PD-161570;PF-1480232

生物活性靶点体外研究 PD-161570;PF-1480232 试剂级价格

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

PD-161570;PF-1480232化学性质

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

安全信息

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

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.