Products
Online Inquiry
Our Products Cannot Be Used As Medicines Directly For Personal Use.
Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.
GDC-0941 dimethanesulfonate
Cat No.
CEI-1345
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.
CAS No.
957054-33-0
Molecular Weight
705.85
Purity
0.98
Storage
Store at -20°C
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
Download
Download Datasheet