OTUB1/USP8-IN-1|西域试剂

OTUB1/USP8-IN-1,98.00%

产品编号：Bellancom-151563| 分子式：C₂₂H₁₆ClFN₂O₄| 分子量：426.82

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-151563	￥3000.00	杭州北京（现货）
Bellancom-151563	￥4800.00	杭州北京（现货）
Bellancom-151563	￥9500.00	杭州北京（现货）
Bellancom-151563	￥14500.00	杭州北京（现货）

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OTUB1/USP8-IN-1

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 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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 IC₅₀ values of 118, 145, 172, 431, and 1004 nM for H1975, H1703, EBC-1, H23, and A549 cells, respectively.

Western Blot Analysis

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

Administration	i.v. (1 mg/kg)	p.o. (10 mg/kg)
T_1/2 (h)	0.83	1.75
T_max (h)		0.33
C_max (μg/L)		4274
AUC (μg·h/L)	1345	3747
CL (L/h/kg)	44
Vdss (L/kg)	0.77

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

Administration	i.v. (1 mg/kg)	p.o. (10 mg/kg)
T_1/2 (h)	0.83	1.75
T_max (h)		0.33
C_max (μg/L)		4274
AUC (μg·h/L)	1345	3747
CL (L/h/kg)	44
Vdss (L/kg)	0.77

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.