TML-2Cl
TML-2Cl is a dichloro-modified trimethyl lock adapter for antibody-drug conjugates and payload releaser.TML-2Cl undergoes 1,6-elimination followed by rapid self-cyclization to facilitate release of the payload Exatecan after cathepsin B cleavage of the associated linker.TML-2Cl exhibits high stability when conjugated to a drug and high intrinsic hydrophobicity.TML-2Cl can be used for the research of gastric carcinoma.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C20H21Cl2N3O3
- 分子量:422.31
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
TML-2Cl (1 h) enables efficient Exatecan release via 1,6-elimination and self-cyclization following reduction in a cell-free system[1].
TML-2Cl-containing linker-payloads with Val-Ala cleavage sites (LP03, L10081, L10082) (4-20 h) exhibit higher cathepsin B-mediated Exatecan release efficiency than those with GGFG cleavage sites; L10081 and L10082 achieve near-complete payload release within 4 h in vitro[1].
TML-2Cl-containing ADCs Her2-L10081 and Her2-L10082 (72 h) exhibit potent, HER2-dependent antiproliferative activity in vitro, with IC50 values ranging from 108.09 nM to 287.40 nM in HER2-positive cell lines and weak activity in HER2-negative MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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分子量 422.31
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分子式 C20H21Cl2N3O3
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SMILES
OC(CC(C)(C)C1=C(C)C(Cl)=C(C)C(Cl)=C1OCC2=CC=C(N=[N+]=[N-])C=C2)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)