Idetrexed  (Synonyms: BGC 945; ONX-0801; CB 300945)

Idetrexed (ONX 0801) is a thymidylate synthase (TS) inhibitor with a K_i of 1.2 nM. Idetrexed can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer^[1][2].

Idetrexed (BGC 945) is designed to further reduce toxicity by more effectively targeting cancer cells that overexpress the α-FR^[1].
Idetrexed (BGC 945) exhibits IC₅₀ values of of 6.6 μM, 1.1 nM, 3.3 nM, 90 nM and 0.32 μM in A431, A431-FBP, KB, IGROV-1 and JEG-3 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Idetrexed (BGC 945) (100 mg/kg, ip/iv injection) in the tumor had a longer half-life (28 hours) compared with other tissues^[2].
Idetrexed (BGC 945) (100 mg/kg daily for 16 days) does not lead to body weight loss, macroscopic signs of toxicity to the major organs, or a change in renal function^[2].
Idetrexed (BGC 945) at 100 mg/kg induces a 5-20-fold increase in tumor dUrd at 4-72 h without increases in the plasma, consistent with tumor targeting^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

647.63

C₃₂H₃₃N₅O₁₀

501332-69-0

C#CCN(C1=CC=C(C=C1)C(N[C@H](C(O)=O)CCC(N[C@@H](C(O)=O)CCC(O)=O)=O)=O)[C@@H]2C3=CC(C(N=C(N4)CO)=O)=C4C=C3CC2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Tochowicz A, Dalziel S, Eidam O, O'Connell JD 3rd, Griner S, Finer-Moore JS, Stroud RM. 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.  [Content Brief]

  [2]. Gibbs DD, Theti DS, Wood N, Green M, Raynaud F, Valenti M, Forster MD, Mitchell F, Bavetsias V, Henderson E, Jackman AL. BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to alpha-folate receptor-overexpressing tumors. Cancer Res. 2005 Dec 15;65(24):11721-8.  [Content Brief]