CB30865

• CAT Number: I002587
• CAS Number: 206275-15-2
• Molecular Formula: C26H22BrN5O2
• Molecular Weight: 516.399
• Purity: ≥95%
• Target: Nampt
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IUPAC Name: 4-[(7-bromo-2-methyl-4-oxo-1H-quinazolin-6-yl)methyl-prop-2-ynylamino]-N-(pyridin-3-ylmethyl)benzamide
• InChI: InChI=1S/C26H22BrN5O2/c1-3-11-32(16-20-12-22-24(13-23(20)27)30-17(2)31-26(22)34)21-8-6-19(7-9-21)25(33)29-15-18-5-4-10-28-14-18/h1,4-10,12-14H,11,15-16H2,2H3,(H,29,33)(H,30,31,34)
• InChIKey: SHNBLWMBWXIKMR-UHFFFAOYSA-N
• SMILES: CC1=NC(=O)C2=CC(=C(C=C2N1)Br)CN(CC#C)C3=CC=C(C=C3)C(=O)NCC4=CN=CC=C4

CB30865(ZM 242421) is a potent inhibitor of Nampt , an enzyme present in the NAD biosynthetic pathway.IC50 value:Target: NamptCancer cells develop dependence on Nampt due to increased energy requirements and the elevated activity of NAD consuming enzymes such as sirtuins and mono and poly(ADP-ribose) polymerases (PARPs). These findings suggest new chemical starting points for Nampt inhibitors and further implicate this enzyme as a target in cancer.

Reference

1:Chemical proteomics identifies Nampt as the target of CB30865, an orphan cytotoxic compound. Fleischer TC, Murphy BR, Flick JS, Terry-Lorenzo RT, Gao ZH, Davis T, McKinnon R, Ostanin K, Willardsen JA, Boniface JJ.Chem Biol. 2010 Jun 25;17(6):659-64. doi: 10.1016/j.chembiol.2010.05.008. PMID: 20609415 Free Article2:The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent. Bavetsias V, Skelton LA, Yafai F, Mitchell F, Wilson SC, Allan B, Jackman AL.J Med Chem. 2002 Aug 15;45(17):3692-702. PMID: 12166942 3:Cell cycle effects of CB30865, a lipophilic quinazoline-based analogue of the antifolate thymidylate synthase inhibitor ICI 198583 with an undefined mechanism of action. Skelton LA, Ormerod MG, Titley JC, Jackman AL.Cytometry. 1998 Sep 1;33(1):56-66. PMID: 9725559