Methylbenzoprim | Dual thymidylate synthase/dihydrofolate reductase inhibitor

Methylbenzoprim supplier | CAS 118344-71-1 | Focus Biomolecules

Available Options

SizePriceQuantity 
5mg$70.00
25mg$250.00
Request Quote / Bulk / Custom Size
Product Inquiry

Methylbenzoprim (118344-71-1; Compound 19-S), a derivative of the antimalarial drug Pyrimethamine, is a non-classical potent inhibitor of mammalian dihydrofolate reductase (IC50 = 3.2 nM rat liver).1 It inhibited melanoma tumor growth both in vitro and in vivo.2 Methylbenzoprim has been recently found to also inhibit thymidylate synthase (TYMS) with activity comparable to the 5-FU metabolite FdUrd.3  It was more potent than 5-fluorouracil in a panel of 4 pancreatic ductal adenocarcinoma cells lines and without TYMS overexpression that frequently leads to drug resistance.3  Methylbenzoprim inhibited tumor growth and progression in two pancreatic cancer xenograft models. Orally bioavailable.

References/Citations:

  1. Griffin et al. (1989), Structural studies on bioactive compounds. 8. Synthesis, crystal structure, and biological properties of a new series pf 2,4-diamino-5-aryl-6-ethylpyrimidine dihydrofolate reductase inhibitors with in vivo activity against methotrexate-resistant tumor cell line; J. Med. Chem., 32 2468
  2. Tommasino et al. (2016), New derivatives of the antimalarial drug Pyrimethamine in the control of melanoma tumor growth: an in vitro and in vivo study; J. Exp. Clin. Cancer Res., 35 137
  3. Guijarro et al. (2023), First-in-class multifunctional TYMS non-classical antifolate inhibitor with potent in vivo activity that prolongs survival; JCI Insight, 8 e158798
118344-71-1, Compound 19-S, dihydrofolate reductase inhibitor, methylbenzoprim, Methylbenzoprim supplier, Thymidylate synthase inhibitor
Alternate Name:
Compound 19-S; NSC-382035

Safety Data Sheet:

Download Safety Data Sheet

Product Data Sheet:

Download Product Data Sheet

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

Methylbenzoprim (118344-71-1; Compound 19-S), a derivative of the antimalarial drug Pyrimethamine, is a non-classical potent inhibitor of mammalian dihydrofolate reductase (IC50 = 3.2 nM rat liver).1 It inhibited melanoma tumor growth both in vitro and in vivo.2 Methylbenzoprim has been recently found to also inhibit thymidylate synthase (TYMS) with activity comparable to the 5-FU metabolite FdUrd.3  It was more potent than 5-fluorouracil in a panel of 4 pancreatic ductal adenocarcinoma cells lines and without TYMS overexpression that frequently leads to drug resistance.3  Methylbenzoprim inhibited tumor growth and progression in two pancreatic cancer xenograft models. Orally bioavailable.

References/Citations:

  1. Griffin et al. (1989), Structural studies on bioactive compounds. 8. Synthesis, crystal structure, and biological properties of a new series pf 2,4-diamino-5-aryl-6-ethylpyrimidine dihydrofolate reductase inhibitors with in vivo activity against methotrexate-resistant tumor cell line; J. Med. Chem., 32 2468
  2. Tommasino et al. (2016), New derivatives of the antimalarial drug Pyrimethamine in the control of melanoma tumor growth: an in vitro and in vivo study; J. Exp. Clin. Cancer Res., 35 137
  3. Guijarro et al. (2023), First-in-class multifunctional TYMS non-classical antifolate inhibitor with potent in vivo activity that prolongs survival; JCI Insight, 8 e158798