A potent inhibitor of PI3K isoforms α

GDC-0032 – 1 mg

Brand:
Cayman
CAS:
1282512-48-4
Storage:
-20
UN-No:
Non-Hazardous - /

GDC-0032 is a potent inhibitor of phosphatidylinositol 3-kinase (PI3K) isoforms α, δ, and γ (IC50s = 0.28, 0.12, and 0.97 nM, respectively) that is 31 times less potent at PI3Kβ.{31881} It is over 1,000-fold selective for p100α over other PI3K-like kinases, including DNA-dependent protein kinase catalytic subunits, ATM, and ATR. GDC-0032 has increased potency in cancer cell lines harboring PIK3CA-activating alterations, and is effective in vivo, suppressing the growth of tumors in a mouse xenograft model at low drug dose levels.{31880,31881,31882}  

 

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Description

A potent inhibitor of PI3K isoforms α, δ, and γ (IC50s = 0.28, 0.12, and 0.97 nM, respectively) that is 31 times less potent at PI3Kβ; has increased potency in cancer cell lines harboring PIK3CA-activating alterations, and is effective in vivo

Formal name: 4-[5,6-dihydro-2-[3-methyl-1-(1-methylethyl)-1H-1,2,4-triazol-5-yl]imidazo[1,2-d][1,4]benzoxazepin-9-yl]-α,α-dimethyl-1H-pyrazole-1-acetamide

Synonyms:  ​Taselisib

Molecular weight: 460.5

CAS: 1282512-48-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Lipid Biochemistry|Glycerophospholipids|Phosphatidyl Inositol Kinases & Phosphatases

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