Capivasertib (AZD5363) | pan-AKT inhibitor | Probechem Biochemicals

Chemical Structure : AZD5363

CAS No.: 1143532-39-1

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AZD5363 (Capivasertib, AZD-5363)

货号: PC-49529Not For Human Use, Lab Use Only.

Capivasertib (AZD5363) is a potent, selective and orally bioavailable inhibitor of pan-Akt kinases with IC50 of <10 nM.

规格	价格	库存
10 mg	￥980	In stock
25 mg	￥1580	In stock
50 mg	￥2580	In stock
100 mg	￥3980	In stock
250 mg		Get quote
1 g		Get quote

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生物&药学活性

Capivasertib (AZD5363) is a potent, selective and orally bioavailable inhibitor of pan-Akt kinases with IC50 of <10 nM.
AZD5363 exhibits similar potency against P70S6K and PKA (IC50=6 and 7 nM) but a lower potency against the Rho kinases ROCK1 and ROCK2.
AZD5363 inhibited phosphorylation of AKT substrates in cells with a potency of 0.3-0.8 uM.
AZD5363 inhibited the proliferation of 41 of 182 solid and hematologic tumor cell lines with IC50 of <3 uM.
Oral dosing of AZD5363 (100 and 200mg/kg twice daily) reduces PRAS40, GSK3β, and S6 phosphorylation in BT474c xenografts (PRAS40 phosphorylation EC(50)=0.1 μmol/L total plasma exposure), reversible increases in blood glucose concentrations, and dose-dependent decreases in 2[18F]fluoro-2-deoxy-D-glucose ((18)F-FDG) uptake in U87-MG xenografts.
Chronic oral dosing of AZD5363 caused dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2(+) breast cancer models that are resistant to trastuzumab.
AZD5363 also significantly enhanced the antitumor activity of docetaxel, lapatinib, and trastuzumab in breast cancer xenografts.

物理化学性质&存储条件

分子量	428.921
分子式	C21H25ClN6O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-4-amino-N-[1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide

参考文献

1. Addie M, et al. J Med Chem. 2013 Mar 14;56(5):2059-73.

2. Lamoureux F, et al. Clin Cancer Res. 2013 Feb 15;19(4):833-44.

3. Davies BR, et al. Mol Cancer Ther. 2012 Apr;11(4):873-87.

AZD5363 (Capivasertib, AZD-5363)

生物&药学活性

物理化学性质&存储条件

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AZD5363 (Capivasertib, AZD-5363)

生物&药学活性

物理化学性质&存储条件

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