153537-73-6

153537-73-6 structure

Name: Plevitrexed
Chemical Name: Plevitrexed
CAS Number: 153537-73-6
Molecular Formula: C₂₆H₂₅FN₈O₄
Molecular Weight: 532.52600
Catalog: Signaling Pathways Apoptosis Thymidylate Synthase
Create Date: 2018-09-20 12:20:42
Modify Date: 2024-01-30 09:32:59
Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical[1][2][3].

Name	Plevitrexed
Synonyms	(2S)-2-((4-(((2,7-Dimethyl-4-oxo-1,4-dihydroquinazolin-6-yl)methyl)(prop-2-ynyl)amino)-2-fluorobenzoyl)amino)-4-(1H-tetrazol-5-yl)butanoic acid Vamidex BGC 9331 (aS)-a-[[4-[[(1,4-Dihydro-2,7-dimethyl-4-oxo-6-quinazolinyl)methyl]-2-propynylamino]-2-fluorobenzoyl]amino]-1H-tetrazole-5-butanoic Acid ZD 9331 FLUOROBENZAMIDO)-4-(1H-TETRAZOL-5-YL)BUTYRIC ACID

Description	Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical[1][2][3].
Related Catalog	Signaling Pathways >> Apoptosis >> Thymidylate Synthase Research Areas >> Cancer
In Vitro	ZD9331 inhibits the transport of [3H]-methotrexate into L1210 and W1L2 cells with a Ki of∼1 µM[3].
References	[1]. Tochowicz A, et al. Development and binding mode assessment of N-[4-[2-propyn-1-yl[(6S)-4,6,7,8-tetrahydro-2-(hydroxymethyl)-4-oxo-3H-cyclopenta[g]quinazolin-6-yl]amino]benzoyl]-l-γ-glutamyl-D-glutamic acid (BGC 945), a novel thymidylate synthase inhibitor that targets tumor cells. J Med Chem. 2013 Jul 11;56(13):5446-55. [2]. A. Thomas, et al. A phase I/II study of plevitrexed with nutritional vitamin supplementation in gastric cancer. [3]. Marsham PR, et al. Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors. J Med Chem. 1999 Sep 23;42(19):3809-20.