GDC-0575 dihydrochloride

CAS: 1657014-42-0 货号: G656507 分子式: C16H22BrCl2N5O 分子量: 451.19 PubChem CID: 131749450
有货
级别和纯度: 10mM in DMSO
别名
GDC-0575 二盐酸盐
储存条件
干燥,-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
G656507-1ml
期货 Stock Image
¥2,090.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC 50 of 1.2 nM, and has antitumor activity.

In Vitro

GDC-0575 dihydrochloride is a selective and orally bioavailable CHK1 inhibitor, with an IC 50 of 1.2 nM. GDC-0575 (100 nM) suppressses CHK1 activation induced by AraC by decreasing the level of Tyr15-phosphorylated CDK2. GDC-0575 (100 nM) has no effect on the viability of AML cells, but significantly reduces cell viability and induces apoptosis in combination with AraC. In addition, GDC-0575 plus AraC shows no effect on normal hematopoietic stem and progenitor cells (HSPCs). GDC-0575 shows cytotoxic activity against most of 20 melanoma cell lines tested, but several cell lines grown as tumour sphere (TS) are relatively insensitive. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GDC-0575 (7.5 mg/kg, p.o.) in combination with AraC alomost completely eradicates leukemic burden in mice transplanted with U937-Luc cells, and shows more efficient activity than AraC alone. Furthermore, GDC-0575 elevates the cytotoxicity of AraC in different primary AML models in vivo . GDC-0575 (25, 50 mg/kg, p.o.) dose-dependently inhibits the growth of tumor in D20 and C002 xenografts. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:Chk1 1.2 nM (IC 50 )

规格

别名
GDC-0575 二盐酸盐
规格或纯度
10mM in DMSO
英文名称
GDC-0575 dihydrochloride
生化机理
GDC-0575 二盐酸盐(ARRY-575 二盐酸盐)是一种口服生物活性 CHK1 抑制剂,IC 50 为 1.2 nM,具有抗肿瘤活性。
储存条件
干燥,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
PubChem CID
分子量
451.19

技术文档

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