CX-6258 MedChemExpress (MCE)

Product Name	CX-6258
Synonyms	CX6258 CX-6258 CX 6258 (Z)-5-CHLORO-3-((5-(3-(4-METHYL-1,4-DIAZEPANE-1-CARBONYL)PHENYL)FURAN-2-YL)METHYLENE)INDOLIN-2-ONE.HCL (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 Synonyms CX6258 CX-6258 CX 6258 (Z)-5-CHLORO-3-((5-(3-(4-METHYL-1,4-DIAZEPANE-1-CARBONYL)PHENYL)FURAN-2-YL)METHYLENE)INDOLIN-2-ONE.HCL (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 (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 CX-6258 CX6258 (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
CAS	1202916-90-2
EINECS
Chemical Formula	C26H24ClN3O3
Molecular Weight	461.94
inchi
Package	10 mM * 1 mL;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	CX-6258 CX-6258 MedChemExpress (MCE) HY-18095 1202916-90-2 98.71% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions CX-6258 CX-6258 MedChemExpress (MCE) HY-18095 1202916-90-2 98.71% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. CX-6258 is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively. CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively[1]. CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells[2]. CX-6258 treatment results in a significant reduction in NKX3.1 half-life[2]. CX-6258 (50-100 mg/kg p.o daily over a period of 21 days) exhibits robust in vivo efficacy in two Pim kinases driven tumor models[1]. IC50: 5 nM (Pim-1), 25 nM (Pim-2), 16 nM (Pim-3)[1] Cellular Effect Cell Line Type Value Description References \| \| \| \| \| \| \| \| \| \| [1]. Mustapha Haddach, Jerome Michaux, Michael K, Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med. Chem. Lett., 2012, 3 (2), pp 135-139 [2]. Padmanabhan A, Gosc EB, Bieberich CJ. Stabilization of the prostate-specific tumor suppressor NKX3.1 by the oncogenic protein kinase Pim-1 in prostate cancer cells. J Cell Biochem. 2013 May 114(5):1050-7. [Content Brief]
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Last Update	2025-05-21 16:50:25

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