PD 166285 (CAS 212391-63-4)

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备用名: Heparin-Cantithrombin II

应用； PD 166285 is an inhibitor of RTK, c-Src, FGFR1, Wee 1, and PDGFRβ

CAS号码: 212391-63-4

纯度: ≥98%

分子量: 585.35

分子式: C₂₆H₂₇Cl₂N₅O₂•₂HCl

Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.

仅供科研使用。不可用于诊断或治疗。

* 参考分析证明大量特定数据 (包括水含量).

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PD 166285 is a potent inhibitor of the tyrosine kinases c-Src, Flg (fibroblast growth factor receptor 1, FGFR1), and PDGFRβ (platelet-derived growth factor receptor β) (IC₅₀ values are 8.4, 39.3 and 98.3 nM respectively). PD 166285 also inhibits the checkpoint kinases Wee1 and MYT1 (Myt1), abolishes Cdc2 phosphorylation in numerous tumor cell lines, and abrogates the G2 checkpoint. PD 166285 is an RTK inhibitor with broad-spectrum properties and displays anti-angiogenic activity and anti-tumor efficacy when used with PDT (photodynamic therapy). PD 166285 is an inhibitor of EGFR.

参考文献

Star, W., et al.: Cancer Res., 46, 2532 (1986), Sawutz, D., et al.: Biochem. Pharm., 51, 1631 (1996), Voest, E., et al.: Anti-Cancer Drugs, 7, 723 (1996), Connolly, C., et al.: Bioorg. Med. Chem. Lett., 7(18), 2415 (1997), Hamby, J., et al.: J. Med. Chem., 40, 2296 (1997)

物理状态 :

Solid

溶解度 :

Soluble in water, methanol, and DMSO (100 mM).

保存 :

Store at 4° C

熔点 :

236-241° C

折射率 :

n²⁰_D ~1.64 (Predicted)

IC50 :

c-Src: IC₅₀ = 8.4 nM; Wee 1: IC₅₀ = 24 nM; Flg: IC₅₀ = 39.3 nM; MYT1: IC₅₀ = 72 nM; EGFR: IC₅₀ = 87.5 nM

仅供科研使用。不可用于诊断或治疗。

PubChem CID :

9916391

MDL 号码 :

MFCD18086890

SMILES :

CCN(CC)CCOC1=CC=C(C=C1)NC2=NC=C3C=C(C(=O)N(C3=N2)C)C4=C(C=CC=C4Cl)Cl.Cl.Cl

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