PARP-2-IN-3

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PARP-2-IN-3 (Compound 12) 是一种有效的 PARP-2 抑制剂，其 IC50 为 0.07 μM。 PARP-2-IN-3 诱导癌细胞凋亡 (apoptosis) 和坏死。 PARP-2-IN-3 具有较好的预测药代动力学参数和口服生物利用度。

PARP-2-IN-3 (Compound 12) is a potent PARP-2 inhibitor with an IC50 of 0.07 μM. PARP-2-IN-3 induces apoptosis and necrosis in cancer cells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability.

PARP-2-IN-3 (Compound 12) (24 h) shows cytotoxic activities with IC50s of 6.14±0.5 μM and 6.05±0.4 μM against MDA-MB-231 and MCF-7, respectively.PARP-2-IN-3 (6.05 μM; 24 h) arrests cell cycle at G2/M phase, and induces apoptosis and necrosis in MCF-7 cells.PARP-2-IN-3 fills the space inside the PARP-2 pocket in a manner similar to Olaparib (HY-10162).Cell Cytotoxicity Assay Cell Line:MDA-MB-231 and MCF-7 Concentration: Incubation Time:24 h Result:Displayed remarkable cytotoxic activities with IC50s of 6.14±0.5 μM and 6.05±0.4 μM against MDA-MB-231 and MCF-7, respectively.Cell Cycle Analysis Cell Line:MCF-7 Concentration:6.05 μM Incubation Time:24 h Result:The percentage of cells in pre-G1 phase increased from 1.85% to 33.47%, while in G2/M phase increased from 11.84% to 32.04%. The percentage of cells in S phase slightly decreased from 29.95% to 26.18% and in G0/G1 phase decreased from 58.21% to 41.78%.Apoptosis Analysis Cell Line:MCF-7 Concentration:6.05 μM Incubation Time:24 h Result:Induced an early apoptotic effect 22.52% and late apoptotic effect 3.72% in comparison to the untreated negative control MCF-7 cells which induced an early and late apoptotic effect 0.37% and 0.33%, respectively.

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Cell Cycle/DNA Damage

PARP

PARP | Apoptosis

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2915650-86-9

385.84

C20H20ClN3O3

>98% (HPLC)

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O=C(NC=1C=CC(=CC1)C2=NC3=CC(Cl)=CC=C3O2)CCN4CCOCC4

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(-20℃)

With Ice Pack

≥ 2 years