Idetrexed trisodium
Idetrexed (ONX 0801) trisodium is a thymidylate synthase (TS) inhibitor with a Ki of 1.2 nM. Idetrexed trisodium can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer.
For research use only. We do not sell to patients.
- CAS No.: 1097638-00-0
- Formula: C32H30N5Na3O10
- Molecular Weight:713.58
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Idetrexed (BGC 945) trisodium is designed to further reduce toxicity by more effectively targeting cancer cells that overexpress the α-FR[1].
Idetrexed (BGC 945) trisodium 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 daily for 16 days) trisodium 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) trisodium 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.
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Animal Model:Mice (on the folate-free diet for 5 days were transplanted with tumor and the implants)[2].
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Dosage:100 mg/kg (Pharmacokinetic Analysis).
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Administration:Single i.p. or iv injection.
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Result:After i.p. injection, the compound was well absorbed from the peritoneal cavity. The plasma AUC was 50% higher for i.p. compared with i.v. administration and was also higher in spleen, kidney, and liver by this route. Tumor AUC was similar via either route.
Chemical Information
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CAS No. 1097638-00-0
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Molecular Weight 713.58
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Formula C32H30N5Na3O10
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SMILES
O=C(N[C@H](C(O[Na])=O)CCC(N[C@@H](C(O[Na])=O)CCC(O[Na])=O)=O)C1=CC=C(N([C@H]2CCC3=C2C=C4C(NC(CO)=NC4=O)=C3)CC#C)C=C1
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Synonyms
BGC 945 trisodium; ONX 0801 trisodium; CB 300945 trisodium
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Anna Tochowicz, 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. [Content Brief]
[2]. David D Gibbs, et 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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Idetrexed trisodium Related Classifications
HY-10822A Related Classifications
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