| Chemical Properties | Back Directory | [Boiling point ]
609.4±65.0 °C(Predicted) | [density ]
1.440±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
8.72±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
OTUB1/USP8-IN-1 is a potent dual OTUB1/USP8 inhibitor with IC50 values of 0.17 and 0.28 nM for OTUB1 and USP8, respectively. OTUB1/USP8-IN-1 can be used in research of cancer[1]. | [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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| [References]
[1] Tan L, et, al. Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer. J Med Chem. 2022 Oct 11. DOI:10.1021/acs.jmedchem.2c00408 |
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