2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. ATM/ATR
  4. ATM-IN-13

ATM-IN-13 (A36) 是一种具有口服活性的选择性 ATM 激酶抑制剂，对人源 IC50 为 0.3 nM。ATM-IN-13 可阻断 ATM 介导的 DNA 双链断裂修复信号通路，降低 ATM 和 p53 的磷酸化水平，并抑制 ATM 依赖性 DNA 损伤应答。ATM-IN-13 可用于结直肠癌的研究。

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ATM-IN-13

ATM-IN-13 Chemical Structure

CAS No. : 3104731-13-4

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ATM-IN-13 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ATM-IN-13 (A36) is an orally active, selective ATM kinase inhibitor with a human IC50 of 0.3 nM. ATM-IN-13 blocks the ATM-mediated DNA double-strand break repair signaling pathway, reduces the phosphorylation levels of ATM and p53, and inhibits ATM-dependent DNA damage response. ATM-IN-13 can be used in the research of colorectal cancer[1].

体外研究
(In Vitro)

ATM-IN-13 (A36) 可强效抑制纯化的 ATM 激酶，其 IC50 为 0.3 nM[1]。
ATM-IN-13 (A36) 具有高激酶选择性，相对于其 0.3 nM 的 ATM IC50[1]，对 ATR、mTOR 和 PI3Kα 的选择性超过 3333 倍，对 DNA-PK 的选择性为 493 倍。
ATM-IN-13 (A36) 可抑制经 2 Gy 照射的 HCT116 结直肠癌细胞的增殖，其 IC50 为 1.7 nM[1]。
ATM-IN-13 (A36) (20-40 nM; 6 days) 可强效提升伊立替康在 HCT116 和 SW620 结直肠癌细胞中的细胞毒性，且在 SW620 细胞中具有更强的协同作用[1]。
ATM-IN-13 (A36) (10-20 nM) 可增强伊立替康抑制结直肠癌细胞集落形成的能力[1]。
ATM-IN-13 (A36) (2 μM) 可抑制伊立替康激活的 ATM 信号通路在 HCT116 结直肠癌细胞中的作用，降低 γ-H2AX、磷酸化 ATM 及磷酸化 p53 的水平[1]。
ATM-IN-13 (A36) (0.5-2 μM) 可浓度依赖性地降低伊立替康诱导的 HCT116 结直肠癌细胞中 γ-H2AX 水平，证实其对 ATM 介导的 DNA 损伤信号通路具有抑制作用[1]。
ATM-IN-13 (A36) (0.008-1 μM; 48 h) 单独作用不会改变 HCT116 或 SW620 结直肠癌细胞的细胞周期分布，但会以浓度依赖的方式增强伊立替康诱导的 G2/M 期阻滞[1]。
ATM-IN-13 (A36) (0.25-0.5 μM; 48 h) 单独作用不会诱导 HCT116 结直肠癌细胞发生凋亡，但会以浓度依赖的方式增强伊立替康诱导的凋亡[1]。
ATM-IN-13 (A36) 在人源和大鼠肝微粒体、小鼠/大鼠血浆中具有良好的代谢稳定性，在小鼠肝微粒体中稳定性较差，且在 25°C (pH 7) 时的水溶性极佳，达 1258.1 μg/mL[1]。
ATM-IN-13 (A36) 具有较低的药物-药物相互作用潜力，对 CYP1A2、CYP2C9、CYP2C19、CYP2D6 和 CYP3A4 的抑制作用 IC50 > 30 μM[1]。

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

ATM-IN-13 相关抗体:

Cell Viability Assay[1]

Cell Line: HCT116 and SW620 colorectal cancer cells
Concentration: 20 nM, 40 nM (combination with irinotecan)
Incubation Time: 6 days
Result: Reduced the irinotecan IC50 by 10.2-fold and 12.2-fold in HCT116 cells when used at 20 nM and 40 nM in combination with irinotecan, respectively.
Reduced the irinotecan IC50 by 84.3-fold and 253-fold in SW620 cells when used at 20 nM and 40 nM in combination with irinotecan, respectively.

