ||||||||||||||
MGCD-265 analog |
++++
VEGFR1, IC50: 3 nM |
++++
VEGFR2, IC50: 3 nM |
++++
VEGFR3, IC50: 4 nM |
Tie-2 | 99%+ | ||||||||||||||
Lactate |
+++
VEGFR1/FLT1, IC50: 10 nM |
+++
VEGFR2/Flk1, IC50: 13 nM |
+++
VEGFR3/FLT4, IC50: 8 nM |
c-Kit,FLT3 | 85% | ||||||||||||||
AEE788 |
+
FLT1, IC50: 59 nM |
+
KDR, IC50: 77 nM |
EGFR | 98+% | |||||||||||||||
Linifanib |
++++
VEGFR1/FLT1, IC50: 3 nM |
++++
VEGFR2/KDR, IC50: 4 nM |
+
VEGFR3/FLT4, IC50: 190 nM |
FLT3 | 99%+ | ||||||||||||||
Vatalanib 2HCl |
+
VEGFR1/FLT1, IC50: 77 nM |
++
VEGFR2/KDR, IC50: 37 nM VEGFR2/Flk1, IC50: 270 nM |
+
VEGFR3/FLT4, IC50: 660 nM |
c-Kit,c-Fms | 99%+ | ||||||||||||||
Axitinib |
++++
VEGFR1/FLT1, IC50: 0.1 nM |
++++
VEGFR2/KDR, IC50: 0.2 nM VEGFR2/Flk1, IC50: 0.18 nM |
98% | ||||||||||||||||
Dovitinib |
+++
VEGFR1/FLT1, IC50: 10 nM |
+++
VEGFR2/Flk1, IC50: 13 nM |
+++
VEGFR3/FLT4, IC50: 8 nM |
c-Kit,FLT3 | 99%+ | ||||||||||||||
ZM 306416 |
+
VEGFR1, IC50: 0.33 μM |
Src | 99%+ | ||||||||||||||||
KRN-633 |
+
VEGFR1, IC50: 170 nM |
+
VEGFR2, IC50: 160 nM |
+
VEGFR3, IC50: 125 nM |
c-Kit,BTK | 98% | ||||||||||||||
OSI-930 |
+++
FLT1, IC50: 8 nM |
+++
KDR, IC50: 9 nM |
99%+ | ||||||||||||||||
Lenvatinib |
++
VEGFR1/FLT1, IC50: 22 nM |
++++
VEGFR2/KDR, IC50: 4.0 nM |
+++
VEGFR3/FLT4, IC50: 5.2 nM |
98% | |||||||||||||||
NVP-BAW2881 |
+
hVEGFR1, IC50: 820 nM |
+++
mVEGF2, IC50: 165 nM hVEGFR2, IC50: 9 nM |
+
hVEGFR3, IC50: 420 nM |
98% | |||||||||||||||
Cediranib |
+++
VEGFR1/FLT1, IC50: 5 nM |
++++
VEGFR2/KDR, IC50: 0.5 nM |
c-Kit | 99%+ | |||||||||||||||
Nintedanib |
++
VEGFR1, IC50: 34 nM |
+++
VEGFR2, IC50: 13 nM |
+++
VEGFR3, IC50: 13 nM |
FLT3 | 99+% | ||||||||||||||
BMS-794833 |
++
VEGFR2, IC50: 15 nM |
99%+ | |||||||||||||||||
SKLB1002 |
++
VEGFR2, IC50: 32 nM |
98% | |||||||||||||||||
Cabozantinib S-malate |
++++
VEGFR2/KDR, IC50: 0.035 nM |
99+% | |||||||||||||||||
Ki8751 |
++++
VEGFR2, IC50: 0.9 nM |
c-Kit | 98+% | ||||||||||||||||
SU 5402 |
++
VEGFR2, IC50: 20 nM |
98% | |||||||||||||||||
Rivoceranib Mesylate |
++++
VEGFR2, IC50: 1 nM |
RET | 98+% | ||||||||||||||||
Ponatinib |
++++
VEGFR2, IC50: 1.5 nM |
98% | |||||||||||||||||
LY2874455 |
+++
VEGFR2, IC50: 7 nM |
99%+ | |||||||||||||||||
ZM323881 HCl |
++++
VEGFR2, IC50: <2 nM |
98% | |||||||||||||||||
AZD2932 |
+++
VEGFR-2, IC50: 8 nM |
c-Kit | 98% | ||||||||||||||||
Cabozantinib |
++++
VEGFR2/KDR, IC50: 0.035 nM |
98% | |||||||||||||||||
Sorafenib |
++
VEGFR2/Flk1, IC50: 90 nM VEGFR2, IC50: 90 nM |
99% | |||||||||||||||||
CYC-116 |
++
VEGFR2, Ki: 44 nM |
FLT3 | 99%+ | ||||||||||||||||
Golvatinib |
++
VEGFR2, IC50: 16 nM |
99%+ | |||||||||||||||||
Sunitinib |
+
VEGFR2 , IC50: 80 nM |
FLT3 | 98% | ||||||||||||||||
RAF265 |
++
VEGFR2, EC50: 30 nM |
