Zecdarasib
Zecdarasib is an orally active Kirsten rat sarcoma virus oncogene homolog (KRAS) inhibitor with antitumor activity. Zecdarasib can be used in tumor-related research.
For research use only. We do not sell to patients.
- CAS No.: 3080960-85-3
- Formula: C35H32Cl2FN5O
- Molecular Weight:628.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
K-RAS |
In Vitro
Zecdarasib (INCB161734) induces S-phase inhibition in G12D HPAC cells with an IC50 of 12.8 nM[2].
Zecdarasib induces caspase 3/7 cleavage in G12D HPAC cells, EC50 < 100 nM[2].
Zecdarasib (INCB161734) binds both the GDP and GTP forms of G12D with picomolar KD values[2].
Zecdarasib potently inhibits SOS1-dependent GDP/GTP exchange with an IC50 < 3 nM[2].
Zecdarasib inhibits the KRAS downstream ERK signaling pathway in G12D mutant cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Zecdarasib (oral) produces sustained near-maximal KRAS inhibition in G12D HPAC mouse xenograft tumors, persisting for nearly the entire dosing interval[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3080960-85-3
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Molecular Weight 628.57
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Formula C35H32Cl2FN5O
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SMILES
N#CCCC1=CC2=C(N=C(C3=C2N(C([C@@]4(N(C(C5CC5)=O)[C@@]6(C[C@@]6(C4)[H])[H])[H])=C3)[C@]7([C@]8(CN[C@@]7(C8)[H])[H])[H])C)C(F)=[C@]1[C@]9=C(Cl)C(Cl)=CC=C9
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Synonyms
INCB161734
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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)