Cell Cycle Analysis[1]

Cell Line: HCT116 and SW620 colorectal cancer cells
Concentration: 1 μM (HCT116, monotherapy); 0.25 μM, 0.5 μM, 1 μM (HCT116, combination with 1 μM irinotecan); 0.2 μM (SW620, monotherapy); 0.008 μM, 0.04 μM, 0.2 μM (SW620, combination with 0.1 μM irinotecan)
Incubation Time: 48 h
Result: Had no effect on cell cycle distribution in HCT116 cells when used alone at 1 μM.
Increased the percentage of HCT116 cells in G2/M phase to 66.09%, 68.8%, and 78.01% when used at 0.25 μM, 0.5 μM, and 1 μM in combination with 1 μM irinotecan, respectively.
Had no effect on cell cycle distribution in SW620 cells when used alone at 0.2 μM.
Increased the percentage of SW620 cells in G2/M phase to 57.92%, 58.56%, and 60.26% when used at 0.008 μM, 0.04 μM, and 0.2 μM in combination with 0.1 μM irinotecan, respectively.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-t Vz CL Bioavailability
Mice[1] 5 mg/kg i.v. 3.2 h 0.08 h 319.0 ng/mL 914.5 ng·h/mL 0.02 L/kg 0.01 L/h/kg /
Mice[1] 5 mg/kg p.o. 2.1 h 1.3 h 175.6 ng/mL 736.6 ng·h/mL 0.02 L/kg 0.01 L/h/kg 80.5 %
体内研究
(In Vivo)

ATM-IN-13 (A36) (20-40 mg/kg；灌胃；每日一次；连续 12 天) 与脂质体伊立替康联合使用时，在 HCT116 结直肠癌异种移植模型中分别实现了 82.3%和 92.6%的肿瘤生长抑制率，且安全性良好[1]。
ATM-IN-13 (10-20 mg/kg；灌胃；每日一次；连续 16 天) 与脂质体伊立替康联合使用时，在 SW620 结直肠癌异种移植模型中分别实现 80.8%和 91.1%的肿瘤生长抑制率，且安全性良好[1]。

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

Animal Model: Immunodeficient nude mice (implanted with HCT116 human colorectal cancer cells)[1]
Dosage: 20 mg/kg (combination TGI); 40 mg/kg (monotherapy TGI, combination TGI); 2 mg/kg (liposomal irinotecan)
Administration: p.o.; daily; 12 days
Result: Achieved a tumor growth inhibition (TGI) rate of 41.7% (monotherapy, 40 mg/kg).
Achieved TGI rates of 82.3% (20 mg/kg + liposomal irinotecan) and 92.6% (40 mg/kg + liposomal irinotecan).
Showed statistically significant enhanced efficacy in the 40 mg/kg combination group compared to single-agent groups.
Caused no treatment-related fatalities and only moderate body weight loss in the high-dose group.
Animal Model: Immunodeficient nude mice (implanted with SW620 human colorectal cancer cells)[1]
Dosage: 10 mg/kg (combination TGI); 20 mg/kg (monotherapy TGI, combination TGI); 2 mg/kg (liposomal irinotecan)
Administration: p.o.; daily; 16 days
Result: Achieved a tumor growth inhibition (TGI) rate of 28.4% (monotherapy, 20 mg/kg) without causing body weight loss.
Achieved TGI rates of 80.8% (10 mg/kg + liposomal irinotecan) and 91.1% (20 mg/kg + liposomal irinotecan).
Showed statistically significant enhanced efficacy in combination groups compared to liposomal irinotecan monotherapy.
Caused no treatment-related fatalities across all dosing regimens.
分子量

443.58

Formula

C27H33N5O
CAS 号
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

ATM-IN-13 相关分类

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  • 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.

Keywords:

ATM-IN-133104731-13-4ATM/ATRAtaxia telangiectasia mutatedATM and RAD3 relatedmTORcolorectal cancerATM kinaseHCT116 colorectal cancer cellsATRhuman liver microsomesDNA double-strand break repair signaling pathwayp53DNA-PKPI3KαInhibitorinhibitorinhibit

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