Abitrexate is an antimetabolite and antifolate agent with antineoplastic and immunosuppressant activities. Abitrexate (Methotrexate) inhibits dihydrofolate reductase (DHFR), resulting in inhibition of purine nucleotide and thymidylate synthesis. Abitrexate performed growth inhibitory activity with median IC50 78 nM in a panel of six pediatric leukemia and lymphoma cell lines.
Molecular Weight | 454.44 |
Formula | C20H22N8O5 |
CAS Number | 59-05-2 |
Solubility (25°C) | DMSO 60 mg/mL |
Storage | 2-8°C, protect from light, sealed |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related Antifolate Products |
---|
Methotrexate hydrate
Methotrexate hydrate is an antimetabolite and antifolate that inhibits dihydrofolate reductase, thereby preventing the conversion of folic acid to tetrahydrofolate and inhibiting DNA synthesis. In addition, Methotrexate hydrate is an immunosuppressant and antitumor agent used in studies related to rheumatoid arthritis and various cancers such as acute lymphoblastic leukemia. |
Trimetrexate glucuronate
Trimetrexate glucuronate (NSC 352122) is a folic acid antagonist. Trimetrexate glucuronate affects DNA and RNA synthesis by inhibiting dihydrofolate reductase and preventing the synthesis of purine nucleotides and thymidylate. Trimetrexate glucuronate has potential antitumour activity and can also be used to inhibit Pneumocystis carinii pneumonia. |
Pemetrexed disodium heptahydrate
Pemetrexed disodium heptahydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively. |
Fanotaprim
Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC50s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. Fanotaprim has the potential for the research of toxoplasmosis. |
LSN 3213128
LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.