货号	规格	价格	上海	北京	珠海	重庆	武汉
S87690-5mg买3赠1	98.10%	￥1200.00 S87690-5mg ￥1200.00 现货（买3赠1）	4 4	-	-	-	-
S87690-10mg买3赠1	98.10%	￥1870.00 S87690-10mg ￥1870.00 现货（买3赠1）	5 5	-	-	-	-
S87690-25mg买3赠1	98.10%	￥3150.00 S87690-25mg ￥3150.00 现货（买3赠1）	5 5	-	-	-	-
S87690-100mg	≥98%	￥7200.00 S87690-100mg ￥7200.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2 nM.

靶点：

1.2 nM (Chk1)

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

参考文献：

1. Oo ZY, et al. Endogenous Replication Stress Marks Melanomas Sensitive to CHEK1 Inhibitors In Vivo. Clin Cancer Res. 2018 Mar 13. doi: 10.1158/1078-0432.CCR-17-2701. 2. Laroche-Clary A, et al. CHK1 inhibition in soft-tissue sarcomas: biological and clinical implications. Ann Oncol. 2018 Apr 1;29(4):1023-1029. 3. Di Tullio A, et al. The combination of CHK1 inhibitor with G-CSF overrides cytarabine resistance in human acute myeloid leukemia. Nat Commun. 2017 Nov 22;8(1):1679.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.644 ml	13.218 ml	26.436 ml
5 mM	0.529 ml	2.644 ml	5.287 ml
10 mM	0.264 ml	1.322 ml	2.644 ml
50 mM	0.053 ml	0.264 ml	0.529 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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