Plevitrexed

• 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]. Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

• Product Name Alternative:

  ZD 9331; BGC9331

• UNSPSC:

  12352005

• Target:

  Thymidylate Synthase

• Type:

  Reference compound

• Related Pathways:

  Apoptosis

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/plevitrexed.html

• Purity:

  99.35

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  O=C(NC(C)=N1)C2=C1C=C(C)C(CN(C3=CC=C(C(N[C@H](C(O)=O)CCC4=NNN=N4)=O)C(F)=C3)CC#C)=C2

• Molecular Formula:

  C26H25FN8O4

• Molecular Weight:

  532.53

• References & Citations:

  [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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C, 3 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 2

• CAS Number:

  [153537-73-6]