PD-161570;PF-1480232
- CAS号:192705-80-9
- 英文名:N-[6-(2,6-Dichlorophenyl)-2-[[4-(diethylamino)butyl]amino]pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea
- 中文名:PD-161570;PF-1480232
- CBNumber:CB62518839
- 分子式:C26H35Cl2N7O
- 分子量:532.51
- MOL File:192705-80-9.mol
- 熔点 :215-230?C
- 密度 :1.249±0.06 g/cm3(Predicted)
- 储存条件 :Store at RT
- 溶解度 :DMSO: >10mg/mL
- 形态 :powder
- 酸度系数(pKa) :9.82±0.43(Predicted)
- 颜色 :white to off-white
- 危险品标志 :T
- 危险类别码 :25-36/37/38
- 安全说明 :26-45
- 危险品运输编号 :UN 2811 6.1 / PGIII
- WGK Germany :3
PD-161570;PF-1480232性质、用途与生产工艺
- 生物活性 PD-161570 是一种有效的且具有 ATP 竞争能力的人 FGF-1 受体抑制剂,IC50 为 39.9 nM,Ki 为 42 nM。PD-161570 还抑制 PDGFR,EGFR 和 c-Src 酪氨酸激酶,IC50 值分别为 310 nM,240 nM 和 44 nM。PD-161570 抑制 PDGF 刺激的自磷酸化和 FGF-1 受体磷酸化,IC50 分别为 450 nM 和 622 nM。PD-161570 还是一种骨形态发生蛋白 (BMPs) 和 TGF-β 信号抑制剂。
-
靶点
FGFR1
39.9 nM (IC 50 )
FGFR1
42 nM (Ki)
FGFR1 autophosphorylation
622 nM (IC 50 )
PDGFRβ
262 nM (IC 50 )
PDGFR
310 nM (IC 50 )
EGFR
240 nM (IC 50 )
c-Src
44 nM (IC 50 )
TGF-β Receptor
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体外研究
PD-161570 (Compound 6c; 0.1-1 µM; 1-8 days; VSMCs) treatment inhibits PDGF-stimulated vascular smooth muscle cell proliferation in a dose dependent fashion with an IC 50 of 0.3 µM on day 8.
PD-161570 suppresses constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A 121(p) ) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A 121(p) cells in culture.
PD-161570 can potently inhibit basic fibroblast growth factor (bFGF)-mediated angiogenesis.Cell Proliferation Assay
Cell Line: Vascular smooth muscles cells (VSMCs) Concentration: 0.1 µM, 0.3 µM, 1 µM Incubation Time: 1 day, 3 days, 6 days, 8 days Result: Inhibited VSMC proliferation in a dose dependent fashion with an IC 50 of 0.3 µM at day 8.
- 更新日期:2024/11/08
- 产品编号:HY-100434
- 产品名称:PD-161570;PF-1480232 PD-161570
- CAS编号:192705-80-9
- 包装:5mg
- 价格:1150元
- 更新日期:2024/11/08
- 产品编号:HY-100434
- 产品名称:PD-161570;PF-1480232 PD-161570
- CAS编号:192705-80-9
- 包装:10 mg
- 价格:1850元
- 公司名称:TOCRIS-US
- 联系电话:--
- 电子邮件:customerservice@tocris.co.uk
- 国家:英国
- 产品数:5726
- 优势度:77