Mal-PEG4-Val-Ala-Ph-2,2-dimethylpropanoic acid
Mal-PEG4-Val-Ala-Ph-2,2-dimethylpropanoic acid is a maleimide-functionalized PEG4-Val-Ala dipeptide linker bearing a trimethyl-locked adapter for exatecan conjugation, which enables thiol conjugation via the maleimide group and facilitates payload release. Mal-PEG4-Val-Ala-Ph-2,2-dimethylpropanoic acid is used in cancer research.
For research use only. We do not sell to patients.
- Formula: C37H55N5O12
- Molecular Weight:761.86
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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
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-N87 | IC50 |
48.49 nM
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Antiproliferative activity against human HER2-positive NCI-N87 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against human HER2-positive NCI-N87 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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42218895 |
In Vitro
Mal-PEG4-Val-Ala-Ph-2,2-dimethylpropanoic acid is the linker-payload structure of the ADC drug Her2-W1507. Under the indicated concentration conditions for 72 h, the intact molecule Her2-W1507 exhibits potent HER2-dependent antiproliferative activity against NCI-N87, SK-BR-3, and SK-OV-3 cell lines, with an IC50 of 48.49 nM in NCI-N87 cells[1].
Mal‑PEG4‑Val‑Ala‑Ph‑2,2‑dimethylpropanoic acid is a component of the linker‑payload W1507. When tested at 5 mM for 1 h, the linker‑payload W1507 remains stable in the presence of cathepsin B, with no detectable release of exatecan (HY‑13631)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-N87, SK-BR-3, SK-OV-3, MDA-MB-231
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Concentration:indicated concentrations (Her2-W1507)
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Incubation Time:72 h
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Result:Demonstrated potent inhibitory effects against NCI-N87 with an IC50 value of 48.49 nM.
Exhibited comparable antiproliferative efficacy against HER2-positive SK-OV-3 and SK-BR-3 cell lines.
Exhibited considerably weaker antiproliferative activity against HER2-low-expressing MDA-MB-231 cell line.
Chemical Information
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Molecular Weight 761.86
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Formula C37H55N5O12
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SMILES
O=C(N[C@@H](C(C)C)C(N[C@@H](C)C(NC1=CC=CC=C1CC(C)(C)C(O)=O)=O)=O)CCOCCOCCOCCOCCNC(CCN2C(C=CC2=O)=O)=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)
Mal-PEG4-Val-Ala-Ph-2,2-dimethylpropanoic acid Related Classifications
HY-184906 Related Classifications
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Keywords
- Mal-PEG4-Val-Ala-Ph-2,2-dimethylpropanoic acid
- Drug-Linker Conjugates for ADC
- cancer
- SK-BR-3
- maleimide-functionalized PEG4-Val-Ala dipeptide linker
- cathepsin B
- NCI-N87
- thiol conjugation
- payload release
- trimethyl lock adapter
- HER2-dependent antiproliferative activity
- exatecan conjugation
- Inhibitor
- inhibitor
- inhibit