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.
For research use only. We do not sell to patients.
- Formula: C20H21Cl2N3O3
- Molecular Weight:422.31
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
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. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 422.31
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TML-2Cl Related Classifications
HY-181679 Related Classifications
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