CX-6258

CAS No. 1202916-90-2

CX-6258( CX6258 | CX 6258 )

Catalog No. M10741 CAS No. 1202916-90-2

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 43 In Stock
5MG 72 In Stock
10MG 115 In Stock
25MG 230 In Stock
50MG 372 In Stock
100MG 531 In Stock
200MG 771 In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    CX-6258
  • 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 modelsDosage: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 | CX 6258
  • Pathway
    JAK/STAT Signaling
  • Target
    Pim
  • Recptor
    Pim1| Pim2| Pim3
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    1202916-90-2
  • Formula Weight
    461.9401
  • Molecular Formula
    C26H24ClN3O3
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    CN1CCCN(CC1)C(=O)C2=CC=CC(=C2)C3=CC=C(O3)/C=C/4\C5=C(C=CC(=C5)Cl)NC4=O
  • 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-, (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.
molnova catalog
related products
  • INCB053914

    INCB053914 (INCB-053914) is a novel potent, and selective ATP-competitive, pan-PIM kinase inhibitor with IC50 of 0.24/30.0/0.12 nM for PIM1/2/3, respectively.

  • PIM-447 dihydrochlor...

    A highly potent and selective inhibitor of pan-Pim with IC50s of 6/18/9 pM for Pim/1/2/3 respectively.

  • GDC-0339

    GDC-0339 is a novel small molecule pan-Pim kinase inhibitor that was discovered as a potential treatment for multiple myeloma.