206275-15-2

206275-15-2 structure

Name: CB30865
Chemical Name: 4-[(7-bromo-2-methyl-4-oxo-1H-quinazolin-6-yl)methyl-prop-2-ynylamino]-N-(pyridin-3-ylmethyl)benzamide
CAS Number: 206275-15-2
Molecular Formula: C₂₆H₂₂BrN₅O₂
Molecular Weight: 516.38900
Catalog: Signaling Pathways Metabolic Enzyme/Protease Nampt
Create Date: 2016-05-31 12:03:34
Modify Date: 2024-01-02 18:54:05
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.

Name	4-[(7-bromo-2-methyl-4-oxo-1H-quinazolin-6-yl)methyl-prop-2-ynylamino]-N-(pyridin-3-ylmethyl)benzamide
Synonyms	CB30865

Description	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.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Nampt Research Areas >> Cancer
References	[1]. Lockman JW, et al. Analogues of 4-[(7-Bromo-2-methyl-4-oxo-3H-quinazolin-6-yl)methylprop-2-ynylamino]-N-(3-pyridylmethyl)benzamide (CB-30865) as potent inhibitors of nicotinamide phosphoribosyltransferase (Nampt). J Med Chem. 2010 Dec 23;53(24):8734-8746. [2]. Fleischer TC, et al. Chemical proteomics identifies Nampt as the target of CB30865, an orphan cytotoxic compound. Chem Biol. 2010 Jun 25;17(6):659-664. [3]. Bavetsias V, et al. The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent. J Med Chem. 2002 Aug 15;45(17):3692-3702. [4]. Skelton LA, et al. Cell cycle effects of CB30865, a lipophilic quinazoline-based analogue of the antifolate thymidylate synthase inhibitor ICI 198583 with an undefined mechanism of action. Cytometry. 1998 Sep 1;33(1):56-66.