PARP1/c-Met-IN-1_product_DataBase

Bioactivity	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].
Invitro	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. 0 --> PARP1/c-Met-IN-1 相关抗体: Western Blot Analysis[1] Cell Line:
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
CAS	2944101-99-7
Formula	C40H33FN8O4
Molar Mass	708.74
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Sun Z, et al., Rational Design of PARP1/c-Met Dual Inhibitors for Overcoming PARP1 Inhibitor Resistance Induced by c-Met Overexpression. J Med Chem. 2024 Mar 28;67(6):4916-4935.

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