BTK-IN-49
BTK-IN-49 is a selective, orally active and brain-penetrant BTK inhibitor with an IC50 of 0.14 nM. BTK-IN-49 binds to BTK and blocks B-cell receptor and Fcγ receptor signaling. BTK-IN-49 inhibits the proliferation of CNS-compartmentalized B-cells and FcγR-induced microglial proliferation in a BTK-dependent manner. BTK-IN-49 can be used for the study of multiple sclerosis.
For research use only. We do not sell to patients.
- Formula: C26H30N8O2
- Molecular Weight:486.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
BTK-IN-49 (compound 13) inhibits recombinant active BTK enzyme with an IC50 of 0.14 nM and suppresses CD69 expression on human CD19+ B-cells in whole blood with an IC50 of 0.23 μM[1].
BTK-IN-49 inhibits hERG channels with an IC50 of 25 μM, suggesting moderate cardiovascular risk[1].
BTK-IN-49 (1 μM) shows good kinome selectivity, inhibiting only BTK, KIT, and SRC by > 90% at 1 μM across a panel of 468 kinases[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BTK-IN-49 (5-50 mg/kg; p.o.; every 12 hours; 60 hours) robustly inhibits proliferation of CNS-compartmentalized B-cells in NOD.SCID mice, while peripherally restricted inhibitors show no activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 486.57
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Formula C26H30N8O2
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SMILES
CC(C)(C)C1=NC(C(N[C@H]2C3=CC=C(C4=CC=NC(NC5=NN(C)C=C5)=N4)C=C3CCCC2)=O)=NO1
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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)