Branebrutinib BMS-986195|cas:1912445-55-6|西域试剂

Branebrutinib BMS-986195,99.82%

产品编号：Bellancom-112161| CAS NO：1912445-55-6| 分子式：C₂₀H₂₃FN₄O₂| 分子量：370.42

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货号	价格	库存与货期
Bellancom-112161	￥2200.00	杭州北京（现货）
Bellancom-112161	￥3500.00	杭州北京（现货）
Bellancom-112161	￥9500.00	杭州北京（现货）
Bellancom-112161	￥0.00	杭州北京（现货）
Bellancom-112161	￥0.00	杭州北京（现货）

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Branebrutinib BMS-986195

产品介绍

Branebrutinib (BMS-986195) 是一个强有效的、布鲁顿氏酪氨酸激酶 (BTK) 的不可逆共价、选择抑制剂，其 IC₅₀ 值 0.1 nM。

生物活性

Branebrutinib (BMS-986195) is a highly potent, selective covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), with an IC₅₀ of 0.1 nM.

体外研究

BMS-986195 is a potent and highly selective inhibitor of BTK, which acts by covalently modifying an active-site cysteine residue. BMS-986195 is more than 5000-fold selective for BTK over all kinases outside of the Tec family, and selectivity ranges from 9- to 1010-fold within the Tec family. BMS-986195 inactivates BTK in human whole blood with a rapid rate of inactivation (3.5×10^-4nM^-1•min^-1) and potently inhibits antigen-dependent interleukin-6 production, CD86 expression and proliferation in B cells (IC₅₀<1 nM) without effect on antigen-independent measures in the same cells. A similar potency is measured against FcγR-dependent TNF-α production in human cells.

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

体内研究

In mice, BMS-986195 demonstrates robust efficacy in murine models of RA including CIA and CAIA, protecting against clinically evident disease, histologic joint damage and bone mineral density loss. In both mice and monkeys, maximal efficacy is observed at doses ≤0.5 mg/kg PO QD, which achieves ≥95% inactivation of BTK in vivo. At similar doses, BMS-986195 is also highly protective against nephritis in the NZB/W mouse model of lupus. To investigate the dynamics of BTK inactivation and resynthesis of BTK, cynomolgus monkeys are given single or multiple doses of BMS-986195. 100% peak inactivation of BTK is obtained with a single administration of BMS-986195 at 0.5 mg/kg PO.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 150 mg/mL (404.95 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6996 mL	13.4982 mL	26.9964 mL
5 mM	0.5399 mL	2.6996 mL	5.3993 mL
10 mM	0.2700 mL	1.3498 mL	2.6996 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 3.75 mg/mL (10.12 mM); Clear solution

此方案可获得 ≥ 3.75 mg/mL (10.12 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 37.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 3.75 mg/mL (10.12 mM); Clear solution

此方案可获得 ≥ 3.75 mg/mL (10.12 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 37.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明