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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。
PD-161570图片
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,Ki为 42 nM。PD-161570 还抑制PDGFREGFRc-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 aKiof 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 (A121(p)) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A121(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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM1.8779 mL9.3895 mL18.7790 mL
5 mM0.3756 mL1.8779 mL3.7558 mL
10 mM0.1878 mL0.9389 mL1.8779 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。