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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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A127698-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $58.90 | |
A127698-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $265.90 | |
A127698-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $474.90 |
Potent pan Pim kinase inhibitor
Synonyms | AZD 1208 [WHO-DD] | Q27074698 | FT-0633869 | J-013789 | HY-15604 | S98NFM1378 | SW219766-1 | 1204144-28-4 | AZ-1208 | (R,Z)-5-((2-(3-Aminopiperidin-1-yl)biphenyl-3-yl)methylene)thiazolidine-2,4-dione | CS-1668 | AZD1208 | AZD-1208 | NSC776066 | NSC-776066 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Potent pan Pim kinase inhibitor (IC50values are 0.4, 1.9 and 5.0 nM for Pim-1, 3 and 2, respectively). Exhibits >43-fold higher affinity for Pim kinases over a range of other kinases. Induces cell cycle arrest and apoptosis in AML cell linesin vitroand in |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of Pim-1 proto-oncogene; serine/threonine kinase;Inhibitor of Pim-2 proto-oncogene; serine/threonine kinase;Inhibitor of Pim-3 proto-oncogene; serine/threonine kinase |
Note | 5mg、100mg卖完停产,不再备货 |
Product Description | AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. |
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IUPAC Name | (5Z)-5-[[2-[(3R)-3-aminopiperidin-1-yl]-3-phenylphenyl]methylidene]-1,3-thiazolidine-2,4-dione |
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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 |
InChi Key | MCUJKPPARUPFJM-UWCCDQBKSA-N |
Canonical SMILES | C1CC(CN(C1)C2=C(C=CC=C2C3=CC=CC=C3)C=C4C(=O)NC(=O)S4)N |
Isomeric SMILES | C1C[C@H](CN(C1)C2=C(C=CC=C2C3=CC=CC=C3)/C=C\4/C(=O)NC(=O)S4)N |
PubChem CID | 58423153 |
Molecular Weight | 379.48 |
PubChem CID | 58423153 |
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ChEMBL Ligand | CHEMBL2048872 |
CAS Registry No. | 1204144-28-4 |
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Solubility | Solvent:DMSO, Max Conc. mg/mL: 7.59, Max Conc. mM: 20 with gentle warming |
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1. Keeton EK, McEachern K, Dillman KS, Palakurthi S, Cao Y, Grondine MR, Kaur S, Wang S, Chen Y, Wu A et al.. (2014) AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia.. Blood, 123 (6): (905-13). [PMID:24363397] |
2. Burger MT, Han W, Lan J, Nishiguchi G, Bellamacina C, Lindval M, Atallah G, Ding Y, Mathur M, McBride C et al.. (2013) Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.. ACS Med Chem Lett, 4 (12): (1193-7). [PMID:24900629] |