Mal-Pip-ValCit-PAB-AZ7550
Mal-Pip-ValCit-PAB-AZ7550 is a prodrug of EGFR inhibitor. Mal-Pip-ValCit-PAB-AZ7550 selectively binds covalently to albumin via its maleimide moiety. Mal-Pip-ValCit-PAB-AZ7550 exhibits potent in vivo anticancer activity in non-small cell lung cancer xenograft models. Mal-Pip-ValCit-PAB-AZ7550 can be used in research related to non-small cell lung cancer.
For research use only. We do not sell to patients.
- Formula: C61H79N15O11
- Molecular Weight:1198.37
-
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]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All EGFR Isoforms
More
Biological Activity
Mal-Pip-ValCit-PAB-AZ7550 (Mal-Pip-ValCit) (46 μM; 1.5 h (cleavage without albumin), 3.5 h (pre-incubation with HSA) + 4 h (cleavage)) is efficiently cleaved by cathepsin B to release OsiNHMe, and this cleavage process remains equally efficient when Mal-Pip-ValCit is pre-bound to human serum albumin[1].
Mal-Pip-ValCit-PAB-AZ7550 (50 μM; 10 min (binding), ~10 min (NAC pre-incubation)) rapidly forms covalent bonds with human serum albumin via its maleimide group, achieving a binding rate of over 95% within 10 min at 37 °C[1].
Mal-Pip-ValCit-PAB-AZ7550 (0.25-1.5 equivalents relative to Cys34 thiol; 20 min) binds to the Cys34 thiol residue of human serum albumin; after incubation at 37 °C for 20 min, the binding rate reaches 53% when the ratio of the compound to Cys34 is 1:1[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.
-
Animal Model:C.B.17SCID/SCID (8−16 weeks old)[1]
-
Dosage:83.7 mg/kg
-
Administration:i.v.; twice per week; 2 weeks
-
Result:Achieved significant tumor growth inhibition more effective than non-cleavable Mal-Pip-GlyGly control and osimertinib alone.
Provided a significant survival benefit with average survival of 90 days (some animals surviving up to 122 days) compared to control, Mal-Pip-GlyGly, and osimertinib groups.
Caused no significant weight loss or systemic toxicity.
Chemical Information
-
Molecular Weight 1198.37
-
Formula C61H79N15O11
-
SMILES
O=C(OCC1=CC=C(NC([C@@H](NC([C@@H](NC(CCN2CCN(CCOCCN3C(C=CC3=O)=O)CC2)=O)C(C)C)=O)CCCNC(N)=O)=O)C=C1)N(CCN(C4=CC(OC)=C(NC5=NC=CC(C6=CN(C)C7=C6C=CC=C7)=N5)C=C4NC(C=C)=O)C)C
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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-Pip-ValCit-PAB-AZ7550 Related Classifications
HY-181777 Related Classifications
Powered by Bioz