Methotrexate α-tert-butyl ester 

Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent^[1][2][3][4].

OtBu-MTX-PVG is less HT1080 than MTX-PVG against HT1080 cells. It shows that protection of the α-carboxyl group of MTX results in reduced in vitro activity^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Lys-MTXcleavable- (OtBu) significantly reduces tumor growth in HT1080 tumor bearing mice^[1].
The protection of the α-carboxyl group of methotrexate may be used to improve the circulatory half-life and reduce the liver accumulation of similar MTX-conjugated dendrimers, while still retaining antitumor activity in vivo^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

510.55

C₂₄H₃₀N₈O₅

79640-70-3

固体

Light yellow to yellow

Room temperature in continental US; may vary elsewhere.

• [1]. Kaminskas LM, et al. Capping methotrexate α-carboxyl groups enhances systemic exposure and retains the cytotoxicity of drug conjugated PEGylated polylysine dendrimers. Mol Pharm. 2011;8(2):338-349.  [Content Brief]

  [2]. Tian H, et al. Understanding the mechanisms of action of methotrexate: implications for the treatment of rheumatoid arthritis. Bull NYU Hosp Jt Dis. 2007;65(3):168-73.  [Content Brief]

  [3]. Swierkot J, et al. Methotrexate in rheumatoid arthritis. Pharmacol Rep. 2006 Jul-Aug;58(4):473-92.  [Content Brief]

  [4]. Ehab Tousson, et al. The Effect of L-carnitine on Amethopterin-induced Toxicity in Rat Large Intestine.