产品名称

英文名称：CX-6258

同义词

CX6258;CX 6258;(3E)-5-Chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-2H-indol-2-one、CX6258;CX 6258

产品性质

CAS编号：1202916-90-2

分子式：C26H24ClN3O3

分子量：461.94

PubChem编号：44545852

别名：CX6258;CX 6258

英文别名：CX6258;CX 6258;(3E)-5-Chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-2H-indol-2-one

规格或纯度：≥98%

英文名称：CX-6258

生化机理：DescriptionIC50 Value 5 nM (Pim 1); 25 nM (Pim 2); 16 nM (Pim 3) [1]CX-6258 is a potent, orally efficacious pan-Pim kinases Inhibitor with excellent biochemical potency and kinase selectivity.in vitro CX-6258 inhibited Flt-3 and Pim-3 (IC50=0.134 and 0.016 uM). At 0.5 uM of CX-6258, only Pim-1, Pim-2, Pim-3, and Flt-3 of the 107 kinases tested were inhibited by more than 80%, showing excellent selectivity. CX-6258 was also shown to be a reversible inhibitor of Pim-1 (Ki=0.005 uM). CX-6258 showed robust antiproliferative potencies against all cell lines tested derived from human solid tumors and hematological malignancies. In mechanistic cellular assays with MV-4-11 human AML cells, (13) caused dose-dependent inhibition of the phosphorylation of 2 pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively[1]. Pim-1 inhibition using the small molecule inhibitor CX-6258 (12 mM, 3 h) diminishes endogen

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：卖完停产，不再备货

产品介绍：CX-6258是口服活性的Pim 1，2和3激酶抑制剂，IC50为5 nM，25 nM和16 nM。CX-6258 is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.

IUPAC Name：(3E)-5-chloro-3-[[5-[3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl]furan-2-yl]methylidene]-1H-indol-2-one

INCHI：InChI=1S/C26H24ClN3O3/c1-29-10-3-11-30(13-12-29)26(32)18-5-2-4-17(14-18)24-9-7-20(33-24)16-22-21-15-19(27)6-8-23(21)28-25(22)31/h2,4-9,14-16H,3,10-13H2,1H3,(H,28,31)/b22-16+

InChi Key：KGBPLKOPSFDBOX-CJLVFECKSA-N

Canonical SMILES：CN1CCCN(CC1)C(=O)C2=CC=CC(=C2)C3=CC=C(O3)C=C4C5=C(C=CC(=C5)Cl)NC4=O

Isomeric SMILES：CN1CCCN(CC1)C(=O)C2=CC=CC(=C2)C3=CC=C(O3)/C=C/4\C5=C(C=CC(=C5)Cl)NC4=O

PubChem CID：44545852

ChEMBL Ligand：CHEMBL2037200

BindingDB Ligand：50384714

CAS Registry No.：1202916-90-2

RCSB PDB Ligand：9G5

溶解性：25°C DMSO

产品包装