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GDC 0941 bismesylate
- Pictilisib
- Parent CAS: 957054-30-7
- Soluble in water and DMSO
- MF: C23H27N7O3S2.2CH4O3S
- MW: 705.85
Description
GDC 0941 bismesylate (Pictilicib) is a potent, orally bioavailable class I PI3K inhibitor that inhibits p110α and p110δ most strongly, with additional activity at p110β and p110γ.
Pictilisib suppresses PI3K-dependent AKT signaling and cell-survival pathways while showing substantially weaker inhibition of DNA-PK and mTOR. The bismesylate form is useful for pharmacology, oncology and pathway studies requiring a soluble PI3K inhibitor.
Key Features
- Potent, orally bioavailable pan-class I PI3K inhibitor
- IC50: 3 nM (p110α), 3 nM (p110δ), 33 nM (p110β) and 75 nM (p110γ)
- Weaker activity against DNA-PK and mTOR (IC50: 1230 nM and 580 nM, respectively)
- Water-soluble salt form
Applications
- Class I PI3K isoform profiling
- PI3K–AKT pathway inhibition studies
- Cancer-cell growth and survival models
- Pharmacodynamic and combination-treatment research
More Information
| Parent CAS No. | 957054-30-7 |
|---|---|
| Chemical Name | 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine bismesylate |
| SMILES | CS(O)(=O)=O.N1=C(C2C3C=NNC=3C=CC=2)N=C(N2CCOCC2)C2SC(CN3CCN(S(C)(=O)=O)CC3)=CC1=2.CS(O)(=O)=O |
| MFCD | MFCD12546329 |
| InChi | InChI=1S/C23H27N7O3S2.2CH4O3S/c1-35(31,32)30-7-5-28(6-8-30)15-16-13-20-21(34-16)23(29-9-11-33-12-10-29)26-22(25-20)17-3-2-4-19-18(17)14-24-27-19;2*1-5(2,3)4/h2-4,13-14H,5-12,15H2,1H3,(H,24,27);2*1H3,(H,2,3,4) |
| InChiKey | RFRIKACSFOTIMU-UHFFFAOYSA-N |
| CID | 56972143 |
| Short Description | PI3K inhibitor |
References
- AJ Folkes et al. The identification of GDC-0941 as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer. J. Med. Chem. 2008, 51(18), 5522-5532.
- FI Raynaud et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. Mol. Cancer Ther. 2009, 8(7), 1725-1738.
- List of publications using GDC 0941 bismesylate (Axon 1377) purchased from Axon Medchem
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