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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
ARQ-092 hydrochloride
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1313883-00-9
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1119.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥1085.0 |
| 规格： | 10 mg | 产品价格： | ￥1740.0 |
| 规格： | 25 mg | 产品价格： | ￥3475.0 |
| 规格： | 50 mg | 产品价格： | ￥5560.0 |
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Miransertib hydrochloride
CAS No. : 1313883-00-9
MCE 国际站：Miransertib hydrochloride
产品活性：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 Akt1，Akt2，Akt3 的 IC50 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)。
研究领域：PI3K/Akt/mTOR | Anti-infection
作用靶点：Akt | Parasite
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).
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]
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 t1/2 values of 17 h in rats versus 7 h in monkeys. The Cmax is 198 ng/mL and 258 ng/mL and the AUCinf was 5496 h•ng/mL and 2960 h•ng/mL in rats and monkeys, respectively.
Miransertib (ARQ-092; Compound 21a) inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma.
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