OTUB1/USP8-IN-1 是一种有效的双重OTUB1/USP8抑制剂,抑制 OTUB1 和 USP8 的IC50值分别为 0.17 和 0.28 nM。OTUB1/USP8-IN-1 可用于癌症的研究。
生物活性 | OTUB1/USP8-IN-1 is a potent dualOTUB1/USP8inhibitor withIC50values of 0.17 and 0.28 nM forOTUB1and USP8, respectively. OTUB1/USP8-IN-1 can be used in research ofcancer[1]. |
IC50& Target | IC50: 0.17 nM (OTUB1) and 0.28 nM (USP8)[1] |
体外研究 (In Vitro) | OTUB1/USP8-IN-1 (compound 61; 10 nM-10 μM; 72 h) has antiproliferative effects in KRAS-WT (H1975, EBC-1, H1703) and KRAS-mutated (H23, A549) NSCLC cell lines[1]. OTUB1/USP8-IN-1 (500 nM; 24 h) decreases in protein levels of both UBE2N and EGFR in H1975 cells[1].
Cell Viability Assay[1] Cell Line: | KRAS-WT (H1975, EBC-1, H1703) and KRAS-mutated (H23, A549) NSCLC cell lines | Concentration: | 10 nM-10 μM | Incubation Time: | 72 hours | Result: | Inhibited cell proliferative with IC50values of 118, 145, 172, 431, and 1004 nM for H1975, H1703, EBC-1, H23, and A549 cells, respectively. |
Western Blot Analysis[1] Cell Line: | H1975 cells | Concentration: | 500 nM | Incubation Time: | 24 hours | Result: | Decreased the levels of both UBE2N and EGFR in a dose-dependent manner. |
|
体内研究 (In Vivo) | OTUB1/USP8-IN-1 (compound 61; 10 nM-10 μM; 72 h) decreases the tumor burden in the H1975 xenograft mouse model[1].
Animal Model: | Female BALB/c nude mice with H1975 xenografts (5 weeks of age)[1] | Dosage: | 5 mg/kg | Administration: | Intraperitoneal injection; QD and BID, for 2 weeks | Result: | Reduced total tumor weight and average tumor volume in an over twofold with BID dosing. |
Animal Model: | Female BALB/c nude mice with H1975 xenograft (5 weeks of age)[1] | Dosage: | 1 and 10 mg/kg | Administration: | Intravenous injection (1 mg/kg) and oral administration (10 mg/kg) | Result: | 1.19|
Administration | i.v. (1 mg/kg) | p.o. (10 mg/kg) | T1/2(h) | 0.83 | 1.75 | Tmax(h) | | 0.33 | Cmax(μg/L) | | 4274 | AUC (μg·h/L) | 1345 | 3747 | CL (L/h/kg) | 44 | | Vdss (L/kg) | 0.77 | |
|
|
分子量 | |
Formula | |
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. |