18921-70-5
18921-70-5
Chemical Structure
Methasquin
- CAS. Nr.: 18921-70-5
- Formula:C21H22N6O5
- Molecular Weight:438.44
InChIKey: NTKNUVXCGJPJQP-HNNXBMFYSA-N
SMILES: CC1=C(CNC2=CC=C(C=C2)C(N[C@H](C(O)=O)CC(O)=O)=O)C=CC3=C1C(N)=NC(N)=N3
Biological Activity: Methasquin is an antifolate dihydrofolate reductase inhibitor (antifolate dihydrofolate reductase) with an IC50 of 1.3 nM against dihydrofolate reductase derived from human leukemia cells. Methasquin binds to dihydrofolate reductase, depletes tetrahydrofolate derivatives, disrupts thymidylate synthesis and inhibits DNA synthesis. Methasquin can be used in leukemia-related research[1][2][3][4][5][6].
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Methasquin | Methasquin is an antifolate dihydrofolate reductase inhibitor (antifolate dihydrofolate reductase) with an IC50 of 1.3 nM against dihydrofolate reductase derived from human leukemia cells. Methasquin binds to dihydrofolate reductase, depletes tetrahydrofolate derivatives, disrupts thymidylate synthesis and inhibits DNA synthesis. Methasquin can be used in leukemia-related research. | |||||||||||||||||||||
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References
- [1]. Rader JI, et al. Urinary and biliary excretion of the 2,4-diaminoquinazoline antifolate, methasquin, in rats and dogs. Cancer Res. 1971 Jul;31(7):964-9.
- [2]. Sirotnak FM, et al. Comparative studies on the transport of aminopterin, methotrexate, and methasquin by the L1210 leukemia cell. Cancer Res. 1972 Oct;32(10):2120-6.
- [3]. Biedler JL, et al. Biochemical and karyological properties of cells resistant to the quinazoline antifolate, methasquin. Eur J Cancer (1965). 1978 Jan;14(1):41-9.
- [4]. Sirotnak FM, et al. A basis for the difference in toxicity of methotrexate, aminopterin and methasquin in mice. Biochem Pharmacol. 1975 Jan 1;24(1):156-8.
- [5]. Johns DG, et al. Quinazoline antifolates as inhibitors of dihydrofolate reductase from human leukemia cells. Biochem Pharmacol. 1970 Apr;19(4):1528-33.
- [6]. Philips FS, et al. Uptake of methotrexate, aminopterin, and methasquin and inhibition of dihydrofolate reductase and of DNA synthesis in mouse small intestine. Cancer Res. 1973 Jan;33(1):153-8. [Content Brief]
