2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. BMS-986143

BMS-986143 是一种口服有效的、可逆的 BTK 抑制剂，IC50 为 0.26 nM。BMS-986143 还抑制 TEC、BLK、BMX、TXK FGR、YES1、ITK，IC50 分别为 3 nM、5 nM、7 nM、10 nM、15 nM、19 nM、21 nM。BMS-986143 可用于自身免疫性疾病的研究。

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BMS-986143 Chemical Structure

BMS-986143 Chemical Structure

CAS No. : 1643372-83-1

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BMS-986143 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

体外研究
(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].

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

BMS-986143 相关抗体:
体内研究
(In Vivo)

BMS-986143 demonstrates desirable efficacy in mouse models of collagen-induced arthritis (CIA) and anticollagen antibody-induced arthritis (CAIA)[1].
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].

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

Animal Model: DBA/1 male mice (8-10wk of age) bearing CIA model[1]
Dosage: 15 and 45 mg/kg
Administration: Oral gavage; BID
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).
分子量

587.45

Formula

C31H24Cl2N4O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BMS-986143 相关分类

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  • 稀释计算器

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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.

Keywords:

BMS-9861431643372-83-1BMS986143BMS 986143BtkBruton tyrosine kinaseatropisomerCD69autoimmune diseasereversible BTK inhibitorInhibitorinhibitorinhibit

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