Civorebrutinib
Civorebrutinib (WS-413) is a selective, orally active BTK and TEC inhibitor with an IC50 of <100 nM for both targets. Civorebrutinib inhibits B cell activation. Civorebrutinib significantly suppresses the in vivo growth of diffuse large B-cell lymphoma cells. Civorebrutinib can be used for the research of diffuse large B-cell lymphoma.
For research use only. We do not sell to patients.
- CAS No.: 2155853-43-1
- Formula: C23H22ClN7O2
- Molecular Weight:463.92
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
Civorebrutinib (1 h) exerts weak or no inhibitory effect on T cell activation, with an IC50 >4000 nM[1].
Civorebrutinib (30 min) inhibits the activation of B cells in whole blood, with an IC50 of <200 nM[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.
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Animal Model:NOD.SCID (immunocompromised, TMD-8 cells implanted subcutaneously)[1]
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Dosage:30 mg/kg; 25 mg/kg; 50 mg/kg
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Administration:p.o.; daily; 21 days; p.o.; twice daily; 21 days
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Result:Significantly suppressed the growth of TMD-8 tumors in vivo, with tumor volume substantially lower than the vehicle control and comparable to the positive control Ibrutinib at 30 mg/kg daily.
Showed potent tumor growth inhibition, with tumor volumes remaining at low levels similar to ibrutinib groups at 25 mg/kg twice daily and 50 mg/kg daily.
Chemical Information
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CAS No. 2155853-43-1
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Molecular Weight 463.92
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Formula C23H22ClN7O2
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SMILES
ClC(C=C1)=CN=C1OC2=CC=C(C3=NN([C@@H]4CCC5(CC5)N(C#N)C4)C(N)=C3C(N)=O)C=C2
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Synonyms
WS-413
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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)