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- MedChemExpress(MCE)
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- HY-161372
- 2025年12月05日
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Please store the product under the recommended conditions in the Certificate of Analysis.
- 库存：
货期：询盘
- 供应商：
MedChemExpress LLC
- CAS号：
2944101-99-7
- 规格：
询盘
PARP1/c-Met-IN-1
产品活性：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。
产品来源： www.medchemexpress.cn/parp1-c-met-in-1.html
研究领域：Cell Cycle/DNA Damage | Epigenetics | Protein Tyrosine Kinase/RTK | Apoptosis
作用靶点：PARP | c-Met/HGFR | Apoptosis
In Vitro: PARP1/c-Met-IN-1 (1 μM) improves the thermal stability of PARP1 and c-Met.PARP1/c-Met-IN-1 (1 μM) inhibits the expressions of PARP1 and c-Met related proteins PAR, p-c-Met and p-AKT, affects the interactions of PARP1/c-Met, causes DNA damage.PARP1/c-Met-IN-1 (0.5-1 μM) diminishes the homologous recombination (HR) function in MDA-MB-231 cells through downregulating expressions of BRCA1 and Rad51.
In Vivo: PARP1/c-Met-IN-1 (12.5-100 mg/kg, i.p. for 28 days) exhibits antitumor efficacy with tumor growth inhibition (TGI) values of 49-77 % and 62-70 % in MDA-MB-231 and HCT116OR xenograft nude mice, respectively.Pharmacokinetic Analysis of PARP1/c-Met-IN-1 in BALB/c micerouteDose (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.101.420.25152.4795.4296.701.671.77121232
相关产品：MG-132 | Doxorubicin hydrochloride | Bafilomycin A1 | Tamoxifen | Olaparib | Y-27632 | LY294002 | Paclitaxel | Z-VAD-FMK | Acetylcysteine | Angiotensin II human | 2-Deoxy-D-glucose | Staurosporine | Actinomycin D | SB-431542 | 5-Fluorouracil | Bortezomib | Deferoxamine mesylate | Oxaliplatin | Trametinib | Sorafenib | Temozolomide | Gemcitabine | Decitabine | Mdivi-1 | Elesclomol | Rotenone | Etoposide | Ruxolitinib | SP600125
产品活性：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。
产品来源： www.medchemexpress.cn/parp1-c-met-in-1.html
研究领域：Cell Cycle/DNA Damage | Epigenetics | Protein Tyrosine Kinase/RTK | Apoptosis
作用靶点：PARP | c-Met/HGFR | Apoptosis
In Vitro: PARP1/c-Met-IN-1 (1 μM) improves the thermal stability of PARP1 and c-Met.PARP1/c-Met-IN-1 (1 μM) inhibits the expressions of PARP1 and c-Met related proteins PAR, p-c-Met and p-AKT, affects the interactions of PARP1/c-Met, causes DNA damage.PARP1/c-Met-IN-1 (0.5-1 μM) diminishes the homologous recombination (HR) function in MDA-MB-231 cells through downregulating expressions of BRCA1 and Rad51.
In Vivo: PARP1/c-Met-IN-1 (12.5-100 mg/kg, i.p. for 28 days) exhibits antitumor efficacy with tumor growth inhibition (TGI) values of 49-77 % and 62-70 % in MDA-MB-231 and HCT116OR xenograft nude mice, respectively.Pharmacokinetic Analysis of PARP1/c-Met-IN-1 in BALB/c micerouteDose (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.101.420.25152.4795.4296.701.671.77121232
相关产品：MG-132 | Doxorubicin hydrochloride | Bafilomycin A1 | Tamoxifen | Olaparib | Y-27632 | LY294002 | Paclitaxel | Z-VAD-FMK | Acetylcysteine | Angiotensin II human | 2-Deoxy-D-glucose | Staurosporine | Actinomycin D | SB-431542 | 5-Fluorouracil | Bortezomib | Deferoxamine mesylate | Oxaliplatin | Trametinib | Sorafenib | Temozolomide | Gemcitabine | Decitabine | Mdivi-1 | Elesclomol | Rotenone | Etoposide | Ruxolitinib | SP600125
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PARP1/c-Met-IN-1,2944101-99-7
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