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].

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]

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_1/2values of 17 h in rats versus 7 h in monkeys. The C_maxis 198 ng/mL and 258 ng/mL and the AUC_infwas 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].

468.98

C₂₇H₂₅ClN₆

1313883-00-9

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.