产品
编 号：F756406
分子式：C22H16ClFN2O4
分子量：426.82
分子式：C22H16ClFN2O4
分子量：426.82
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2858800-98-1
产品详情
生物活性：
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.
体内研究：
OTUB1/USP8-IN-1 (compound 61; 10 nM-10 μM; 72 h) decreases the tumor burden in the H1975 xenograft mouse model.Animal Model:Female BALB/c nude mice with H1975 xenografts (5 weeks of age)
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)
Dosage:1 and 10 mg/kg
Administration:Intravenous injection (1 mg/kg) and oral administration (10 mg/kg)
Result:1.19 Administrationi.v. (1 mg/kg)p.o. (10 mg/kg)
T1/2 (h)0.831.75
Tmax (h)0.33
Cmax (μg/L)4274
AUC (μg·h/L)13453747
CL (L/h/kg)44
Vdss (L/kg)0.77
体外研究：
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.OTUB1/USP8-IN-1 (500 nM; 24 h) decreases in protein levels of both UBE2N and EGFR in H1975 cells.
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.
体内研究：
OTUB1/USP8-IN-1 (compound 61; 10 nM-10 μM; 72 h) decreases the tumor burden in the H1975 xenograft mouse model.Animal Model:Female BALB/c nude mice with H1975 xenografts (5 weeks of age)
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)
Dosage:1 and 10 mg/kg
Administration:Intravenous injection (1 mg/kg) and oral administration (10 mg/kg)
Result:1.19 Administrationi.v. (1 mg/kg)p.o. (10 mg/kg)
T1/2 (h)0.831.75
Tmax (h)0.33
Cmax (μg/L)4274
AUC (μg·h/L)13453747
CL (L/h/kg)44
Vdss (L/kg)0.77
体外研究：
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.OTUB1/USP8-IN-1 (500 nM; 24 h) decreases in protein levels of both UBE2N and EGFR in H1975 cells.
产品资料
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