AZD-5363

SKU: orb1226921

描述

AZD5363, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms (IC50 30 μM).(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.

图片与验证

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关键属性

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CAS 号	1143532-39-1
MW	428.92
纯度	>98% (HPLC)
分子式	C₂₁H₂₅ClN₆O₂
SMILES	O=C(C1(N)CCN(C2=C3C(NC=C3)=NC=N2)CC1)N[C@H](C4=CC=C(Cl)C=C4)CCO
靶点	Akt
溶解性	DMSO: 86 mg/mL (200.5 mM)

生物活性

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体内

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.

体外

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 IC50 value 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 ser473 and thr308. In BT474c cells, Capivasertib induces FOXO3a nuclear translocation with EC50 value of 0.69 μM; a concentration of 3 μM is sufficient to almost completely localize FOXO3a to the nucleus.

储存与操作

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储存	Storage temperature: -20°C. Stability: ≥ 2 years
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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AZD5363 | AZD-5363 | AZD 5363 | Capivasertib

相似产品

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Capivasertib [orb1307109]
纯度：
99.68% (May vary between batches)
CAS 号：
1143532-39-1
MW:
428.92
分子式：
C₂₁H₂₅ClN₆O₂
可选规格： 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 1 ml x 10 mM (in DMSO), 200 mg

质量保证

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常用数据库链接

基因符号

Akt

实验方案信息

查看更多实验方案

纯度：	99.68% (May vary between batches)
CAS 号：	1143532-39-1
MW:	428.92
分子式：	C₂₁H₂₅ClN₆O₂