CAS NO: | 1143532-39-1 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Capivasertib (AZD5363) is an orally active and potentpan-AKTkinase inhibitor withIC50of 3, 7 and 7 nM forAkt1,Akt2andAkt3, respectively. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | Capivasertib, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms with a potency of 10 nM or less. Capivasertib inhibits phosphorylation of these substrates with an IC50value of 0.06 to 0.76 μM in the 3 cell lines. Capivasertib effectively inhibits phosphorylation of S6 and 4E-BP1 in these cell lines, whereas it increases phosphorylation of AKT at both ser473and thr308. In BT474c cells, Capivasertib induces FOXO3a nuclear translocation with EC50value of 0.69 μM; a concentration of 3 μM is sufficient to almost completely localize FOXO3a to the nucleus. AZD5363Capivasertibhibitor MK-2206 is much less active (IC50>30 μM)[1]. | ||||||||||||||||
体内研究 (In Vivo) | Oral dosing of Capivasertib (AZD5363) to nude mice causes dose- and time-dependent reduction of PRAS40, GSK3β, and S6 phosphorylation in BT474c xenografts (PRAS40 phosphorylation EC50~0.1 μM total plasma exposure), reversible increases in blood glucose concentrations, and dose-dependent decreases in 2[18F]fluoro-2-deoxy-D-glucose (18F-FDG) uptake in U87-MG xenografts. Chronic oral dosing of Capivasertib caused dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2+breast cancer models. Capivasertib also significantly enhances the antitumor activity of RP-56976 and GW572016 in breast cancer xenografts[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 428.92 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C21H25ClN6O2 | ||||||||||||||||
CAS 号 | 1143532-39-1 | ||||||||||||||||
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 : 125 mg/mL(291.43 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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