Phone: 1-617-401-8149
Fax: 1-617-606-5019
Email: message@sydlabs.com
Or leave a message with a formal purchase
order (PO) Or credit card.
Catalog No. | Product Name | Size | List Price (US$) | Quantity |
---|
Price/availability/specifications subject to change without notice. Unless otherwise indicated, our catalog and customized products are for research use only and not intended for human or animal diagnostic or therapeutic use.
Phone: 1-617-401-8149
Fax: 1-617-606-5019
Email: message@sydlabs.com
Or leave a message with a formal purchase
order (PO) Or credit card.
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.
APIM050013: AZD3458
CAS No.: 2132961-46-5.
Molecular Formula: C20H23N3O4S2.
Molecular Weight: 433.5l.
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.
Copyright © 2009-2022 sydlabs.com. All rights reserved.
Use of this website means that you have read, understood, and accepted the Syd Labs Privacy Policy and Terms & Conditions.