CX-6258 - CAS 1202916-90-2
Catalog number: 1202916-90-2
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
Pim
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Related CAS:
1353858-99-7 (CX-6258 HCl salt, hydrate)
Appearance:
orange solid powder
Synonyms:
(E)-5-chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one; CX6258; CX-6258; CX 6258
MSDS:
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InChIKey:
KGBPLKOPSFDBOX-CJLVFECKSA-N
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+
Canonical SMILES:
O=C1NC2=C(C=C(Cl)C=C2)/C1=C\C3=CC=C(C4=CC=CC(C(N5CCN(C)CCC5)=O)=C4)O3
1.Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.
Haddach M1, Michaux J1, Schwaebe MK1, Pierre F1, O'Brien SE1, Borsan C1, Tran J1, Raffaele N1, Ravula S1, Drygin D1, Siddiqui-Jain A1, Darjania L1, Stansfield R1, Proffitt C1, Macalino D1, Streiner N1, Bliesath J1, Omori M1, Whitten JP1, Anderes K1, Rice ACS Med Chem Lett. 2011 Dec 27;3(2):135-9. doi: 10.1021/ml200259q. eCollection 2012.
Structure-activity relationship analysis in a series of 3-(5-((2-oxoindolin-3-ylidene)methyl)furan-2-yl)amides identified compound 13, a pan-Pim kinases inhibitor with excellent biochemical potency and kinase selectivity. Compound 13 exhibited in vitro synergy with chemotherapeutics and robust in vivo efficacy in two Pim kinases driven tumor models.
2.Synthesis of [11C]CX-6258 as a new PET tracer for imaging of Pim kinases in cancer.
Wang M1, Tzintzun R1, Gao M1, Xu Z2, Zheng QH3. Bioorg Med Chem Lett. 2015 Sep 15;25(18):3831-5. doi: 10.1016/j.bmcl.2015.07.061. Epub 2015 Jul 26.
The reference standard CX-6258 {(E)-5-chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one, 4a} and its desmethylated precursor N-desmethyl-CX-6258 {(E)-3-((5-(3-(1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)-5-chloroindolin-2-one, 5} for radiolabeling were synthesized from 5-bromo-2-furaldehyde and 3-carboxybenzeneboronic acid in 3 and 4 steps with 29-49% and 24-32% overall chemical yield, respectively. The target tracer [(11)C]CX-6258 {(E)-5-chloro-3-((5-(3-(4-[(11)C]methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one, [(11)C]4a} was prepared from N-desmethyl-CX-6258 (5) with [(11)C]CH3OTf under basic condition (2N NaOH) through N-[(11)C]methylation and isolated by HPLC combined with solid-phase extraction (SPE) in 40-50% radiochemical yield based on [(11)C]CO2 and decay corrected to end of bombardment (EOB) with 370-1110GBq/μmol specific activity at EOB.
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