2. Cell Cycle/DNA Damage Epigenetics Protein Tyrosine Kinase/RTK Apoptosis
  3. PARP c-Met/HGFR Apoptosis
  4. PARP1/c-Met-IN-1

PARP1/c-Met-IN-1 (Compound 16) 是 PARP1 和 c-Met 的选择性双重抑制剂，IC50分别为 3.3 和 32.2 nM。PARP1/c-Met-IN-1 可以诱导细胞凋亡 (apoptosis)，在 G2/M 期阻滞细胞周期。PARP1/c-Met-IN-1 在小鼠体内表现出抗肿瘤活性。

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PARP1/c-Met-IN-1 Chemical Structure

PARP1/c-Met-IN-1 Chemical Structure

CAS No. : 2944101-99-7

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PARP1/c-Met-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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice[1].

IC50 & Target

PARP1

3.3 nM (IC50)

c-Met

32.2 nM (IC50)

体外研究
(In Vitro)

PARP1/c-Met-IN-1 (1 μM) 可提高 PARP1 和 c-Met 的热稳定性[1]。
PARP1/c-Met-IN-1 (1 μM) 抑制 PARP1 和 c-Met 相关蛋白 PAR，p-c-Met 和 p-AKT 的表达，影响 PARP1/c-Met 的相互作用，导致 DNA 损伤[1]。
PARP1/c-Met-IN-1 (0.5-1 μM) 通过下调 BRCA1 和 Rad51 的表达来减弱 MDA-MB-231 细胞的同源重组 (HR) 功能[1].

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

PARP1/c-Met-IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231
Concentration: 1 μM
Incubation Time: 72 h
Result: Enhanced the thermostability of these proteins within the temperature range of 43–55 °C.
Decreased expressions of BRCA1 and Rad51.
体内研究
(In Vivo)

PARP1/c-Met-IN-1 (12.5-100 mg/kg，腹腔注射，28 天) 在裸鼠肿瘤异种移植模型中抑制 MDA-MB-231 和 HCT116OR 异种移植的肿瘤，TGI) 分别为 49-77 % 和 62-70 %[1]。

PARP1/c-Met-IN-1 在 BALB/c mice 体内的药代动力学分析[1]

route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) AUC0-inf (ng·h/mL) MRT0-t (h) MRT0-inf (h) CLblood (mL/h/kg)
i.p. 10 1.42 0.25 152.47 95.42 96.70 1.67 1.77 121232

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

Animal Model: MDA-MB-231 and HCT116OR xenograft BALB/c nude mice[1]
Dosage: 12.5-50 mg/kg for MDA-MB-231 xenograft mice, 20-100 mg/kg for HCT116OR xenograft mice
Administration: I.p., 21 days for HCT116OR xenograft mice, 28 days for MDA-MB-231 xenograft mice
Result: Inhibited tumor growth with TGI of 49-77% in MDA-MB-231 xenograft mice.
Inhibited tumor growth with TGI of 62-70% in HCT116OR xenograft mice.
分子量

708.74

Formula

C40H33FN8O4
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

PARP1/c-Met-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:

PARP1/c-Met-IN-12944101-99-7PARPc-Met/HGFRApoptosispoly ADP ribose polymerase MDA-MB-231HCT116ORBALB/c miceInhibitorinhibitorinhibit

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