メイタンシノイド2

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H300：飲み込むと生命に危険

  H310：皮膚に接触すると生命に危険

  H314：重篤な皮膚の薬傷?眼の損傷

  H340：遺伝性疾患のおそれ

  H360：生殖能または胎児への悪影響のおそれ

  H370：臓器の障害

• 注意書き

  P260：粉じん/煙/ガス/ミスト/蒸気/スプレーを吸入しないこ と。

  P262：眼、皮膚、衣類につけないこと。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P301+P310：飲み込んだ場合：直ちに医師に連絡すること。

  P301+P330+P331：飲み込んだ場合：口をすすぐこと。無理に吐かせ ないこと。

  P302+P350：皮膚に付着した場合：多量の水と石鹸で優しく洗うこと。

  P303+P361+P353：皮膚（または髪）に付着した場合：直ちに汚染された衣 類をすべて脱ぐこと/取り除くこと。皮膚を流水/シャワー で洗うこと。

  P304+P340：吸入した場合：空気の新鮮な場所に移し、呼吸しやすい 姿勢で休息させること。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

  P307+P311：暴露した場合：医師に連絡すること。

  P310：ただちに医師に連絡すること。

  P321：特別な処置が必要である（このラベルの．．． を見よ）。

  P322：特別な処置が必要である（このラベルの．．． を見よ）。

  P330：口をすすぐこと。

  P361：汚染された衣類をすべて脱ぐこと。

  P363：汚染された衣類を再使用す場合には洗濯をすること。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

メイタンシノイド2 価格

メイタンシノイド2 化学特性,用途語,生産方法

• 説明

  Maytansine, a natural alkaloid, was first isolated from Maydens ovale in 1972 and exists in the genus Maydens of the family Weedaceae and its relatives. The mechanism of action of maytansine, acting on microtubules and tubulin, blocks the formation of spindles in the process of cell mitosis by inhibiting the depolymerization of cell microtubules, and has a strong ability to inhibit tumor cell proliferation.

• 化学的特性

  Mertansine is a white powder. It is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of mertansine in these solvents is approximately 0.25, 20, and 33 mg/ml, respectively.

• 使用

  Mertansine (DM1) is a microtubulin inhibitor which binds at the tips of microtubules and suppresses the dynamicity of microtubules.. Mertansine is an antibody-conjugatable maytansinoid that was developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. It can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC).

• 定義

  ChEBI: Mertansine is an organic heterotetracyclic compound and 19-membered macrocyclic lactam that is maytansine in which one of the hydrogens of the terminal N-acetyl group is replaced by a sulfanylmethyl group. It has a role as an antineoplastic agent and a tubulin modulator. It is an alpha-amino acid ester, a carbamate ester, an epoxide, an organic heterotetracyclic compound, an organochlorine compound, a thiol and a maytansinoid. It derives from a maytansine.

• 生物活性

  Mertansine is a thiol-containing derivative of maytansine that is cytotoxic to human epidermoid carcinoma KB and human breast cancer SK-BR-3 cells (IC50 = 1.10 nM for both). Formulations containing mertansine have been studied for the treatment of multiple myeloma and squamous cell carcinoma.

• 副作用

  Dose-limiting toxicity was observed at 2 mg/m2, and was manifested as profound weakness, diarrhea, nausea, and vomiting.

• 合成

  Mertansine synthesis steps: A solution of N 2'-deacetyl-N 2'- (3-methyldithio-1-oxopropyl)- maytansine (2b) (1.95 g, 2.5 mmol) in a mixture of ethyl acetate (140 mL) and methanol (210 mL) was stirred at room temperature under an argon atmosphere and treated with a solution of dithiothreitol (0.95 g, 6.2 mmol) in 0.05 M potassium phosphate buffer (140 mL) at pH 7.5 containing 2 mM ethylenediaminetetraacetic acid (EDTA). The progress of the reaction was monitored by HPLC and was complete in three hours. The reaction mixture was treated with a solution of 0.2 M potassium phosphate buffer (250 mL) at pH 6.0 containing 2 mM EDTA and then extracted with ethyl acetate (3 x 600 mL). The organic layers were combined, washed with brine (100 mL), and then dried over sodium sulfate. Evaporation of the solvent gave a residue of crude thiol-containing maytansinoid 25a. The crude residue was purified by HPLC using a preparative Diazem cyano HPLC column (250 mm x 50 mm, 10 micron particle size) that was equilibrated in a mixture of hexanes/2-propanol/ethyl acetate (78.0:5.5:16.5, v/v/v) and run at a flow rate of 150 mL/min. The desired product 25a eluted as a peak centered at 16 min. The fractions containing the product were evaporated to give mertansine as a white solid (76% yield).
  
  Fig The synthetic method 1 of Mertansine.

• Solubility in organics

  Mertansine is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF). The solubility of mertansine in these solvents is approximately 0.25, 20, and 33 mg/ml, respectively. Mertansine is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, Mertansine should first be dissolved in DMF and then diluted with the aqueous buffer of choice. Mertansine has a solubility of approximately 0.03 mg/ml in a 1:30 solution of DMF: PBS(pH 7.2)using this method.

• Mode of action

  Mertansine is a 19-member ansa macrolide structure attached to a chlorinated benzene ring. It was originally isolated from the shrub Maytenus ovatus. The antimitotic effect of maytansine has been attributed to its ability to inhibit microtubule assembly by binding to tubulin with a KD of ～1 μmol/L, at or near the vinblastine-binding site. Mertansine is effective in vivo against Lewis lung carcinoma and B16 murine melanocarcinoma solid tumors and has antileukemic activity against P388 murine lymphocytic leukemia.

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