AZD6482 - CAS 1173900-33-8
Catalog number: 1173900-33-8
Category: Inhibitor
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AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ. Phase 1.
KIN193; AZD6482; KIN 193; AZD 6482; KIN-193; AZD-6482
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1.Potent phosphatidylinositol 3-kinase inhibitors and their biology.
Joshi MC;Kumar K;Kumar V Curr Drug Discov Technol. 2014 Jun;11(2):113-26.
The Phosphoinositide 3-kinase (PI3k) is an important regulator of intracellular signalling pathways, like cell proliferation, migration, survival, and angiogenesis upon activation by growth factor or receptors. The PI3k's pathway is frequently up-regulated in human cancers, thus inhibition of PI3k's is a promising approach for cancer therapy. Many potent PI3k's inhibitors have been reported so far and few of them are in clinical trial like GDC-0941, BGT-226, AZD-6482 and others are natural products etc.
2.High selectivity of PI3Kβ inhibitors in SETD2-mutated renal clear cell carcinoma.
Wang J;Wen J;Yi R;Liu F;Zhou J;Liu G;Li Q;Yang Z;Su X J BUON. 2015 Sep-Oct;20(5):1267-75.
PURPOSE: ;Clear cell renal cell carcinoma (ccRCC) is characterized with frequent mutations of SETD2 gene and our purpose was to explore targeted therapy for this entity.;METHODS: ;By bioinformatic investigation of two major databases, the Genomics of Drug Sensitivity in Cancer (GDSC) database and The Cancer Genome Atlas (TCGA) database, we identified the selective PI3Kβ inhibitors TGX221 and AZD6482 as selective inhibitors for ccRCC with SETD2 mutations, with AZD6482 additionally targeting PIK3CA and CDK6 mutations.;RESULTS: ;Further investigation on AZD6482 profile revealed that mutations in RB1, KRAS, NRAS and APC contributed in drug resistance. Changes in both AZD6482-sensitive and -resistant gene sets showed limited impact on prognosis. Western blotting showed AZD6482 did not induce changes in a panel of major downstream effectors of AKT, but substantially increased PMS2 level. AZD6482 also selectively inhibited migration, invasiveness, and colony formation of ccRCC cells with SETD2 mutations. Integrative network analysis revealed complex interactions between these genes except SETD2.;CONCLUSION: ;AZD6482 is a novel inhibitor with high selectivity for ccRCC SETD2 mutations. Increased activity of PI3K/AKT/PMS2 could play a role in SETD2 mutated ccRCC.
3.Addition of the p110α inhibitor BYL719 overcomes targeted therapy resistance in cells from Her2-positive-PTEN-loss breast cancer.
Zhang C;Xu B;Liu P Tumour Biol. 2016 Nov;37(11):14831-14839. Epub 2016 Sep 17.
Breast cancer is one of the leading causes of death for women worldwide. Among various subtypes of breast cancer, human epidermal growth factor receptor 2 (HER2)-positive and phosphatase and tensin homolog (PTEN) loss breast cancer is a cause of great concern in terms of its resistance to HER2-targeted therapies and its poor prognosis. Phosphatidylinositol 3-kinase (PI3K)/AKT hyperphosphorylation is considered one of key mechanisms leading to this resistance, thus combination therapy of PI3K inhibitors and HER2 antibodies is promising for overcoming this problem, and more specific regimens should be designed in this age of precision medicine. In this study, we established an HER2-positive and PTEN loss cell line and confirmed it by western blot analysis. This cell line and its orthotopic xenograft models were exposed to p110α-specific inhibitor BYL719, p110β-specific inhibitor AZD6482, or pan-PI3K inhibitor BKM120, respectively, and the results showed sensitivity to both BYL719 and BKM120 but not AZD6482, which indicated a p110α-reliance for HER2-positive-PTEN-loss breast cancer. Then, the addition of BYL719 to HER2 antibody greatly reduced tumor growth both in vitro and in vivo, accompanied by inhibited PI3K effector phosphorylation.
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CAS 1173900-33-8 AZD6482

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