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CX-6258Pan-Pim kinases Inhibitor

CX-6258

Catalog No. A3337
Size Price Stock Qty
10mM (in 1mL DMSO) $132.00 In stock
5mg $90.00 In stock
10mg $140.00 In stock
25mg $270.00 In stock
50mg $450.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

CX-6258

Biological Activity

Description CX-6258 HCl is a potent, orally efficacious inhibitor of pan-Pim kinase with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively.
Targets Pim1 Pim3 Pim2      
IC50 5 nM 16 nM 25 nM      

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Chemical Properties

Cas No. 1202916-90-2 SDF Download SDF
Synonyms CX6258;CX 6258
Chemical Name (E)-5-chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one
Canonical SMILES CN1CCCN(C(C2=CC(C3=CC=C(/C=C4C(C=C(Cl)C=C5)=C5NC\4=O)O3)=CC=C2)=O)CC1
Formula C26H24ClN3O3 M.Wt 461.94
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

Pim kinases (Provirus Integration site for Moloney murine leukemia virus) are a family of serine/threonine kinases that regulate cell survival. This family of kinases is composed of three different isoforms (Pim-1, Pim-2, and Pim-3). The simultaneous inhibition of Pim-1, Pim-2, and Pim-3 kinases is emerging as a promising strategy for anticancer drug development. CX-6258 is a potent, selective, and orally efficacious pan-Pim kinases inhibitor.

In vitro: CX-6258 exhibited in vitro synergy with chemotherapeutics. The antiproliferative activity of CX-6258 was examined against a panel of cell lines derived from human solid tumors and hematological malignancies. CX-6258 demonstrated robust antiproliferative potencies against all cell lines tested [1].

In vivo: CX-6258 was evaluated in two human tumor xenograft growth efficacy models, acute myeloid leukemia MV-4-11, and prostate adenocarcinoma PC3. The drug 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. In addition, CX-6258 displayed significant efficacy in vivo in two xenograft models representing the diseases where Pim kinases had been shown to play an important role [1].

Clinical trial: No clinical data are available

Reference:
[1] Haddach M, Michaux J, Schwaebe MK, et al.  Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med Chem Lett. 2011;3(2):135-9.