A potent inhibitor of class I PI3K isoforms (IC50 values of 5

GDC-0980 – 10 mg

Brand:
Cayman
CAS:
1032754-93-0
Storage:
-20
UN-No:
Non-Hazardous - /

GDC-0980 is a potent inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms, with IC50 values of 5, 27, 7, and 14 nM for PI3Kα, β, δ, and γ, respectively, in cell-free assays.{29877,29878} It also inhibits mTOR (Ki = 17 nM) but is inactive against a large panel of additional kinases.{29877,29878} GDC-0980 induces cell cycle arrest or apoptosis in a range of cancer cell lines.{29878} It is effective in vivo, suppressing the growth of a number of tumor xenografts in mice and enhancing the antitumor activity of docetaxel (Item No. 11637) in mice.{29878}  

 

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Description

A potent inhibitor of class I PI3K isoforms (IC50 values of 5, 27, 7, and 14 nM for PI3Kα, β, δ, and γ, respectively) and mTOR (Ki = 17 nM); induces cell cycle arrest or apoptosis in a range of cancer cell lines; effective in vivo, suppressing the growth of a number of tumor xenografts in mice

Formal name: (2S)-1-[4-[[2-(2-amino-5-pyrimidinyl)-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-2-hydroxy-1-propanone

Synonyms:  Apitolisib|RG7422

Molecular weight: 498.6

CAS: 1032754-93-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|mTOR||Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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