CX-6258 is a pan-Pim kinases inhibitor with excellent biochemical potency and kinase selectivity. CX-6258 exhibited in vitro synergy with chemotherapeutics and robust in vivo efficacy in two Pim kinases driven tumor models. Inhibition of Pim kinases is expected to have a beneficial effect as cancer therapy.
CAS Number: 1202916-90-2
Molecular Weight: 461.94
Chemical Name: (E)-5-chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
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.
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.
- Mustapha Haddach *, Jerome Michaux , Michael K. Schwaebe , Fabrice Pierre , Sean E. OÂ’Brien , Cosmin Borsan , Joe Tran , Nicholas Raffaele , Suchitra Ravula , Denis Drygin , Adam Siddiqui-Jain , Levan Darjania , Ryan Stansfield , Chris Proffitt , Diwata Macalino , Nicole Streiner , Joshua Bliesath , May Omori , Jeffrey P. Whitten , Kenna Anderes , William G. Rice , and David M. Ryckman. ACS Med. Chem. Lett., 2012, 3 (2), pp 135Â–139.
Products are for research use only. Not for human use.
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