マイタンシン

マイタンシン 価格

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マイタンシン 化学特性,用途語,生産方法

効能

抗悪性腫瘍薬, 微小管重合阻害薬

説明

This novel ansa macrolide alkaloid occurs in a number of May tan us species. The structure given has been elucidated from chemical and spectroscopic data. In low doses (25-50 mcg/kg), maytansine prolonged the survival of mice bearing vincristine-sensitive P388 leukemia but not those bearing vincristine-resistant tumour lines. In vitro, it suppressed the growth of U21 0, LSl78Y and P388 leukemia cells with ED₅₀ of 2 X 10^-9 , 1.5 X 10^-9 and 6 X 10^-10M respectively and elevated the mitotic index in L 121 0 cells. From labelling studies it was shown that the alkaloid inhibited DNA formation by P388 cells to a greater extent than RNA and protein synthesis. Maytensine did not inhibit RNA polymerase from Escherichia coli at levels as high as 1 X 10^-4M.

使用

Antineoplastic.

定義

ChEBI: An organic heterotetracyclic compound and 19-membered macrocyclic lactam antibiotic originally isolated from the Ethiopian shrub Maytenus serrata but also found in other Maytenus species. It exhibits cytotoxicity against many tumo r cell lines.

生物学の機能

Maytansine is a potent microtubule-targeted compound that inhibits proliferation of cells at mitosis. Antibody-maytansinoid conjugates consisting of maytansinoids (DM1 and DM4) attached to tumor-specific antibodies have shown promising clinical results The microtubule-targeting maytansinoids accumulate in cells and induce mitotic arrest at 250- to 1000-fold lower concentrations than those required for their association with tubulin or microtubules.

毒性学

Maytansine, an ansa macrolide isolated from African plants of the genera Maytenus and Putterlickia was first described almost two decades ago. It had been reported to be active against several forms of cancer, but a later phase II evaluation suggested no major role for this drug in tumor treatment. Although the toxic side effects were moderate, the antitumor activity was also not impressive.
Maytansine binds to tubulin rapidly and reversibly. Competitive inhibition of binding between maytansine and the vinca alkaloids has been observed, suggesting that maytansine must occupy at least one of vinblastine's binding sites on the tubulin molecule. The number of the maytansine binding sites is not known. Assembly of MT is inhibited at maytansine concentrations below 1μM. This suggests a substoichiometric poisoning mechanism as in the cases of colchicine, vinblastine and podophyllotoxin, but the details are not known. In contrast to many other MT-interacting toxins，maytansine does not promote the formation of aberrant tubulin polymers, even at millimolar concentrations. In fact, low concentrations of maytansine even inhibit vinblastine-induced formation of aberrant polymers.

参考文献

Walpert-Defillipes et al., Biochem. Pharmacol., 24, 751 (1975)

マイタンシン 上流と下流の製品情報

原材料

準備製品

マイタンシン 生産企業

名前	電話番号	電子メール	国籍	製品カタログ	優位度
BOC Sciences	16314854226; +16314854226	inquiry@bocsci.com	United States	19743	58
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32760	60
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
Hubei Ipure Biology Co., Ltd	+8613367258412	ada@ipurechemical.com	China	10326	58
Career Henan Chemica Co	+86-0371-86658258 +8613203830695	laboratory@coreychem.com	China	30253	58
Wuhan Monad Medicine Tech Co.,LTD	02768782018 18771942761	sales01@whmonad.com	CHINA	992	58
ANHUI WITOP BIOTECH CO., LTD	+8615255079626	eric@witopchemical.com	China	23556	58
Dorne Chemical Technology co. LTD	+86-86-13583358881 +8618560316533	Ethan@dornechem.com	China	3148	58
Alfa Chemistry	+1-5166625404	Info@alfa-chemistry.com	United States	21317	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58

35846-53-8(マイタンシン)キーワード:

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• 35846-53-8
• maitansine
• Maytansine
• NSC 153858
• (14S,16S,32S,33S,2R,4S,10E,12E,14R)-86-Chloro-14-hydroxy-85,14-dimethoxy-33,2,7,10-tetramethyl-12,6-dioxo-7-aza-1(6,4)-oxazinana-3(2,3)-oxirana-8(1,3)-benzenacyclotetradecaphane-10,12-dien-4-yl N-acetyl-N-methyl-L-alaninate
• Maitansina
• Microtubule/Tubulin,tumor,mitotic,microtubule-targeted,arrest,Inhibitor,potent,subnanomolar,Maytansine,inhibit
• メイタンシン
• マイタンシン
• (1S,2R,3S,5S,16Z,18Z,20R,21S)-11-クロロ-21-ヒドロキシ-12,20-ジメトキシ-2,5,9,16-テトラメチル-8,23-ジオキソ-4,24-ジオキサ-9,22-ジアザテトラシクロ[19.3.1.110,14.03,5]ヘキサコサ-10(26),11,13,16,18-ペンタエン-6-イル (2S)-2-(N-メチルアセトアミド)プロパノアート
• 抗腫瘍薬