BTK inhibitor 13
BTK inhibitor 13 is an orally active Bruton's tyrosine kinase (BTK) inhibitor, with an IC50 value of 1.2 nM against human BTK. BTK inhibitor 13 covalently modifies the Cys481 residue of BTK when binding to the inactive conformation of BTK. BTK inhibitor 13 is used for the research of autoimmune diseases.
For research use only. We do not sell to patients.
- CAS No.: 2376726-26-8
- Formula: C29H26FN5O3
- Molecular Weight:511.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
BTK 1.2 nM (IC50) |
In Vitro
BTK inhibitor 13 exhibits potent inhibitory activity against human BTK kinase domain in a biochemical enzyme inhibition assay, achieving a mean IC50 of 1.2 nM[1].
BTK inhibitor 13 exhibits low intrinsic clearance in both rat and human liver microsomes in the in vitro metabolic stability assay[1].
BTK inhibitor 13 (Compound 8) demonstrates strong functional cellular potency in human whole blood against anti-IgM/IL-4 stimulated B cell CD69 upregulation, with a mean IC50 of 16 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:Female rat[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Reached 44% BTK occupancy in spleen homogenates at 5 hours post-administration.
Measured corresponding blood concentration of 1.5 nM at 5 hours post-administration.
Chemical Information
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CAS No. 2376726-26-8
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Molecular Weight 511.55
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Formula C29H26FN5O3
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SMILES
O=C(NC1=CC(F)=CC(C2=C3C(NC=C3C(CN(C)C(C=C)=O)=O)=NC=N2)=C1C)C4=CC=C(C5CC5)C=C4
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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)
BTK inhibitor 13 Related Classifications
HY-130255 Related Classifications
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