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GSK 2636771 dihydrochloride
- Parent CAS: 1372540-25-4
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C22H22F3N3O3.2HCl
- MW: 506.35
Description
GSK 2636771 dihydrochloride is a potent, orally available and specific PI3K p110β inhibitor used to block PI3Kβ-dependent phosphoinositide signaling.
PI3Kβ can drive AKT pathway activation and tumor-cell survival in PTEN-deficient settings. GSK 2636771 is useful for interrogating PI3Kβ isoform dependence and pathway inhibition in oncology models.
Key Features
- Specific PI3K p110β inhibitor
- Orally available PI3K isoform-selective compound
- Targets PI3Kβ-dependent AKT signaling
- Relevant to PTEN-deficient cancer research
Applications
- PI3Kβ/PIK3CB pharmacology
- PTEN-deficient tumor model studies
- AKT phosphorylation and pathway assays
- PI3K isoform selectivity profiling
More Information
| Parent CAS No. | 1372540-25-4 |
|---|---|
| Chemical Name | 2-methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic acid dihydrochloride |
| SMILES | C1(C)N(CC2=CC=CC(C(F)(F)F)=C2C)C2=CC(N3CCOCC3)=CC(C(O)=O)=C2N=1.Cl.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C22H22F3N3O3.2ClH/c1-13-15(4-3-5-18(13)22(23,24)25)12-28-14(2)26-20-17(21(29)30)10-16(11-19(20)28)27-6-8-31-9-7-27;;/h3-5,10-11H,6-9,12H2,1-2H3,(H,29,30);2*1H |
| InChiKey | VDEKRYFLVUQCDF-UHFFFAOYSA-N |
| CID | 91826489 |
| Short Description | PI3K p110β inhibitor |
References
- RA Rivero, MA Hardwick. Identification of GSK2636771, a potent and selective, orally bioavailable inhibitor of phosphatidylinositol 3-kinase-beta (PI3Kβ) for the treatment of PTEN deficient tumors. Cancer Res. 2012, 72(8 Supplement), 2913.
- RM Sanchez et al. Synthesis and structure–activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent β isoform selective phosphatidylinositol 3-kinase inhibitors. Bioorg. Med. Chem. Lett. 2012, 22(9), 3198-3202.
- H Lin. Isoform Selective PI3K-beta Inhibitors. Chin. J. Chem. 2013, 31(3), 299-303.
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