ATM Inhibitor-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ATM Inhibitor-1 

ATM Inhibitor-1 是一种有效、选择性、可口服的 ATM 抑制剂，IC50 值为 0.7 nM，对 mTOR (IC50，21 μM)，DNAPK (IC50，2.8 μM)，PI3Kα (IC50，3.8 μM)，PI3Kβ (IC50，10.3 μM)，PI3Kγ (IC50，3 μM) 和 PI3Kδ (IC50，0.73 μM) 的作用很弱。ATM Inhibitor-1 具有抗肿瘤活性。

ATM Inhibitor-1

ATM Inhibitor-1 Chemical Structure

CAS No. : 2135639-94-8

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生物活性

ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity[1].

IC50 & Target[1]

ATM

0.7 nM (IC50)

ATM

2.8 nM (IC50, Cellular assay)

mTOR

21 μM (IC50)

DNAPK

2.8 μM (IC50)

PI3Kα

3.8 μM (IC50)

PI3Kβ

10.3 μM (IC50)

PI3Kγ

3 μM (IC50)

PI3Kδ

0.73 μM (IC50)

体外研究
(In Vitro)

ATM Inhibitor-1 (Compound 21) is a highly potent, selective and orally active ATM Inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM)[1].
In cellular assays, ATM Inhibitor-1 exhibits IC50s of 2.8 nM, >30 μM and >19 μM for ATM, ATR/PI3Kα and PI3Kβ/mTOR, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

ATM Inhibitor-1 (Compound 21; 50 mg/kg p.o. once daily for 3 days every week starting 24 h post-irinotecan dosing, 21 days) in combination with 50 mg/kg irinotecan significantly reduces tumor growth in SW620 mice model[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SW620 mice model[1]
Dosage: 50 mg/kg
Administration: P.O., once daily for 3 days every week starting 24 h post-irinotecan dosing, 21 days
Result: Inhibited the growth of tumor combined with 50 mg/kg irinotecan in SW620 mice model.

分子量

492.61

Formula

C27H36N6O3
CAS 号

2135639-94-8
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.
参考文献

  • [1]. Barlaam B, et al. Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors. CS Med Chem Lett. 2018 Jul 13;9(8):809-814.

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