化合物 Miransertib (ARQ 092) HCl|T22247|TargetMol

Miransertib (ARQ 092) HCl
1313883-00-9

￥1640 10mg 起订

￥536 2mg 起订

￥882 5mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

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邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 Miransertib (ARQ 092) HCl

英文名称：: Miransertib (ARQ 092) HCl

CAS号：: 1313883-00-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

产品类别：: 抑制剂

货号：: T22247

Product Introduction

Bioactivity

名称	Miransertib (ARQ 092) HCl
描述	Miransertib hydrochloride (ARQ-092 hydrochloride) is a powerful, orally bioavailable, selective, and allosteric inhibitor of Akt. It exhibits an inhibitory concentration (IC50) of 2.7 nM, 14 nM, and 8.1 nM against Akt1, Akt2, and Akt3, respectively. In addition to its Akt inhibitory activity, Miransertib hydrochloride also demonstrates significant potency as an inhibitor of the AKT1-E17K mutant protein. This compound shows promise in research related to PI3K/AKT-driven tumors and Proteus syndrome. Furthermore, Miransertib hydrochloride displays efficacy against Leishmania [1, 2].
体外活性	In a large panel of cell lines derived from various tumor types, Miransertib (ARQ-092; Compound 21a) exhibits potent anti-proliferative activity in cell lines containing PIK3CA/PIK3R1 mutations compared to those with wild-type (wt) PIK3CA/PIK3R1 or PTEN loss. Miransertib exhibits 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 (IC 50 =0.31 μM) [1]. Miransertib is markedly effective against intracellular amastigotes of L. donovani or L. amazonensis -infected macrophages. Miransertib also enhances mTOR dependent autophagy in Leishmania -infected macrophages [2]
体内活性	Miransertib (ARQ-092; Compound 21a) exhibits 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 t 1/2 values of 17 h in rats versus 7 h in monkeys. The C max is 198 ng/mL and 258 ng/mL and the AUC inf was 5496 h ng/mL and 2960 h ng/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].
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
关键字	Miransertib (ARQ 092) HCl

Miransertib (ARQ 092) HCl|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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