CAS NO: | 1313883-00-9 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | 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]. | |||||
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 | 468.98 | |||||
Formula | C27H25ClN6 | |||||
CAS 号 | 1313883-00-9 | |||||
运输条件 | Room temperature in continental US; may vary elsewhere. | |||||
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |