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GSK 2110183 hydrochloride
- Afuresertib hydrochloride
- Parent CAS: 1047644-62-1
- Optical Purity: Optically pure
- Soluble in water and DMSO
- MF: C18H17Cl2FN4OS.HCl
- MW: 463.78
Description
GSK 2110183 hydrochloride (Afuresertib) is a potent, reversible and orally bioavailable inhibitor of AKT kinases. It inhibits AKT1, AKT2 and AKT3 and suppresses PI3K/AKT pathway signaling in cancer-cell models.
AKT regulates survival, metabolism, proliferation and therapy resistance downstream of PI3K. GSK 2110183 hydrochloride is useful for studying AKT dependency, pathway inhibition and combination strategies in oncology and metabolic signaling research.
Key Features
- Potent pan-AKT kinase inhibitor
- Reported Ki values: 0.08 nM for AKT1, 2 nM for AKT2 and 2.6 nM for AKT3
- Reversible and orally bioavailable pharmacology
- Preferentially inhibits proliferation in AKT-dependent tumor models
Applications
- PI3K/AKT pathway research
- Cancer cell survival and proliferation studies
- Kinase inhibitor combination assays
- Phospho-AKT signaling analysis
More Information
| Parent CAS No. | 1047644-62-1 |
|---|---|
| Chemical Name | N-((S)-1-amino-3-(3-fluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide hydrochloride |
| SMILES | C1(C(N[C@@H](CC2=CC=CC(F)=C2)CN)=O)SC(Cl)=C(C2N(C)N=CC=2Cl)C=1.Cl |&1:3,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C18H17Cl2FN4OS.ClH/c1-25-16(14(19)9-23-25)13-7-15(27-17(13)20)18(26)24-12(8-22)6-10-3-2-4-11(21)5-10;/h2-5,7,9,12H,6,8,22H2,1H3,(H,24,26);1H/t12-;/m0./s1 |
| InChiKey | YFQJOPFTGMHYNV-YDALLXLXSA-N |
| CID | 46843056 |
| Short Description | Akt inhibitor |
References
- M. Dumble et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One. 2014 Jun 30;9(6):e100880.
- A. Spencer et al. The novel AKT inhibitor afuresertib shows favorable safety, pharmacokinetics, and clinical activity in multiple myeloma. Blood. 2014 Oct 2;124(14):2190-5.
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