BMS-986143
BMS-986143 is an orally active, reversible BTK inhibitor with an IC50 of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases.
For research use only. We do not sell to patients.
- CAS No.: 1643372-83-1
- Formula: C31H24Cl2N4O4
- Molecular Weight:587.45
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B cell | IC50 |
1 nM
Compound: 6d; BMS-986143
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Antiproliferative activity against anti-IgM/IgG-induced human peripheral B cells
Antiproliferative activity against anti-IgM/IgG-induced human peripheral B cells
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[PMID: 33214829] |
In Vitro
BMS-986143 inhibits BTK with IC50s of 6.9±3.4 and 25±19 nM in Ramos cellular assay and the human whole blood assay, respectively[1].
BMS-986143 provides potent inhibition of end points derived from IgG-containing immune complex low affinity activating Fcγ receptor signaling in peripheral blood mononuclear cells (PBMC) (IC50=2 nM)[1].
BMS-986143 inhibits the expression of CD63 on the surface of basophils in human whole blood, driven by FcεRI signaling (IC50 of 54 nM)[1].
BMS-986143 inhibits calcium flux in Ramos B Cells, proliferation of human peripheral B Cells, CD86 surface expression in peripheral B Cells, and TNFα from human PBMC Cells with IC50s of 7±3, 1±0.4, 1±0.5, and 2 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
BMS-986143 exhibits high oral bioavailability (mouse 100%, dog 82%) and moderate Cmax (mouse 4.3, dog 1.2 μM) following oral administration (mouse 6, dog 2 mg/kg)[1].
BMS-986143 exhibits long elimination half-lives (mouse 3.6, dog 7.9 h) due to moderate plasma clearance (8.6, 4.4 mL/min/kg respectively) combined with low volumes of distribution (1.8, 2.6 L/kg respectively) following intravenous administration (mouse 3.0, dog 1.0 mg/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DBA/1 male mice (8-10wk of age) bearing CIA model[1]
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Dosage:15 and 45 mg/kg
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Administration:Oral gavage; BID
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Result:15 and 45 mg/kg provided dose-dependent inhibition of observed clinical disease progression (63% and 80%, respectively), representing 17 and 19 h coverage of the mouse whole blood IC50 (130 nM).
Chemical Information
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CAS No. 1643372-83-1
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Molecular Weight 587.45
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Formula C31H24Cl2N4O4
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SMILES
CC1=C(C=CC=[C@@]1[C@@]2=C(C=C(C3=C2C4=C(N3)C=C(C=C4)C(C)(O)C)C(N)=O)Cl)N5C(C=C6C(Cl)=CC=CN6C5=O)=O
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BMS-986143 Related Classifications
HY-145373 Related Classifications
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