2. Cell Cycle/DNA Damage Epigenetics Protein Tyrosine Kinase/RTK
  3. PARP c-Met/HGFR DNA/RNA Synthesis
  4. PARP1/c-Met-IN-2

PARP1/c-Met-IN-2 是一种高效具有口服活性的 PARP1 (IC50 = 21.8 nM) 和 c-Met (IC50 = 30.2 nM) 双重抑制剂。PARP1/c-Met-IN-2 可提高 γH2AX 的表达水平，导致 DNA 损伤。PARP1/c-Met-IN-2 在Olaparib (HY-10162) 耐药的 HCT116 细胞 (HCT116OR) 异种移植模型中表现出显著的抗肿瘤活性。PARP1/c-Met-IN-2 可用于结肠癌研究。

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PARP1/c-Met-IN-2

PARP1/c-Met-IN-2 Chemical Structure

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PARP1/c-Met-IN-2 相关抗体

Top Publications Citing Use of Products

查看 PARP 亚型特异性产品:

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PARP1/c-Met-IN-2 is a highly potent, orally active, PARP1 (IC50 = 21.8 nM) and c-Met (IC50 = 30.2 nM) dual inhibitor. PARP1/c-Met-IN-2 can elevate the expression level of γH2AX, cause DNA damage. PARP1/c-Met-IN-2 exhibits remarkable anti-tumor efficacy in the Olaparib (HY-10162)-resistant HCT116 (HCT116OR) xenograft models. PARP1/c-Met-IN-2 can be used for the study of Colon Cancer[1].

IC50 & Target

PARP1

21.8 nM (IC50)

c-Met

30.2 nM (IC50)

体外研究
(In Vitro)

PARP1/c-Met-IN-2 (Compound S12) 在体外对 HCT116OR 细胞表现出显著的抗增殖活性 (IC50 = 4.05)，并且在 NRK 细胞中表现出较高的安全性 (IC50 = 17.16)[1]。
在 MDA-MB-231 细胞中，当温度超过 43 ℃时，PARP1/c-Met-IN-2 (1 μM，72 h) 显著增强 c-Met 的热稳定性，表明 PARP1/c-Met-IN-2 可以直接与 PARP1 和 c-Met 相互作用[1]。
PARP1/c-Met-IN-2 (5 μM，72 h) 显著抑制 c-Met 磷酸化，但不改变 HCT116OR 细胞中 c-Met 蛋白的总表达水平[1]。
PARP1/c-Met-IN-2 (5 μM，72 h) 不仅显著提高 γH2AX 的表达水平，表明诱导了 DNA 损伤，并抑制了 c-Met 的活性，从而削弱了 PARP1 的活化，最终导致 PAR 水平下降，而且还降低了 HCT116OR 细胞中 PARP1 的蛋白表达水平[1]。

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

PARP1/c-Met-IN-2 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1 μM
Incubation Time: 72 h
Result: Significantly enhanced the thermal stability of c-Met.

Western Blot Analysis[1]

Cell Line: H2O2-Induced HCT116OR cells
Concentration: 5 μM
Incubation Time: 72 h
Result: Significantly suppressed c-Met phosphorylation without altering the total expression level of c-Met protein.

Western Blot Analysis[1]

Cell Line: HCT116OR cells
Concentration: 5 μM
Incubation Time: 72 h
Result: Markedly elevates the expression level of γH2AX.
Inhibited c-Met activity weakened the activation of PARP1.
Led to a decrease in the PAR level.
Decrease the protein expression level of PARP1.
体内研究
(In Vivo)

PARP1/c-Met-IN-2 (Compound S12) (25 mg/kg、50 mg/kg，腹腔注射，每日一次，连续 21 天) 可有效抑制小鼠中奥拉帕尼耐药的 HCT116OR 肿瘤的生长，且在测试剂量下未表现出明显毒性[1]。

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

Animal Model: Each 6 to 8-week-old female Balb/c nude mouse was subcutaneously inoculated with 200 μL of HCT116OR cells at a concentration of 1 × 107 under the right axillary tissue[1].
Dosage: 25 mg/kg, 50 mg/kg
Administration: I.p., once daily for 21 days
Result: Exhibited dose-dependent anti-tumor effects and could reverse the acquired resistance in HCT116OR cells, with tumor growth inhibition (TGI) values of 67 % and 72 %, respectively.
Did not cause any decrease in body weight in mice at either dosage, demonstrating a favorable safety profile in vivo.
分子量

676.12

Formula

C36H30ClN7O5
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

PARP1/c-Met-IN-2 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:

PARP1/c-Met-IN-2PARPc-Met/HGFRDNA/RNA Synthesispoly ADP ribose polymerasePARP1c-MetAcquired drug-resistanceDual target inhibitorInhibitorinhibitorinhibit

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