CAS NO: | 1313881-70-7 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | 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]. | ||||||||||||||||
IC50& Target[1][2] |
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体外研究 (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)[1]. | ||||||||||||||||
体内研究 (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 t1/2values of 17 h in rats versus 7 h in monkeys. The Cmaxis 198 ng/mL and 258 ng/mL and the AUCinfwas 5496 hong/mL and 2960 hong/mL in rats and monkeys, respectively[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 432.52 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C27H24N6 | ||||||||||||||||
CAS 号 | 1313881-70-7 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 12.5 mg/mL(28.90 mM;Need ultrasonic) 配制储备液
* 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。 In Vivo: 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
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