DC Chemicals Limited
China
Product Name: Methotrexate α-tert-butyl ester
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Purity: 98.0%
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79640-70-3

79640-70-3 structure

Name: Methotrexate α-tert-butyl ester
Chemical Name: α-OtBu-MTX
CAS Number: 79640-70-3
Molecular Formula: C₂₄H₃₀N₈O₅
Molecular Weight: 510.54600
Catalog: Signaling Pathways Cell Cycle/DNA Damage Antifolate
Create Date: 2018-03-29 18:04:23
Modify Date: 2025-08-26 13:38:58
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
Synonyms	(S)-2-{4-[(2,4-Diamino-pteridin-6-ylmethyl)-methyl-amino]-benzoylamino}-pentanedioic acid 1-tert-butyl ester methotrexate-α-tert-butylester methotrexate-α-OtBu methotrexate methotrexate α-tert-butyl ester α-tert-butyl-N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-L-glutamate MTX-α-OtBu

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.

Molecular Formula	C₂₄H₃₀N₈O₅
Molecular Weight	510.54600
Exact Mass	510.23400
PSA	199.54000
LogP	3.07880

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