2. Cell Cycle/DNA Damage Epigenetics PI3K/Akt/mTOR Apoptosis
  3. PARP ATM/ATR Apoptosis
  4. ATR/PARP1-IN-1

ATR/PARP1-IN-1 是一种 ATR/PARP1 双重抑制剂，对 ATR 的 IC50 为 17.3 nM，对 PARP1 的 IC50 为 0.38 nM。ATR/PARP1-IN-1 能有效降低细胞活力，诱导细胞凋亡 (apoptosis) 和 DNA 损伤。ATR/PARP1-IN-1 在三阴性乳腺癌 (TNBC) 模型中显著抑制了集落形成、迁移和侵袭。ATR/PARP1-IN-1 在 MDA-MB-468 移植瘤小鼠模型中有效抑制了肿瘤生长，且未引起显著体重变化。

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ATR/PARP1-IN-1 Chemical Structure

ATR/PARP1-IN-1 Chemical Structure

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Customer Review

ATR/PARP1-IN-1 相关抗体

Top Publications Citing Use of Products

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

查看 ATM/ATR 亚型特异性产品:

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ATM ATR

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ATR/PARP1-IN-1 is a potent ATR and PARP1 dual inhibitor with IC50s of 17.3 nM and 0.38 nM, respectively. ATR/PARP1-IN-1 effectively reduces cell viability, induces apoptosis and DNA damage. ATR/PARP1-IN-1 significantly impairs triple-negative breast cancer (TNBC) colony formation, migration, and invasion. ATR/PARP1-IN-1 suppresses tumor growth effectively in MDA-MB-468 xenografted mice, with no significant body weight change[1].

IC50 & Target[1]

PARP1

0.38 nM (IC50)

PARP2

5.1 nM (IC50)

TNKS1

116 nM (IC50)

TNKS2

740.5 nM (IC50)

PARP7

28.5 nM (IC50)

ATM

＞5000 nM (IC50)

ATR

17.3 nM (IC50)

PI3Kα

＞2500 nM (IC50)

DNA-PK

＞5000 nM (IC50)

体外研究
(In Vitro)

ATR/PARP1-IN-1 (Compound B8) 在 TNBC 细胞中显示出抗增殖活性，其对 MDA-MB-231 的 IC50 为 1.89 μM，对 MDA-MB-468 的 IC50 为 0.32 μM，对 MDA-MB-436 的 IC50 为 0.009 μM[1]。

ATR/PARP1-IN-1 (0.5-1 μM, 48 h) 在 MDA-MB-231 和 MDA-MB-468 细胞中诱导 G2/M 期细胞周期阻滞，其效果显著强于 Ceralasertib (AZD6738) (HY-19323) 和 Olaparib (HY-10162) 的联合用药[1]。

ATR/PARP1-IN-1 (0.5-1 μM, 72 h) 在 MDA-MB-231 和 MDA-MB-468 细胞中，通过 Annexin V/PI 染色实验检测，显示出比 AZD6738 和 Olaparib 联合用药更强的诱导凋亡能力[1]。

ATR/PARP1-IN-1 (0.5-1 μM, 10天) 对 MDA-MB-231 和 MDA-MB-468 细胞的集落形成率、迁移和侵袭的抑制作用显著强于 AZD6738 或 Olaparib 单药治疗，以及它们的联合用药[1]。

ATR/PARP1-IN-1 (1-2 μM, 48 h) 干扰 MDA-MB-468 细胞的上皮-间质转化 (EMT)[1]。

ATR/PARP1-IN-1 (0.5-1 μM, 48 h) 在 MDA-MB-231 和 MDA-MB-468 细胞中诱导显著的 DNA 损伤[1]。

ATR/PARP1-IN-1 (1-2 μM, 48 h) 在 MDA-MB-468 细胞中通过抑制 ATR 来抑制 CHK1 磷酸化[1]。

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

ATR/PARP1-IN-1 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells and MDA-MB-468 cells
Concentration: 0.5, 1 μM
Incubation Time: 48 h
Result: Induced G2/M cell cycle arrest in MDA-MB-231 cells and MDA-MB-468 cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells and MDA-MB-468 cells
Concentration: 0.5, 1 μM
Incubation Time: 72 h
Result: Induced apoptosis in MDA-MB-231 cells and MDA-MB-468 cells.

Immunofluorescence[1]

Cell Line: MDA-MB-231 cells and MDA-MB-468 cells
Concentration: 0.5, 1 μM
Incubation Time: 48 h
Result: Increased tail intensity more markedly than AZD6738, Olaparib, and their combination treatment.
Increased the formation of γH2AX.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 1, 2 μM
Incubation Time: 48 h
Result: Decreased the protein expression of BCL-2.
Induced more BAX and cleaved-caspase-3 protein expression compared to the combination of AZD6738 and Olaparib.
Increased the expression of the epithelial cell marker E-cadherin.
Decreased the expression of the mesenchymal cell marker Vimentin.
Reduced the protein levels of both ATR and PARP1.
Increased the DSB marker γH2AX.
Decreased CHK1Ser345 phosphorylation.
Enhanced CDK1 Tyr15 phosphorylation.
体内研究
(In Vivo)

ATR/PARP1-IN-1 (25-50 mg/kg，腹腔注射，每日两次，持续 28 天) 在 MDA-MB-468 移植瘤小鼠模型中显示出良好的抗肿瘤功效，并具有良好的安全性[1]。

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

Animal Model: Female nude mice were subcutaneously with MDA-MB-468 cells (1 x107)[1]
Dosage: 25, 50 mg/kg
Administration: i.p. daily for 28 days
Result: Suppressed the growth of MDA-MB-468 xenografted mice.
Decreased Ki67 expression and increased γH2AX and cleaved-caspase-3 expression.
Showed no significant effect on body weight.
Did not cause significant changes in organ structure or cellular morphology of heart, liver, spleen, lungs, and kidneys.
分子量

820.87

Formula

C45H41FN10O5
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

ATR/PARP1-IN-1 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:

ATR/PARP1-IN-1PARPATM/ATRApoptosispoly ADP ribose polymerase Ataxia telangiectasia mutatedATM and RAD3 relatedATRPARP1MDA-MB-468MDA-MB-231cancerInhibitorinhibitorinhibit

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