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.
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- Fòrmula: C20H21Cl2N3O3
- Peso molecular:422.31
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Peso molecular 422.31
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TML-2Cl Related Classifications
HY-181679 Related Classifications
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