AZD3458
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C20H23N3O4S2
- MW: 433.54
Description
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 in vitro, AZD3458 inhibits pAKTS308/S473 in human macrophages and mouse CD11b activation at 32nM and 30nM free IC50 respectively. 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, suggesting that AZD3458 can reverse myeloid suppressive tumor microenvironment and revert tumor resistance to immunotherapy in myeloid-enriched immunosuppressive tumor types.
More Information
| Parent CAS No. | 2132961-46-5 |
|---|---|
| Chemical Name | (S)-N-(5-(2-(1-cyclopropylethyl)-7-(methylsulfonyl)-1-oxoisoindolin-5-yl)-4-methylthiazol-2-yl)acetamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1C(S(C)(=O)=O)=C2C(=O)N([C@@H](C)C3CC3)CC2=CC=1C1=C(C)N=C(NC(=O)C)S1 |&1:10,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C20H23N3O4S2/c1-10-18(28-20(21-10)22-12(3)24)14-7-15-9-23(11(2)13-5-6-13)19(25)17(15)16(8-14)29(4,26)27/h7-8,11,13H,5-6,9H2,1-4H3,(H,21,22,24)/t11-/m0/s1 |
| InChiKey | PAQUFWFUOVDUIO-NSHDSACASA-N |
| CID | 134611894 |
| Short Description | PI3Kγ inhibitor |
References
- LS Carnevalli et al. Novel selective PI3Kγ inhibitor AZD3458 promotes anti-tumor immune responses and reverts resistance to immunotherapy in checkpoint blockade refractory preclinical models. Cancer Res (2019) 79 (13_Supplement): 100.
- PM Gutierrez et al. Mechanistic insights and dose optimization for AZD3458, a novel selective PI3Kg immuno-modulator, using a quantitative systems approach. Cancer Res (2019) 79 (13_Supplement): 104.
- K Hudson et al. Intermittent High-Dose Scheduling of AZD8835, a Novel Selective Inhibitor of PI3Kα and PI3Kδ, Demonstrates Treatment Strategies for PIK3CA-Dependent Breast Cancers. Mol Cancer Ther. 2016 May;15(5):877-89.
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