1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. 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.

Mal-Pip-ValCit-PAB-AZ7550

Mal-Pip-ValCit-PAB-AZ7550 Chemical Structure

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Description

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[1].

In Vitro

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.

In Vivo

Mal-Pip-ValCit-PAB-AZ7550 (83.7 mg/kg; i.v.; twice weekly for 2 weeks) exhibits potent in vivo anticancer activity in the H1650 non-small cell lung cancer xenograft model, delivers significant survival benefits, and results in a median survival time of 90 days[1].

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.
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

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Mal-Pip-ValCit-PAB-AZ7550
Cat. No.:
HY-181777
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