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

ATM-IN-2 是一种选择性且口服有效的 ATM 抑制剂，其 IC50 为 4 nM。ATM-IN-2 具有高度的激酶选择性 (相对于 PIKK 家族成员的选择性超过 700 倍)。ATM-IN-2 通过抑制 ATM 磷酸化和下游信号通路 (p53、H2AX) 发挥抗肿瘤作用并促进细胞凋亡 (apoptosis)。ATM-IN-2 可用于实体瘤，如结肠癌的研究。

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ATM-IN-2

ATM-IN-2 Chemical Structure

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ATM-IN-2 相关抗体

Top Publications Citing Use of Products

查看 ATM/ATR 亚型特异性产品:

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ATM ATR TRRAP

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ATM-IN-2 is a selective and orally active ATM inhibitor with an IC50 of 4 nM. ATM-IN-2 exhibits excellent kinase selectivity (>700-fold over PIKK family members). ATM-IN-2 exerts its anti-tumor effect by inhibiting ATM phosphorylation and the downstream signaling pathways (p53, H2AX), and promotes cell apoptosis. ATM-IN-2 can be used for the study of chemosensitizer candidate such as colon cancer[1].

IC50 & Target[1]

ATM

4 nM (IC50)

体外研究
(In Vitro)

ATM-IN-2 (Compound 25a) (0-10000 nM, 6-7 days) 对 HEL116 和 SW620 细胞显示出良好的抑制活性，IC50 值分别为 58.2 和 66.6 nM，并有效抑制细胞克隆形成能力[1]。
ATM-IN-2 (1-4 μM, 2 days) 通过加剧 G2/M 期停滞、促进细胞凋亡，增强了 Irinotecan (HY-16562) 的治疗效果，并在 HCT116 细胞中实现了协同的抗增殖作用[1]。
ATM-IN-2 (0.25-2 μM, 4 h) 显著抑制了 HCT116 和 SW620 细胞中的 ATM 信号激活[1]。

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

ATM-IN-2 相关抗体:

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 1, 2, 4 μM co-treated with Irinotecan (HY-16512)
Incubation Time: 2 days
Result: Alone had no significant effect on the cell cycle.
Increased the G2/M phase population in a concentration-dependent manner accompanied by a reduction in the G0/G1 phase population.

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 1, 2, 4 μM co-treated with Irinotecan
Incubation Time: 2 days
Result: Exhibited significantly higher apoptosis rates compared to monotherapy.

Western Blot Analysis[1]

Cell Line: HCT116 and SW620 cells
Concentration: 0.5, 1, 2 μM in HCT116 cells and 0.25, 0.5, 1 μM in SW620 cells
Incubation Time: 4 h
Result: Reduced the phosphorylation levels of ATM-S1981 and p53.
Reduced the accumulation of γH2AX.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 10 mg/kg i.v. Cmax 1460.9 ng/mL
Mice 10 mg/kg p.o. Tmax 1.32 h
Mice 10 mg/kg i.v. Tmax 0.08 h
Mice 10 mg/kg p.o. T1/2 4.1 h
Mice 10 mg/kg i.v. T1/2 4 h
Mice 10 mg/kg p.o. AUC0-t 14841.7 ng·h/mL
Mice 10 mg/kg i.v. AUC0-t 10055.3 ng·h/mL
Mice 10 mg/kg p.o. F 147.6 %
Mice 10 mg/kg p.o. Cmax 1285.8 ng/mL
体内研究
(In Vivo)

ATM-IN-2 (Compound 25a) (15-30 mg/kg, p.o., 共 14-20 天) 在小鼠异种移植模型的癌症治疗中与 Irinotecan 发挥协同抗肿瘤作用[1]。

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

Animal Model: Xenograft model induced by HCT116 or SW620 cells established in 6-weeks NOD-SCID mice[1]
Dosage: 30 mg/kg alone and 15 and 30 mg/kg with 2 mg/kg Irinotecan in HCT116 model; 45 mg/kg with 2 mg/kg Irinotecan in SW620 model
Administration: Oral administration (p.o.), for 14 days in HCT116 model and 20 days for SW620 model
Result: Demonstrated superior antitumor at high-dose coadministration with Irinotecan in HCT116 model.
Demonstrated a favorable safety profile with little body weight loss observed in HCT116 model.
Demonstrated a dose-dependent enhancement of inhibitory effects in SW620 model.
分子量

443.52

Formula

C25H21N3O3S
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-2 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

ATM-IN-2ATM/ATRApoptosisAtaxia telangiectasia mutatedATM and RAD3 relatedIrinotecanXenograft modelHCT116 cellsSW620 cellsBALB/c miceInhibitorinhibitorinhibit

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