Methotrexate α-tert-butyl ester

Modify Date: 2024-01-13 22:52:46

Methotrexate α-tert-butyl ester structure	Common Name	Methotrexate α-tert-butyl ester
	CAS Number	79640-70-3	Molecular Weight	510.54600
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₄H₃₀N₈O₅	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of 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].

Name	α-OtBu-MTX
Synonym	More Synonyms

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> Antifolate Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis
In Vitro	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].
In Vivo	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]. Animal Model: Female, Balb/c nu/nu, 6 weeks (bearing HT1080 cells)[1] Dosage: 30 mg/kg Administration: Once per week for 2 weeks Result: Showed a significant (63%) reduction in tumor size on day 12.
References	[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. [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. [3]. Swierkot J, et al. Methotrexate in rheumatoid arthritis. Pharmacol Rep. 2006 Jul-Aug;58(4):473-92. [4]. Ehab Tousson, et al. The Effect of L-carnitine on Amethopterin-induced Toxicity in Rat Large Intestine.