7-Hydroxymethotrexate
Names
Biological Activity
[Description]:
7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis[1][2].
[Related Catalog]:
[In Vitro]
7-Hydroxymethotrexate (7-OHMTX) has the affinity of DHFR markedly lower (>100-fold) than for Methotrexate (MTX) [1].
[In Vivo]
7-Hydroxymethotrexate (4 mg/kg; IV) has a terminal half-life of 97.2 min and a total clearance value of 9.6 mL/min•mg[1]. Animal Model: Male Wistar rats (270-440 g)[1] Dosage: 4 mg/kg (Pharmacokinetic Analysis) Administration: IV Result: Had a terminal half-life of 97.2 min and a total clearance value of 9.6 mL/min•mg.
[References]
Chemical & Physical Properties
[ Density]:
1.68g/cm3
[ Melting Point ]:
230ºC dec.
[ Molecular Formula ]:
C20H22N8O6
[ Molecular Weight ]:
470.43900
[ Exact Mass ]:
470.16600
[ PSA ]:
230.77000
[ LogP ]:
1.52730
[ Index of Refraction ]:
1.76
Toxicological Information
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- MA1000000
- CHEMICAL NAME :
- L-Glutamic acid, N-(4-(((2,4-diamino-1,7-dihydro-7-oxo-6-pteridinyl)me thyl)methylamino) benzoyl)-
- CAS REGISTRY NUMBER :
- 5939-37-7
- LAST UPDATED :
- 199712
- DATA ITEMS CITED :
- 1
- MOLECULAR FORMULA :
- C20-H22-N8-O6
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 300 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- CCPHDZ Cancer Chemotherapy and Pharmacology. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.1- 1978- Volume(issue)/page/year: 37,415,1996