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Chemical Structure : CCT128930
CAS No.: 885499-61-6
Catalog No.: PC-43440Not For Human Use, Lab Use Only.
CCT128930 is a potent, selective, ATP-competitive AKT inhibitor with IC50 of 6 nM (AKT2), 28-fold selectivity over the closely related PKA.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $118 | In stock | |
| 10 mg | $188 | In stock | |
| 25 mg | $328 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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CCT128930 is a potent, selective, ATP-competitive AKT inhibitor with IC50 of 6 nM (AKT2), 28-fold selectivity over the closely related PKA.
CCT128930 also exhibits 20-fold selectivity over p70S6K (IC50=120 nM).
CCT128930 shows growth inhibition for U87MG human glioblastoma cells (IC50=6.3 uM), for LNCaP human prostate cancer cells (IC50=0.35 uM), and for PC3 human prostate cancer cells (IC50=1.9 uM) consistent with AKT pathway blockade.
CCT128930 blocks the phosphorylation of several downstream AKT biomarkers in U87MG tumor xenografts, indicating AKT inhibition in vivo.
CCT128930 demonstrates antitumor activity in U87MG and HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts.
| M.Wt | 341.84 | |
| Formula | C18H20ClN5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-Piperidinamine, 4-[(4-chlorophenyl)methyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)- |
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1. Caldwell JJ, et al. J Med Chem. 2008 Apr 10;51(7):2147-57.
2. Yap TA, et al. Mol Cancer Ther. 2011 Feb;10(2):360-71.
3. Yap TA, et al. Clin Cancer Res. 2012 Jul 15;18(14):3912-23.
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