AZD1208

• CAT Number: I000752
• CAS Number: 1204144-28-4
• Molecular Formula: C₂₁H₂₁N₃O₂S
• Molecular Weight: 379.48
• Purity: ≥95%
• Synonyms: (5E)-5-[[2-[(3R)-3-aminopiperidin-1-yl]-3-phenylphenyl]methylidene]-1,3-thiazolidine-2,4-dione
• Target: Pim
• Solubility: DMSO: ≥ 28.5 mg/mL
• Storage: Store at -20°C
• IC50: < 5 nM
• IUPAC Name: (5Z)-5-[[2-[(3R)-3-aminopiperidin-1-yl]-3-phenylphenyl]methylidene]-1,3-thiazolidine-2,4-dione
• 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
• SMILES: C1CC(CN(C1)C2=C(C=CC=C2C=C3C(=O)NC(=O)S3)C4=CC=CC=C4)N

AZD1208 (Cat No.:I000752) is a potent orally available Pim kinase inhibitor with IC50 of 0.4nM, 5nM, and 1.9nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest, and apoptosis. If you need, please contact us in time, and we will reply as soon as possible within 24 hours.

Reference

1:Next-generation sequencing identifies a novel ELAVL1-TYK2 fusion gene in MOLM-16, an AML cell line highly sensitive to the PIM kinase inhibitor AZD1208. Tron AE, Keeton EK, Ye M, Casas-Selves M, Chen H, Dillman KS, Gale RE, Stengel C, Zinda M, Linch DC, Lai Z, Khwaja A, Huszar D.Leuk Lymphoma. 2016 Dec;57(12):2927-2929. Epub 2016 May 17. No abstract available. PMID: 27189703 2:Protein profiling identifies mTOR pathway modulation and cytostatic effects of Pim kinase inhibitor, AZD1208, in acute myeloid leukemia. Chen LS, Yang JY, Liang H, Cortes JE, Gandhi V.Leuk Lymphoma. 2016 Dec;57(12):2863-2873. Epub 2016 Apr 7. PMID: 27054578 3:Loss of PIM2 enhances the anti-proliferative effect of the pan-PIM kinase inhibitor AZD1208 in non-Hodgkin lymphomas. Kreuz S, Holmes KB, Tooze RM, Lefevre PF.Mol Cancer. 2015 Dec 8;14:205. doi: 10.1186/s12943-015-0477-z. PMID: 26643319 Free PMC Article4:The novel combination of dual mTOR inhibitor AZD2014 and pan-PIM inhibitor AZD1208 inhibits growth in acute myeloid leukemia via HSF pathway suppression. Harada M, Benito J, Yamamoto S, Kaur S, Arslan D, Ramirez S, Jacamo R, Platanias L, Matsushita H, Fujimura T, Kazuno S, Kojima K, Tabe Y, Konopleva M.Oncotarget. 2015 Nov 10;6(35):37930-47. doi: 10.18632/oncotarget.6122. PMID: 26473447 Free PMC Article5:The PIM inhibitor AZD1208 synergizes with ruxolitinib to induce apoptosis of ruxolitinib sensitive and resistant JAK2-V617F-driven cells and inhibit colony formation of primary MPN cells. Mazzacurati L, Lambert QT, Pradhan A, Griner LN, Huszar D, Reuther GW.Oncotarget. 2015 Nov 24;6(37):40141-57. doi: 10.18632/oncotarget.5653. PMID: 26472029 Free PMC Article6:PIM kinase inhibitor AZD1208 for treatment of MYC-driven prostate cancer. Kirschner AN, Wang J, van der Meer R, Anderson PD, Franco-Coronel OE, Kushner MH, Everett JH, Hameed O, Keeton EK, Ahdesmaki M, Grosskurth SE, Huszar D, Abdulkadir SA.J Natl Cancer Inst. 2014 Dec 13;107(2). pii: dju407. doi: 10.1093/jnci/dju407. Print 2015 Feb. PMID: 25505253 Free PMC Article7:AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia. Keeton EK, McEachern K, Dillman KS, Palakurthi S, Cao Y, Grondine MR, Kaur S, Wang S, Chen Y, Wu A, Shen M, Gibbons FD, Lamb ML, Zheng X, Stone RM, Deangelo DJ, Platanias LC, Dakin LA, Chen H, Lyne PD, Huszar D.Blood. 2014 Feb 6;123(6):905-13. doi: 10.1182/blood-2013-04-495366. Epub 2013 Dec 20. PMID: 24363397 Free PMC Article