1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. 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.

Civorebrutinib

Civorebrutinib Chemical Structure

CAS No. : 2155853-43-1

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Description

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[1].

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

Civorebrutinib (25-50 mg/kg; p.o.; once daily/twice daily; 21 days) exhibits potent in vivo anti-tumor activity against diffuse large B-cell lymphoma TMD-8 xenografts[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD.SCID (immunocompromised, TMD-8 cells implanted subcutaneously)[1]
Dosage: 30 mg/kg; 25 mg/kg; 50 mg/kg
Administration: p.o.; daily; 21 days; p.o.; twice daily; 21 days
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.
Molecular Weight

463.92

Formula

C23H22ClN7O2

CAS No.
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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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:
Civorebrutinib
Cat. No.:
HY-111781
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