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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. PI3Kalpha, beta, and delta are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kgamma is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit. AZD 6482 is a PI3K inhibitor that targets the beta isoform more potently than PI3Kdelta, PI3Kgamma, or PI3Kalpha (IC50s = 0.69, 13.6, 47.8, and 136 nM, respectively). It displays 80-fold selectivity for PI3Kbeta over PI3k-C2 and DNA-PK and more than 1,000-fold over other PI3K-related kinases. AZD 6482 blocks Akt signaling and tumor growth in a large number of cancer cell lines, including those that are dependent on PI3Kbeta activation or PTEN loss. AZD 6482 (20 mg/kg, i.p.) suppresses the growth of PTEN-deficient xenograft tumors in mice. It also produces an anti-thrombotic effect in dogs without an increase in bleeding time or blood loss.Formal Name: 2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]-benzoic acid. CAS Number: 1173900-33-8. Synonyms: KIN-193. Molecular Formula: C22H24N4O4. Formula Weight: 408.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 5 mg/ml. lambdamax: 218, 268, 342 nm. SMILES: O=C1N2C(C([C@@H](C)NC3=C(C(O)=O)C=CC=C3)=CC(C)=C2)=NC(N4CCOCC4)=C1. InChi Code: InChI=1S/C22H24N4O4/c1-14-11-17(15(2)23-18-6-4-3-5-16(18)22(28)29)21-24-19(12-20(27)26(21)13-14)25-7-9-30-10-8-25/h3-6,11-13,15,23H,7-10H2,1-2H3,(H,28,29)/t15-/m1/s1. InChi Key: IRTDIKMSKMREGO-OAHLLOKOSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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