生物活性分子抑制剂Ibrutinib-biotin(Synonyms: 依鲁替尼-生物素)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域
Ibrutinib-biotin (Synonyms: 依鲁替尼-生物素) 纯度: 98.18%

Ibrutinib-biotin 是一种由 Ibrutinib 通过长链接头连接到生物素上组成的探针,具体可参考 WO2014059368A1 中 Compound 1-5,抑制 BTKIC50 值为 0.755-1.02 nM。

Ibrutinib-biotin(Synonyms: 依鲁替尼-生物素)

Ibrutinib-biotin Chemical Structure

CAS No. : 1599432-18-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥13278 In-stock
5 mg ¥7500 In-stock
10 mg ¥11000 In-stock
50 mg ¥40000 In-stock
100 mg   询价  
200 mg   询价  

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Ibrutinib-biotin 相关产品

相关化合物库:

  • Bioactive Compound Library Plus

生物活性

Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, extracted from patent WO2014059368A1 Compound 1-5, has an IC50 of 0.755-1.02 nM for BTK.

IC50 & Target

IC50: 0.755-1.02 nM (BTK), 1.71-2.29 nM (TEC), 3.66-4.27 nM (BLK), 4.42-5.57 nM (BMX), 5.99-6.92 nM (LCK), 33.8-36.3 nM (Src), 0.187-0.198 μM (ITK),5.34-4.87 μM (JAK3)[1]

体外研究
(In Vitro)

Ibrutinib-biotin (Compound 1-5) is a probe that consists of Ibrutinib linked to biotin via a long chain linker. Ibrutinib is a TEC family kinase inhibitor. The TEC kinase family is composed of five members, TEC, BTK (Bruton’s Tyrosine Kinase), ITK (interleukin-2-inducible T-cell kinase)/EMT/TSK, BMX and TXK/RLK. The TEC family kinases participate in phosphotyrosine- mediated and phospholipid-mediated signaling systems. Many TEC family proteins are abundantly expressed in hematopoietic tissues, and play important roles in the growth and differentiation processes of blood cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

1097.37

Formula

C56H80N12O9S

CAS 号

1599432-18-4

中文名称

依鲁替尼-生物素

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (45.56 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9113 mL 4.5563 mL 9.1127 mL
5 mM 0.1823 mL 0.9113 mL 1.8225 mL
10 mM 0.0911 mL 0.4556 mL 0.9113 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: ≥ 2.5 mg/mL (2.28 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.28 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (2.28 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.28 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (2.28 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.28 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Betty Y. CHANG, et al. Companion diagnostics for tec family kinase inhibitor therapy. WO 2014059368 A1.

Kinase Assay
[1]

In this study, assay formats are tested for sensitivity, specificity, range, and to determine most suitable anti BTK Antibody. An aliquot of DOHH2 cell lysate (1 mg/mL) is inhibited with 1 μM Ibrutinib then labeled with probe (1 μM). Negative controls: Untreated DOHH2 and Jurkat cell lysates (l mg/mL) are labeled with probe (1 μM) and Untreated DOHH2 cell lysate. Standard Streptavidin plate (5-pack); Read Buffer T (50 mL), SULFO TAG Goat Anti-mouse (50 μg); SULFO TAG Goat Anti-rabbit (50 μg); SULFO TAG streptavidin (50 ug); MSD Standard Plates; MSD Blocker A; Protease inhibitor cocktail; Positive Control lysates from BTK expressing cell line (DOHH2); Negative Control lysates; Ibrutinib (PCI); probe compound 1-5 (biotinylated probe).

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Betty Y. CHANG, et al. Companion diagnostics for tec family kinase inhibitor therapy. WO 2014059368 A1.

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