GDC-0941 (Pictilisib)

• CAT Number: I006942
• CAS Number: 957054-30-7 (free base); 957054-33-0 (mesylate).
• Molecular Formula: C23H27N7O3S2
• Molecular Weight: 513.63
• Purity: ≥95%
• Synonyms: 4-(2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine
• Target: PI3K inhibitor
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4°C for short term or -20 °C for long term
• SMILES: O=S(N1CCN(CC2=CC3=NC(C4=CC=CC5=C4C=NN5)=NC(N6CCOCC6)=C3S2)CC1)(C)=O

Pictilisib, also known as Pictrelisib, GDC-0941, RG7321 and GNE0941 , is an orally bioavailable, and is a potent small-molecule thieno[3,2-d]pyrimidine inhibitor of the class I phosphatidylinositol 3 kinase (PI3K) isoforms p100alpha and p100delta with potential antineoplastic activity. PI3K inhibitor GDC-0941 selectively binds to PI3K isoforms in an ATP-competitive manner, inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway; inhibition of tumor cell growth, motility and survival in susceptible tumor cell populations may result.

Reference

1:Ehrhardt M, Craveiro RB, Holst MI, Pietsch T, Dilloo D. The PI3K inhibitor GDC-0941 displays promising in vitro and in vivo efficacy for targeted medulloblastoma therapy. Oncotarget. 2015 Jan 20;6(2):802-13. PubMed PMID: 25596739.