CX-6258 hydrochloride hydrate

CAS No. 1353858-99-7

CX-6258 hydrochloride hydrate( CX6258 hydrochloride hydrate )

Catalog No. M11441 CAS No. 1353858-99-7

A potent, selective, and orally efficacious pan-Pim inhibitor with IC50 of 5/25/16 nM for Pim1/2/3, respectively.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    CX-6258 hydrochloride hydrate
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective, and orally efficacious pan-Pim inhibitor with IC50 of 5/25/16 nM for Pim1/2/3, respectively.
  • Description
    A potent, selective, and orally efficacious pan-Pim inhibitor with IC50 of 5/25/16 nM for Pim1/2/3, respectively; exhibits in vitro synergy with chemotherapeutics and robust in vivo efficacy in driven tumor models; also decreases steady state levels and half-life of NKX3.1 protein but not mRNA in prostate cancer cells.Blood Cancer Discontinued.
  • In Vitro
    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.CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells.CX-6258 treatment results in a significant reduction in NKX3.1 half-life.Western Blot Analysis Cell Line:MV-4-11 human AML cells.Concentration:0.1 μM, 1 μM, 10 μM.Incubation Time:2 hours.Result:Caused 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.
  • 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. Animal Model:Nude mice, MV-4-11 xenograft models 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.
  • Synonyms
    CX6258 hydrochloride hydrate
  • Pathway
    JAK/STAT Signaling
  • Target
    Pim
  • Recptor
    Pim
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    1353858-99-7
  • Formula Weight
    516.4163
  • Molecular Formula
    C26H27Cl2N3O4
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    CN1CCCN(CC1)C(=O)C2=CC=CC(=C2)C3=CC=C(O3)C=C4C5=C(C=CC(=C5)Cl)NC4=O.O.Cl
  • Chemical Name
    2H-Indol-2-one, 5-chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-, hydrochloride, hydrate (1:1:1), (3E)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Haddach M, et al. ACS Med Chem Lett. 2011 Dec 27;3(2):135-9. 2. Padmanabhan A, et al. J Cell Biochem. 2013 May;114(5):1050-7. 3. Rebello RJ, et al. Clin Cancer Res. 2016 Nov 15;22(22):5539-5552.
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