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AZD1208
Axon 2795
CAS:
1204144-28-4
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C21H21N3O2S
- MW: 379.48
Description
AZD1208 is a highly potent, selective and orally available Pim kinase inhibitor with IC50 values of 0.4 nM, 5.0 nM and 1.9 nM for Pim-1, Pim-2 and Pim-3, respectively. By blocking all three PIM kinase isoforms, AZD1208 suppresses downstream survival and translation pathways (such as mTORC1, p70S6K, and 4EBP1). AZD1208 induces the cell cycle arrest in the G1 phase and triggers a dose-dependent apoptosis (programmed cell death) across various AML cell lines, independent of their FLT3 mutation status.
More Information
| Parent CAS No. | 1204144-28-4 |
|---|---|
| Chemical Name | (R,Z)-5-((2-(3-Aminopiperidin-1-yl)biphenyl-3-yl)methylene)thiazolidine-2,4-dione |
| SMILES | C1C(/C=C2SC(=O)NC2=O)=C(N2CCC[C@@H](N)C2)C(C2C=CC=CC=2)=CC=1 |&1:15,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C21H21N3O2S/c22-16-9-5-11-24(13-16)19-15(12-18-20(25)23-21(26)27-18)8-4-10-17(19)14-6-2-1-3-7-14/h1-4,6-8,10,12,16H,5,9,11,13,22H2,(H,23,25,26)/b18-12-/t16-/m1/s1 |
| InChiKey | MCUJKPPARUPFJM-UWCCDQBKSA-N |
| CID | 58423153 |
| Short Description | PIM inhibitor |
References
- LA Dakin et al. Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4599-604.
- LS Chen et al. Protein profiling identifies mTOR pathway modulation and cytostatic effects of Pim kinase inhibitor, AZD1208, in acute myeloid leukemia. Leuk Lymphoma. 2016 Dec;57(12):2863-2873.
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