A selective PI3K inhibitor that targets the β isoform more potently than PI3Kδ

AZD6482 – 1 mg

Brand:
Cayman
CAS:
1173900-33-8
Storage:
-20
UN-No:
Non-Hazardous - /

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3′ hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit.{14518} AZD6482 is a PI3K inhibitor that targets the β isoform more potently than PI3Kδ, PI3Kγ, or PI3Kα (IC50s = 0.69, 13.6, 47.8, and 136 nM, respectively).{29907} It displays 80-fold selectivity for PI3Kβ over PI3k-C2 and DNA-PK and more than 1,000-fold over other PI3K-related kinases.{29907} AZD6482 blocks Akt signaling and tumor growth in a large number of cancer cell lines, including those that are dependent on PI3Kβ activation or PTEN loss.{29907,29910,29908} AZD6482 (20 mg/kg, i.p.) suppresses the growth of PTEN-deficient xenograft tumors in mice.{29907} It also produces an anti-thrombotic effect in dogs without an increase in bleeding time or blood loss.{29909}  

 

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Description

A selective PI3K inhibitor that targets the β isoform more potently than PI3Kδ, PI3Kγ, or PI3Kα (IC50s = 0.69, 13.6, 47.8, and 136 nM, respectively); blocks Akt signaling and tumor growth in a large number of cancer cell lines and suppresses the growth of PTEN-deficient xenograft tumors in mice

Formal name: 2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]-benzoic acid

Synonyms:  KIN-193

Molecular weight: 408.5

CAS: 1173900-33-8

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|Cardiovascular System|Blood|Thrombosis

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