GDC-0941 dimethanesulfonate
957054-33-0
0.98%
2026-06-24
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Product Description
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Seller Information
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Description
ProductName 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 category Inhibitors(c1514) cas_num 957054-33-0 Basic Info-
Product Name:
Thieno[3,2-d]pyrimidine, 2-(1H-indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-, methanesulfonate (1:2)
Other Name:Thieno[3,2-d]pyrimidine,2-(1H-indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-,methanesulfonate (1:2)
CAS No.:957054-33-0
Molecular Formula:C23H27N7O3S2.2CH4O3S
InChIKeys:InChIKey=OZRVQTBMLHRDIR-UHFFFAOYSA-N
Molecular Weight:608.7333
Exact Mass:705.138
UNII:G3D7HF2GS9
NCI Thesaurus Code:C82380
Categories:
Characteristics-
PSA:
270
XLogP3:4.33960
Melting Point:>280°C (dec.)
Storage Conditions:Refrigerator
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Seller Information
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Business Type:
Manufactory
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Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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