99%+ | |||||||||||||||||
PD173074 | 99%+ | ||||||||||||||||||
BFH772 |
++++
VEGFR2, IC50: 3 nM |
98% | |||||||||||||||||
Semaxinib |
+
VEGFR2/Flk1, IC50: 1.23 μM |
98% | |||||||||||||||||
Vandetanib |
++
VEGFR2, IC50: 40 nM |
+
VEGFR3, IC50: 110 nM |
EGFR | 98% | |||||||||||||||
SAR131675 |
++
VEGFR3, IC50: 23 nM |
99%+ | |||||||||||||||||
ENMD-2076 |
+
VEGFR2/KDR, IC50: 58.2 nM |
++
VEGFR3/FLT4, IC50: 15.9 nM |
RET,FLT3 | 98% | |||||||||||||||
Telatinib |
+++
VEGFR2, IC50: 6 nM |
++++
VEGFR3, IC50: 4 nM |
c-Kit | 99%+ | |||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Angiogenesis, playing a major role in the progression of human diseases such as diabetic retinopathy, atherosclerosis and cancer, involves the concerted action of a number of polypeptide factors such as VEGF, Ang1 and FGF. PD173074 is a selective dual inhibitor of both FGFR1 and VEGFR2 with IC50 value of 21.5nM (measured by kinase activity) and 100-200nM (measured by VEGFR2 auto-phosphorylation in NIH 3T3 cells), respectively. PD173074 inhibited auto-phosphorylation of FGFR1, induced by aFGF and heparin, of NIH-3T3 cells expressing FGFR1 endogenously in a dose-dependent manner with an IC50 in the range 1–5nM, as well as auto-phosphorylation of overexpressed VEGFR2 stimulated with VEGF (100ng/ml) with an IC50 of 100–200nM. Mice treated daily with PD173074 by intraperitoneal injection per day starting 3 days prior to pellet implantation exhibited inhibition of bFGF-induced neovascularization by 86% at a dose of 1mg/kg, as well as inhibition of VEGF induced neovascularization by 81% at a dose of 2mg/kg[1]. PD173704 can specifically and effectively inhibit multiple FGF-2-mediated responses of both oligodendrocyte progenitors, as well as differentiated oligodendrocytes with complete antagonization on two phenotypic alterations, downregulation of myelin proteins, and their re-entry into the cell cycle[2]. |
作用机制 | PD173074 is an ATP-competitive inhibitor of FGFR1.[1] |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
A204 | Growth Inhibition Assay | IC50=3.92075 μM | SANGER | ||
A2058 | Growth Inhibition Assay | IC50=35.6061 μM | SANGER | ||
A253 | Growth Inhibition Assay | IC50=15.3869 μM | SANGER | ||
A2780 | Growth Inhibition Assay | IC50=11.0308 μM | SANGER | ||
Dose | Nude Mice[3]: 12 mg/kg Mice: 1 mg/kg, 2 mg/kg[1] (i.p.), 25 mg/kg - 100 mg/kg[4] (p.o.) |
Administration | i.p., p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.91mL 0.38mL 0.19mL |
9.55mL 1.91mL 0.95mL |
19.10mL 3.82mL 1.91mL |
CAS号 | 219580-11-7 |
分子式 | C28H41N7O3 |
分子量 | 523.67 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 105 mg/mL(200.51 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear PO 0.5% CMC-Na 35 mg/mL suspension |