您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > Miransertib hydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Miransertib hydrochloride
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。
Miransertib hydrochloride图片
CAS NO:1313883-00-9
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
ARQ-092 hydrochloride
产品介绍
Miransertib hydrochloride (ARQ-092 hydrochloride) 是一种有效的,具有口服活性的,选择性和变构性Akt抑制剂,对Akt1Akt2Akt3IC50分别为 2.7 nM,14 nM 和 8.1 nM。Miransertib hydrochloride 还是有效的AKT1-E17K突变蛋白抑制剂,并可用于 PI3K/AKT 驱动的肿瘤和 Proteus 综合征的研究。Miransertib hydrochloride 有效抑制利什曼原虫 (Leishmania)。
生物活性

Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allostericAktinhibitor withIC50s of 2.7 nM, 14 nM and 8.1 nM forAkt1,Akt2,Akt3, respectively. Miransertib hydrochloride is also a potent theAKT1-E17K mutant proteininhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research[1]. Miransertib hydrochloride is effective againstLeishmania[2].

IC50& Target[1][2]

Akt1

2.7 nM (IC50)

Leishmania

 

Akt3

8.1 nM (IC50)

Akt2

174 nM (IC50)

Akt1 E17K mutant

 

体外研究
(In Vitro)

In a large panel of cell lines derived from various tumor types, Miransertib (ARQ-092; Compound 21a) shows potent anti-proliferative activity in cell lines containing PIK3CA/PIK3R1 mutations compared to those with wild-type (wt) PIK3CA/PIK3R1 or PTEN loss. Miransertib shows excellent inhibition of p-Akt (S473) and p-Akt (T308) in both AN3CA and A2780 cells. The inhibition of the downstream protein p-PRAS40 (T246) is observed with Miransertib (IC50=0.31 μM)[1].
Miransertib is markedly effective against intracellular amastigotes ofL. donovaniorL. amazonensis-infected macrophages. Miransertib also enhances mTOR dependent autophagy inLeishmania-infected macrophages[2]

体内研究
(In Vivo)

Miransertib (ARQ-092; Compound 21a) shows good absolute oral bioavailability in rats (5 mg/kg) and monkeys (10 mg/kg) with F values of 62% and 49%, respectively. The half-life is longer in rats compared to monkeys with t1/2values of 17 h in rats versus 7 h in monkeys. The Cmaxis 198 ng/mL and 258 ng/mL and the AUCinfwas 5496 hong/mL and 2960 hong/mL in rats and monkeys, respectively[1].
Miransertib (ARQ-092; Compound 21a) inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma[1].

Clinical Trial
分子量

468.98

Formula

C27H25ClN6

CAS 号

1313883-00-9

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.