Miransertib (ARQ-092) is a potent, orally active, selective and allostericAktinhibitor withIC₅₀s of 2.7 nM, 14 nM and 8.1 nM forAkt1,Akt2,Akt3, respectively. Miransertib is also a potent theAKT1-E17K mutant proteininhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research^[1]. Miransertib 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].

432.52

Solid

C₂₇H₂₄N₆

1313881-70-7

Room temperature in continental US; may vary elsewhere.

DMSO : 12.5 mg/mL(28.90 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 1.25 mg/mL (2.89 mM); Clear solution

  此方案可获得 ≥ 1.25 mg/mL (2.89 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液