| Identification | Back Directory | [Name]
CX 6258 hydrochloride hydrate | [CAS]
1353858-99-7 | [Synonyms]
CX-6258 HCl hydrate
CX6258 hydrochloride hydrate
CX 6258 hydrochloride hydrate
CX-6258 (hydrochloride hydrate)
CX-6258 hydrochloride hydrate
(CX6258 hydrochloride hydrate)
(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 hydrochloride hydrate (1:1:1) | [Molecular Formula]
C26H27Cl2N3O4 | [MDL Number]
MFCD26142938 | [MOL File]
1353858-99-7.mol | [Molecular Weight]
516.42 |
| Hazard Information | Back Directory | [Uses]
CX-6258 hydrochloride hydrate 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[1]. | [in vivo]
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].
| Animal Model: | Nude mice, MV-4-11 xenograft models[1] | | Dosage: | 50 mg/kg, 100 mg/kg. | | Administration: | Oral administration; once daily; over a period of 21 days. | | Result: | Exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI. |
| [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. DOI:10.1002/jcb.24444 |
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SPIRO PHARMA
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Musechem
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Twochem Co.Ltd.
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InvivoChem
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