PD-161570

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PD-161570  纯度: 99.04%

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。

PD-161570

PD-161570 Chemical Structure

CAS No. : 192705-80-9

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10 mg ￥4000 In-stock
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生物活性

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively[1][2]. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor[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 IC50 of 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50 of 0.3 µM at day 8.

分子量

532.51

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Hamby JM, et al. Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. J Med Chem. 1997 Jul 18;40(15):2296-303.

    [2]. Batley BL, et al. Inhibition of FGF-1 receptor tyrosine kinase activity by PD 161570, a new protein-tyrosine kinase inhibitor. Life Sci. 1998;62(2):143-50.

    [3]. Kyosuke Hino, et al. An mTOR Signaling Modulator Suppressed Heterotopic Ossification of Fibrodysplasia Ossificans Progressiva. Stem Cell Reports. 2018 Nov 13;11(5):1106-1119.

    [4]. Wolfe A, et al. Pharmacologic characterization of a kinetic in vitro human co-culture angiogenesis model using clinically relevant compounds. J Biomol Screen. 2013 Dec;18(10):1234-45.

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