1. Cell Cycle/DNA Damage
  2. Checkpoint Kinase (Chk)
  3. SAR-020106

SAR-020106 

目录号: HY-100195 纯度: 98.53%
产品使用指南

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。

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SAR-020106 Chemical Structure

SAR-020106 Chemical Structure

CAS No. : 1184843-57-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2200
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5 mg ¥2000
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10 mg ¥3200
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25 mg ¥6000
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50 mg ¥9500
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查看 Checkpoint Kinase (Chk) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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 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 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C19H19ClN6O

CAS 号
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
SAR-020106
目录号:
HY-100195
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