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. |
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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 | |
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| 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. |
