PD-161570

立即咨询

PD-161570

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

192705-80-9

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议

产品介绍

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，K_i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。

生物活性

PD-161570 is a potent and ATP-competitivehumanFGF-1receptorinhibitor with anIC₅₀of 39.9 nM and aK_iof 42 nM. PD-161570 also inhibits thePDGFR,EGFRandc-Src tyrosine kinaseswithIC₅₀values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibitsPDGF-stimulated autophosphorylation andFGF-1receptorphosphorylation withIC₅₀s of 450 nM and 622 nM, respectively^[1]^[2]. PD-161570 is also abone morphogenetic proteins (BMPs)andTGF-β signalinginhibitor^[3].

IC₅₀& Target^[1]^[2]^[3]

FGFR1

39.9 nM (IC₅₀)

FGFR1

42 nM (Ki)

FGFR1 autophosphorylation

622 nM (IC₅₀)

PDGFRβ

262 nM (IC₅₀)

PDGFR

310 nM (IC₅₀)

EGFR

240 nM (IC₅₀)

c-Src

44 nM (IC₅₀)

TGF-β Receptor

体外研究
(In Vitro)

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 IC₅₀of 0.3 μM on day 8^[1].
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^[2].
PD-161570 can potently inhibit basic fibroblast growth factor (bFGF)-mediated angiogenesis^[4].

Cell Proliferation Assay^[1]

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 IC₅₀of 0.3 μM at day 8.

分子量

532.51

性状

Solid

Formula

C₂₆H₃₅Cl₂N₇O

CAS 号

192705-80-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL(62.59 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.8779 mL	9.3895 mL	18.7790 mL
5 mM	0.3756 mL	1.8779 mL	3.7558 mL
10 mM	0.1878 mL	0.9389 mL	1.8779 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。