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AZD1208 Catalog No : 51702

Chemical Information

Product NameAZD1208
Iupac Chemical Name(5Z)-5-[[2-[(3R)-3-amino-1-piperidinyl][1,1'-biphenyl]-3-yl]methylene]-2,4-thiazolidinedione 
SynonymsAZD1208;AZ-1208 
Molecular FormulaC21H21N3O2S 
Molecular Weight379.48 
SmileN[C@H]1CN(CCC1)C1=C(C=CC=C1\C=C/1\C(NC(S1)=O)=O)C1=CC=CC=C1
InChiKeyMCUJKPPARUPFJM-UWCCDQBKSA-N
InChiInChI=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
Cas1204144-28-4

Technical Data

Appearancelight-yellow solid to off-white solid 
Purity98% by HPLC/HNMR 
Solubility2mg/ml in DMSO 
Storage3 years -20ºCpowder 
Shipping ConditionShipped under ambient temperature. 
Quality control HNMR HPLC

Description

AZD1208 is a potent, highly selective, and orally available Pim kinase inhibitor that effectively inhibits all three isoforms at <5 nM or <150 nM in enzyme and cell assays, respectively. AZD1208 inhibited the growth of 5 of 14 acute myeloid leukemia (AML) cell lines tested, and sensitivity correlates with Pim-1 expression and STAT5 activation. AZD1208 causes cell cycle arrest and apoptosis in MOLM-16 cells, accompanied by a dose-dependent reduction in phosphorylation of Bcl-2 antagonist of cell death, 4EBP1, p70S6K, and S6, as well as increases in cleaved caspase 3 and p27. Inhibition of p4EBP1 and p-p70S6K and suppression of translation are the most representative effects of Pim inhibition in sensitive AML cell lines. AZD1208 inhibits the growth of MOLM-16 and KG-1a xenograft tumors in vivo with a clear pharmacodynamic-pharmacokinetic relationship. AZD1208 also potently inhibits colony growth and Pim signaling substrates in primary AML cells from bone marrow that are Flt3 wild-type or Flt3 internal tandem duplication mutant.

 

Chemical Structure

51702 - AZD1208 | CAS 1204144-28-4

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