Description
GDC-0941 dimethanesulfonate is an orally bioavailable and selective inhibitor of class I PI3K with IC50 values of 15 nM, 185 nM, 7 nM and 224 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.
Product Overview
GDC-0941 is a novel selective class I phosphatidylinositol-3-kinase (PI3K) inhibitor. Activation of PI3K/Akt signaling pathway is frequently associated with tumorigenesis. Deregulation of this pathway occurs frequently with a variety of cancers and may contribute to the resistance to many anticancer agents. Developing novel small molecules that specifically block the PI3K/Akt pathway may inhibit tumor growth. GDC-0941 is designed to bind the ATP-binding pocket of PI3K and to prevent formation of phosphatidylinositol-3, 4, 5-triphosphate (PIP3), a second messenger that transmits PI3K downstream signals. It binds to PI3K in an ATP-competitive manner. GDC-0941 is a potent small-molecule thieno [3, 2-d] pyrimidine inhibitor of the class I PI3K. It is highly selective against isoforms p110(and p110(with IC50 of 3 nM, and moderately selective against isoforms p110(and p110(with IC50s of 33 nM and 75 nM, respectively. GDC-0941 inhibits cell proliferation in vitro and in vivo. It causes growth inhibition in a variety of cancer cell lines, including A2780, MDA-MB-361, PC3, and U87MG. It also inhibits the growth of trastuzumab-sensitive and -resistant HER2-amplied cancer cells which harbor p110(mutations or PTEN loss. GDC-0941 also reduces tumor volume in different xenograft models. GDC-0941 can be taken orally.
Synonyms
GDC-0941 (2 MeSO3H salt); GDC0941 dimethanesulfonate; GDC-0941; GDC0941; GDC 0941
Targets
PI3Kα; PI3Kβ; PI3Kδ; PI3Kγ
IC50
15 nM; 185 nM; 7 nM; 224 nM
Molecular Formula
C25H35N7O9S4
Chemical Name
4-[2-(1H-indazol-4-yl)-6-[(4-methylsulfonylpiperazin-1-yl)methyl]thieno[3,2-d]pyrimidin-4-yl]morpholine; methanesulfonic acid
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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