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Miransertib (ARQ 092) HCl

产品编号 T22247 CAS 1313883-00-9

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].

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Miransertib (ARQ 092) HCl Chemical Structure

Miransertib (ARQ 092) HCl, CAS 1313883-00-9

规格	价格/CNY	货期
2 mg	￥ 536	5日内发货
5 mg	￥ 882	5日内发货
10 mg	￥ 1,640	5日内发货

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Miransertib (ARQ 092) HCl 的其他形式现货产品:

Miransertib

其他形式的 Miransertib (ARQ 092) HCl:

Miransertib
现货
Miransertib mesylate
询价

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生物活性

化学信息

存储 & 溶解度

产品描述	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].

分子量	468.98
分子式	C27H25ClN6
CAS No.	1313883-00-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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