供货周期: | 一周 |
品牌: | 爱必信 |
规格: | >98% |
货号: | abs814659 |
CAS号: | 1196541-47-5 |
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抑制剂描述: 产品名称:GDC-0575 产品别名:见爱必信官网 英文别名:GDC-0575 靶点:Chk CAS:1196541-47-5 纯度:>98% 外观:见爱必信官网 保存方法:Store at -20°C 描述: GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2?nM. 溶解性:DMSO :75 mg/mL (198.27 mM) 体外研究: GDC-0575 is significantly more potent in promoting DNA damage, replication stress and cell death than V158411, LY2603618, and MK-8776 in a panel of melanoma cell lines. GDC-0575 abrogates DNA damage-induced S and G2–M checkpoints, exacerbates DNA double-strand breaks and induces apoptosis in STS cells. GDC-0575 has a synergistic or additive effect together with gemcitabine. CHK1 inhibitor GDC-0575 in combination with AraC enhances the killing of primary acute myeloid leukemia cells ex vivo by inducing apoptosis. 体内研究:GDC-0575 is active at 25 mg/kg as a single agent, but the efficacy is improved at the higher drug dose. GDC-0575 effectively blocks tumor growth in the D20 and C002 xenografts, and the effect is maintained for at least 10 days after the final dose is administered.
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