SAR-020106

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SAR-020106

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1184843-57-9

SAR-020106 是一种 ATP 竞争性的、选择性好的CHK1抑制剂，IC₅₀为 13.3 nM。SAR-020106 对 CHK2 具有良好的选择性。SAR-020106 在几种结肠肿瘤细胞系中以 p53 依赖性方式将 Gemcitabine 和 SN38 的细胞杀伤力提高了 3.0 到 29 倍。SAR-020106 可通过选择抗癌药物增强抗肿瘤活性。

生物活性

SAR-020106 is an ATP-competitive, potent, and selectiveCHK1inhibitor with anIC₅₀of 13.3 nM for humanCHK1. SAR-020106 shows excellent selectivity overCHK2. 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 drugs^[1]^[2].

IC₅₀& Target^[1]

Chk1

13.3 nM (IC₅₀)

体外研究
(In Vitro)

SAR-020106 (0.1-1 μM; 23 hours) abrogates an Etoposide-induced S and G2 arrest^[1].
SAR-020106 is capable of abrogating Etoposide-induced cell cycle arrest with an IC₅₀of 55 nM and 91 nM in HT29 and SW620 cells, respectively. SAR-020106 is relatively nontoxic with a GI₅₀of 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^[1].

体内研究
(In Vivo)

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^[1].

Animal Model:	Nude mice bearing SW620 xenograft tumors^[1]
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.

分子量

382.85

性状

Solid

Formula

C₁₉H₁₉ClN₆O

CAS 号

1184843-57-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 5 mg/mL(13.06 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.6120 mL	13.0599 mL	26.1199 mL
5 mM	0.5224 mL	2.6120 mL	5.2240 mL
10 mM	0.2612 mL	1.3060 mL	2.6120 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。