PF-0477736-其他小分子化合物-深圳欣博盛生物科技有限公司

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PF-0477736

品牌：Adipogen

官网链接

说明书

折扣/货期

货号：AG-CR1-3537-M005	规格：5 mg	目录价：￥1020
货号：AG-CR1-3537-M010	规格：10 mg	目录价：￥1800
货号：AG-CR1-3537-M050	规格：50 mg	目录价：￥7200

产品详情

* 以下信息仅供参考，详情请以原厂网站为准

产品名称:

PF-0477736

别名:

PF0477736; PF-477736; PF-00477736

产品描述:

PF-0477736 is a potent, selective ATP-competitive inhibitor of Chk1 (Ki = 0.49nM) with 100-fold selectivity over Chk2 (Ki = 47nM). When used in combination with various chemotherapeutics (e.g. gemcitabine and carboplatin), PF-0477736 abrogates DNA damage-induced cell cycle arrest, sensitizes cells to DNA damage, potentiating the antiproliferative effects of these compounds in vitro and in vivo in tumor cell lines and xenografts. PF-0477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3 and Ret (Ki = 10, 14, 23, 23, 25 and 39 nM, respectively). Checkpoint kinase 1 (Chk1) belongs to the Ca2+/calmodulin-dependent protein kinase class of enzymes (CAMK). CAMKs are activated by increases in the concentration of intracellular calcium ions (Ca2+) and calmodulin. When activated, the CAMKs transfer phosphates from ATP to defined serine or threonine residues in other proteins, therefore CAMKs are serine/threonine-specific protein kinases. Chk1 regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. Antagonizing the Chk1-mediated cell cycle checkpoints has emerged as an attractive target for anticancer therapy. If Chk1 activity is blocked, DNA-damaged or spindle-disrupted cells would exit cell cycle arrest before full repair and subsequently undergo mitotic catastrophe or cell death. Chk1 inhibitors consequently increase the therapeutic index of DNA-damaging or antimitotic agents as well.

保存温度:

+4°C

运输温度:

Ambient

预期分子量:

419.5

产品形式:

solid

产地:

瑞士

纯度:

>95% (HPLC)