| Bioactivity | Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia[1][2]. | |||||||||
| Invitro | The IC50 value of Aminopterin (4-Aminofolic acid) against CCRF-CEM cells during 72 h of exposure is 4.4 nM[2].Aminopterin (4-Aminofolic acid) produces a marked inhibition of mitosis in low concentrations in human leukemic leukocytes[4]. | |||||||||
| Name | Aminopterin | |||||||||
| CAS | 54-62-6 | |||||||||
| Formula | C19H20N8O5 | |||||||||
| Molar Mass | 440.41 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. MEYER LM, et al. Aminopterin, a folic acid antagonist, in the treatment of leukemia. Am J Clin Pathol. 1949 Feb;19(2):119-26. [2]. Rosowsky A, et al. Synthesis and in vitro antifolate activity of rotationally restricted aminopterin and methotrexate analogues. J Med Chem. 2004 Dec 30;47(27):6958-63. [3]. Gebhardt DO, et al. The influence of aminopterin on limb regeneration in Ambystoma mexicanum. J Embryol Exp Morphol. 1966 Aug;16(1):143-58. [4]. F. W Gtmrz, et al. THE EFFECT OF 4-AMINO-PTEROYLGLUTAMIC ACID (AMINOPTERIN) ON HUMAN LEUKEMIC LEUKOCYTES IN VITRO. Blood (1950) 5 (2): 161-166. |