Miransertib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Miransertib (ARQ-092) 是一种有效的、选择性的 Akt1/2/3 变构抑制剂，IC50 分别为 5/4.5/16 nM。

Miransertib (ARQ-092) is a potent, selective and allosteric inhibitor of Akt1/2/3 with IC50 of 5/4.5/16 nM respectively; inhibits cellular AKT activation and the phosphorylation of the downstream target PRAS40; inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma; orally bioavailable.Blood Cancer Phase 1 Clinical(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(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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ARQ-092

PI3K/Akt/mTOR signaling

Akt

Akt

Cancer

Blood cancer

1313881-70-7

432.5197

C27H24N6

>98% (HPLC)

DMSO: ≥ 40.2 mg/mL

C1CC(C1)(C2=CC=C(C=C2)N3C4=C(C=CC(=N4)C5=CC=CC=C5)N=C3C6=C(N=CC=C6)N)N

2-Pyridinamine, 3-[3-[4-(1-aminocyclobutyl)phenyl]-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl]-

(-20℃)

With Ice Pack

≥ 2 years