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

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 可通过选择抗癌活性分子增强抗肿瘤活性。

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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 ¥1430
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1 mg ¥520
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5 mg ¥1300
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10 mg ¥2100
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25 mg ¥4200
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50 mg ¥6700
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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 agents[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
性状

固体

颜色

Off-white to light yellow

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 中的溶解度 : 5 mg/mL (13.06 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6120 mL 13.0599 mL 26.1199 mL 65.2997 mL
5 mM 0.5224 mL 2.6120 mL 5.2240 mL 13.0599 mL
10 mM 0.2612 mL 1.3060 mL 2.6120 mL 6.5300 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
SAR-020106
目录号:
HY-100195
需求量: