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Chemical Structure : AZD5363
CAS No.: 1143532-39-1
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $228 | In stock | |
| 50 mg | $388 | In stock | |
| 100 mg | $528 | In stock | |
| 500 mg | $998 | In stock | |
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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.
| M.Wt | 428.921 | |
| Formula | C21H25ClN6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-4-amino-N-[1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide |
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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.
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