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OTUB1/USP8-IN-1
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。
OTUB1/USP8-IN-1图片
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
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
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
分子量

426.82

Formula

C22H16ClFN2O4

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.