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AZD3458 (AZD-3458)
AZD3458 is an orally bioavailable potent and selective PI3Kγ inhibitor, and an immuno-oncology modulator. It selectively inhibits PI3Kγ with a cellular IC50 of 8 nM, a 100-fold selective over PI3Kδ (ref. 1). in vitro, AZD3458 inhibits pAKTS308/S473 in human macrophages and mouse CD11b activation at 32nM and 30nM free IC50 respectively (ref. 1). Application of AZD3458 in vivo with checkpoint inhibitors α-PD-1 or α-PD-L1 had greater anti-tumor effects than checkpoint inhibitor alone in 4T1, LLC, CT-26 and MC-38 mouse syngeneic models (ref. 2), suggesting that AZD3458 can reverse myeloid suppressive tumor microenvironment and revert tumor resistance to immunotherapy in myeloid-enriched immunosuppressive tumor types (ref. 2).
Catalog NO: CT-A3458
Synonym: AZD-3458
CAS NO: 2132961-46-5
Mol. Formula: C20H23N3O4S2
MW: 433.5
** in vivo Quality Material, 99.9-100% by Achiral and Chiral HPLCs. Anhydrous, validated by a spot-on Quantitative Elemental Analysis. Clean & Impeccable. Bulk Stock!! Prompt.