货号	规格	价格	上海	北京	珠海	重庆	武汉
S87999-5mg买3赠1	98.10%	￥700.00 S87999-5mg ￥700.00 现货（买3赠1）	4 4	-	-	-	-
S87999-10mg买3赠1	98.10%	￥1200.00 S87999-10mg ￥1200.00 现货（买3赠1）	4 4	-	-	-	-
S87999-25mg买3赠1	98.10%	￥2200.00 S87999-25mg ￥2200.00 现货（买3赠1）	4 4	-	-	-	-
S87999-100mg	≥98%	￥6600.00 S87999-100mg ￥6600.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents

靶点：

Chk1:13.3 nM (IC50);Chk

体外研究：

SAR-020106 (0.1-1 μM; 23 hours) abrogates an Etoposide-induced S and G2 arrest.
SAR-020106 is capable of abrogating Etoposide-induced cell cycle arrest with an IC50 of 55 nM and 91 nM in HT29 and SW620 cells, respectively. SAR-020106 is relatively nontoxic with a GI50 of 0.48 μM in HT29 and 2 μM in SW620, resulting in an activity index of 8.7 and 22, respectively. SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion.

体内研究：

SAR-020106 (40 mg/kg; i.p.; administered on days 0, 1, 7, 8, 14, and 15) in combination with Irinotecan potentiates the antitumor activity in SW620 xenografts Animal Model: Nude mice bearing SW620 xenograft tumors Dosage: 40 mg/kg Administration: I.p.; administered on days 0, 1, 7, 8, 14, and 15 Result: There was a clear decrease in tumor growth associated with the combination with tumors reaching 300% by 12.5 days.

参考文献：

1. Walton MI, et al. The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106. Mol Cancer Ther. 2010;9(1):89-100.
2. Reader JC, et al. Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. J Med Chem. 2011;54(24):8328-8342.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.612 ml	13.06 ml	26.12 ml
5 mM	0.522 ml	2.612 ml	5.224 ml
10 mM	0.261 ml	1.306 ml	2.612 ml
50 mM	0.052 ml	0.261 ml	0.522 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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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

SAR-020106

(R)-5-((8-chloroisoquinolin-3-yl)amino)-3-((1-(dimethylamino)propan-2-yl)oxy)pyrazine-2-carbonitrile

参考文献

质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)