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Chemical Structure : Taselisib
CAS No.: 1282512-48-4
Catalog No.: PC-22488Not For Human Use, Lab Use Only.
Taselisib (GDC-0032) is a potent, selective inhibitor of PIK3CA (PI3Kα) with Ki of 0.29 nM and pAkt IC50 of 4 nM, 31-fold selective over PI3Kβ.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $98 | In stock | |
| 25 mg | $158 | In stock | |
| 50 mg | $258 | In stock | |
| 100 mg | Get quote |
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Taselisib (GDC-0032) is a potent, selective inhibitor of PIK3CA (PI3Kα) with Ki of 0.29 nM and pAkt IC50 of 4 nM, 31-fold selective over PI3Kβ.
Taselisib (GDC-0032) maintains biochemical selectivity over the non-class I PI3Ks, with IC50 values for PI3K-C2 beta and hVPS34 measuring 292 and 374 nM, respectively.
Taselisib (GDC-0032) achieves a 1000-fold selectivity against a panel of potential off-targets.
Taselisib (GDC-0032) potently inhibits cell proliferation of MCF7-neo/HER2 cells with IC50 of 25 nM.
Taselisib (GDC-0032) (2.8 mg/kg) resulted in a similar decrease in Akt phosphorylation (59%).
Taselisib (GDC-0032) orally at 1.4, 2.8, 5.8, 11.25, or 22.5 mg/kg resulted in dose-dependent increase in TGI (19%, 76%, 95%, 103%, and 123%, respectively) and tumor regressions in the MCF7-neo/Her2 xenograft model grown in nude mice.
| M.Wt | 460.54 | |
| Formula | C24H28N8O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-(4-(2-(1-Isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide |
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1. Zumsteg ZS, et al. Clin Cancer Res. 2016 Apr 15;22(8):2009-19.
2. Ndubaku CO, et al. J Med Chem. 2013 Jun 13;56(11):4597-610.
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