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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1643372-83-1
- 分子式: C31H24Cl2N4O4
- 分子量:587.45
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
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] |
体外実験
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.
体内実験
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).
化学情報
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CAS 番号 1643372-83-1
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分子量 587.45
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
BMS-986143 関連分類
HY-145373 関連分類
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