1. Cell Cycle/DNA Damage
  2. Antifolate
    DNA/RNA Synthesis
  3. Methotrexate α-tert-butyl ester

Methotrexate α-tert-butyl ester 

目录号: HY-133887
产品使用指南

Methotrexate α-tert-butyl ester,经 OtBu 修饰,显著降低 HT1080 荷瘤小鼠的肿瘤生长。Methotrexate 是一种抗代谢和抗叶叶酸剂,也是一种免疫抑制剂和抗肿瘤药物。

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Methotrexate α-tert-butyl ester Chemical Structure

Methotrexate α-tert-butyl ester Chemical Structure

CAS No. : 79640-70-3

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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].

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.
Molecular Weight

510.55

Formula

C₂₄H₃₀N₈O₅

CAS No.

79640-70-3

SMILES

O=C(O)CC[C@H](NC(C1=CC=C(N(CC2=NC3=C(N)N=C(N)N=C3N=C2)C)C=C1)=O)C(OC(C)(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

Methotrexate α-tert-butyl esterAntifolateDNA/RNA SynthesisOtButumorgrowthHT1080cellscirculatoryhalf-lifeInhibitorinhibitorinhibit

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产品名称:
Methotrexate α-tert-butyl ester
目录号:
HY-133887
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