CX-6258

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.

Product information

CAS Number: 1202916-90-2

Molecular Weight: 461.94

Formula: C26H24ClN3O3

Synonym:

CX-6258

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

Smiles: CN1CCCN(CC1)C(=O)C1=CC(=CC=C1)C1=CC=C(/C=C2\C3=CC(Cl)=CC=C3NC\2=O)O1

InChiKey: KGBPLKOPSFDBOX-CJLVFECKSA-N

InChi: InChI=1S/C26H24ClN3O3/c1-29-10-3-11-30(13-12-29)26(32)18-5-2-4-17(14-18)24-9-7-20(33-24)16-22-21-15-19(27)6-8-23(21)28-25(22)31/h2,4-9,14-16H,3,10-13H2,1H3,(H,28,31)/b22-16+

Technical Data

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

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.

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.

References:

1. Mustapha Haddach *, Jerome Michaux , Michael K. Schwaebe , Fabrice Pierre , Sean E. O’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 135–139.

Products are for research use only. Not for human use.