1. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  2. ATM/ATR Apoptosis
  3. A011

A011 是一种有效的选择性 ataxia-telangiectasia mutated (ATM) 抑制剂,IC50 值为 1.0 nM。A011 与 CPT-11 (HY-16562) 结合使用时诱导细胞凋亡 (Apoptosis) 和细胞周期停滞在 G2/M 期。A011 与 CPT-11 结合显示出抗肿瘤活性。

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A011 Chemical Structure

A011 Chemical Structure

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查看 ATM/ATR 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

A011 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. A011 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). A011 combines with CPT-11 shows antitumor activity[1].

IC50 & Target[1]

ATM

1.0 nM (IC50)

体外研究
(In Vitro)

A011 (compound 8d) (10, 30, 100 nM; 5 days) 增加 SW620 和 HCT116 细胞对 CPT-11 (HY-16562) (100 nM) 的敏感性[1]
A011 (0-100 nM; 24, 72 h) 与 CPT-11 联用可诱导细胞凋亡和细胞周期停滞在 G2/M 期[1]
A011 (3, 9, 27, 83, 250 nM) 在 1.5 或 3 Gy 照射条件下以剂量依赖性方式降低 SW620 细胞中 p-ATM 和 p-Chk2 的表达[1] .

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

Cell Proliferation Assay[1]

Cell Line: SW620, HCT116 cells
Concentration: 10, 30, 100 nM
Incubation Time: 5 days
Result: Increased the sensitivity of SW620 and HCT116 cells to CPT-11 (100 nM).

Cell Cycle Analysis[1]

Cell Line: SW620, HCT116 cells
Concentration: 0-100 nM
Incubation Time: 24 h
Result: Dose-dependent increased in G2/M arrest was noted when A011 was combined with CPT-11 in SW620 and HCT116 cells.

Apoptosis Analysis[1]

Cell Line: SW620, HCT116 cells
Concentration: 0-100 nM
Incubation Time: 72 h
Result: Significantly increased the apoptotic cell populations when combined with CPT-11.

Western Blot Analysis[1]

Cell Line: SW620, HCT116 cells
Concentration: 3, 10, 30 nM
Incubation Time: 24 h
Result: Reduced the expression of p-Chk2 when combined with CPT-11.
体内研究
(In Vivo)

A011 (5 mg/kg;腹腔注射;每天一次,持续 23 天) 与 CPT-11 (5 mg/kg,腹腔注射;每周一次) 联合用药在小鼠体内显示出抗肿瘤活性[1]

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

Animal Model: Female nude mice (SW620 tumor xenograft model)[1]
Dosage: 5 mg/kg; CPT-11 (5 mg/kg, i.p.; once a week)
Administration: I.p.; once daily for 23 days
Result: Increased the antitumor activity of CPT-11.
分子量

452.55

Formula

C27H28N6O

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
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
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:
A011
目录号:
HY-149291
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