Information Onatasertib (CC 223) Onatasertib (CC 223) is a potent, selective, and orally bioavailable mTOR inhibitor with IC50 of 16 nM, >200-fold selectivity over the related PI3K-α. Phase 1/2. Targets mTOR (Cell-free assay); cFMS (Cell-free assay); FLT4 (Cell-free assay); DNA-PK (Cell-free assay) 16 nM; 28 nM; 651 nM; 840 nM In vitro In a panel of cell lines, CC-223 inhibits both mTORC1 (S6RP and 4EBP1) and mTORC2 [AKT(S473)] markers with IC50 ranges of 27 to 184 nM for pS6RP, 120 to 1,050 nM for p4EBP1 and 11 to 150 nM for pAKT(S473), respectively. CC-223 also inhibits cell growth and induces apoptosis across a number of cancer cell lines. In vivo In PC-3 tumor-bearing mice, CC-223 (25 mg/kg, p.o.) inhibits both mTORC1 and mTORC2. CC-223 (25 mg/kg, p.o.) also results in tumor growth inhibition by 47% to 95% in xenograft models of prostate, glioma, breast, lung, and colon. Cell Research(from reference) Cell lines：PC-3, CAL-51, A549,T47D,NCI-H460, HepG2, AU565, Hep3B, HCC, U87MG, HCT116, MDA-MB-231, and NCI-H23 cells Concentrations：~ 10 μM Incubation Time：72 h
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Onatasertib (CC 223)
CAS number：1228013-30-6 molecular formula：C21H27N5O3
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| Chinese alias | - | ||
| English alias | AKOS030526335 | Pyrazino(2,3-b)pyrazin-2(1H)-one, 3,4-dihydro-7-(6-(1-hydroxy-1-methylethyl)-3-pyridinyl)-1-(trans-4-methoxycyclohexyl)- | 3-[6-(2-hydroxypropan-2-yl)pyridin-3-yl]-5-(4-methoxycyclohexyl)-7,8-dihydropyrazino[2,3-b]pyrazin-6-one | CHEBI:169 | ||
| CAS number | 1228013-30-6 | molecular formula | C21H27N5O3 |
| molecular weight | 397.47 g/mol | Exact mass | - |
| PSA | 100.000 Ų | logp | 1.66 |
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