- Product Details
- Description
- Additional information
- More Offers
Description
Background Information:
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 selectivity 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).
Reference:
1. L. S. Carnevalli, et al, Novel selective PI3Kγ inhibitor AZD3458 promotes anti-tumor immune responses and reverts resistance to immunotherapy in checkpoint blockade refractory preclinical models, In: Proceedings of the American Association for Cancer Research Annual Meeting 2019; 2019 Mar 29-Apr 3; Atlanta, GA. Philadelphia (PA): AACR; Cancer Res 2019;79(13 Suppl):Abstract nr 100.
2. P. M. Gutierrez, et al, Mechanistic insights and dose optimization for AZD3458, a novel selective PI3Kg immuno-modulator, using a quantitative systems approach In: Proceedings of the American Association for Cancer Research Annual Meeting 2019; 2019 Mar 29-Apr 3; Atlanta, GA. Philadelphia (PA): AACR; Cancer Res 2019;79(13 Suppl):Abstract nr 104.
APIM050094: AZD3458 (AZD-3458)
CAS No.: 2132961-46-5.
Molecular Formula: C20H23N3O4S2.
Molecular Weight: 433.5.
Purity: >99.5 Pure by Achiral and Chiral HPLCs.
QC: Achiral and Chiral HPLCs, MS, 1H-NMR, and Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
Additional information
| Ship from Country | USA |
|---|---|
| Size | 10 mg, 100 mg, 5 mg, 50 mg |
