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Antitumor agent-81
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Antitumor agent-81图片
CAS NO:2765180-17-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
Antitumor agent-81 (化合物 5 a) 是一种低细胞毒性的P62-RNF168激动剂,能促进P62RNF168的相互作用。Antitumor agent-81 诱导RNF168介导的H2A泛素化减少,并损害同源重组介导的 DNA 修复。Antitumor agent-81 还能以剂量依赖的方式抑制小鼠异种移植肿瘤的生长。
生物活性

Antitumor agent-81 (compound 5a) is a low cytotoxicP62-RNF168agonist that promotes the interaction ofP62withRNF168. Antitumor agent-81 induces a decrease inRNF168-mediatedH2Aubiquitination and impairs homologous recombination-mediated DNA repair. Antitumor agent-81 also inhibits mice xenograft tumor growth in a dose-dependent manner[1].

体外研究
(In Vitro)

Antitumor agent-81 (0-20 μM; 72 h) exhibits antiproliferative activity in cells of the most common cancer types[1].
Antitumor agent-81 (1, 2, 5 μM; 24 h) compromises HR (homologous recombination)-mediated DSB repair in HCT-116 cells[1].
Antitumor agent-81 tethers the interaction between P62 and RNF168 in HCT-116 cells[1].
Antitumor agent-81 inhibits the catalytic activity of RNF168 and RNF168 E3 ligase activity in HCT-116 cells[1].

Cell Proliferation Assay[1]

Cell Line:A549, HCT-116, A375, HeLa, HepG2, MCF-7, MDA-MB-231, MGC-803, U2OS and MCF-10A cells
Concentration:0-20 μM
Incubation Time:72 h
Result:Inhibited A549, HCT-116, A375, HeLa, HepG2, MCF-7, MDA-MB-231, MGC-803, U2OS and MCF-10A cells, with IC50values of 1.18, 0.36, 1.93, 2.48, 19.61, 2.79, 1.17, 1.88, 3.64 and 6.98, respectively.

Cell Cycle Analysis[1]

Cell Line:HCT-116 cells
Concentration:1, 2, 5 μM
Incubation Time:24 h
Result:Induced a G2/M arrest but no significant accumulation of sub-G1 phase.
Compromised both HR(homologous recombination)- and NHEJ (non-homologous end joining)- mediated DSB repair in a dose-dependent manner, but HR was the more severely impacted process.
体内研究
(In Vivo)

Antitumor agent-81 (5, 10 mg/kg; i.p.; single every 3 days for 22 days) suppresses tumor volumes in a dose-dependent manner in mice[1].
1.19Pharmacokinetic Parameters of Antitumor agent-81 in Female BALB/c nude mice[1].

DoseT1/2(h)Cmax(ng/mL)AUC0-t(h?ng/mL)CL ((mL/h)/kg)
IP (5 mg/kg)16.1726.10215.6919647.83
IP (10 mg/kg)31.0039.87408.1816554.30
IP (20 mg/kg)22.1052.231003.5814669.81

Animal Model:Female BALB/c nude mice (xenograft tumor model)[1].
Dosage:5, 10 mg/kg
Administration:Intraperitoneal injection; single every 3 days for 22 days
Result:Suppressed tumor growth by promoting apoptosis in xenografted tumorigenesis.
Animal Model:Female BALB/c nude mice[1].
Dosage:5, 10, 20 mg/kg
Administration:Intraperitoneal injection; single
Result:Exhibited plasma concentration peaked 1 h after administration.
Showed a relatively high maximum concentration (Cmax= 52.23 ng/mL) and exposure (AUC0-t= 1003.58 hong/mL) at a dose of 20 mg/kg.
分子量

393.40

Formula

C19H19N7O3

CAS 号

2765180-17-2

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.