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Miransertib

CAS No. : 1313881-70-7

MCE 站：Miransertib

产品活性：Miransertib (ARQ-092) 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 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 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 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.
Miransertib (ARQ-092; Compound 21a) inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma.

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