Idetrexed
Idetrexed (ONX 0801) is a thymidylate synthase (TS) inhibitor with a Ki of 1.2 nM. Idetrexed can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer.
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- No. CAS: 501332-69-0
- Fòrmula: C32H33N5O10
- Peso molecular:647.63
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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 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.
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 501332-69-0
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Peso molecular 647.63
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Fòrmula C32H33N5O10
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SMILES
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
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Synonyms
BGC 945; ONX-0801; CB 300945
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Idetrexed Related Classifications
HY-10822 Related Classifications
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