Src Inhibitor 1(Synonyms: Src Kinase Inhibitor 1; Src-l1)

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。

Src Inhibitor 1 (Synonyms: Src Kinase Inhibitor 1; Src-l1) 纯度: 99.98%

Src Inhibitor 1是高效选择性的,ATP-竞争性的双位点Src酪氨酸激酶抑制剂,对Src和Lck的IC50值分别为44 nM和88 nM。

Src Inhibitor 1(Synonyms: Src Kinase Inhibitor 1;  Src-l1)

Src Inhibitor 1 Chemical Structure

CAS No. : 179248-59-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥575 In-stock
2 mg ¥500 In-stock
5 mg ¥700 In-stock
10 mg ¥950 In-stock
25 mg ¥2200 In-stock
50 mg ¥3950 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Src Inhibitor 1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library

生物活性

Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.

IC50 & Target

IC50: 44 nM (Src), 88 nM (Lck)[1]

体外研究
(In Vitro)

Src-I1 is competitive with both ATP and peptide binding sites of the kinase. The IC50 values are 44 and 88 nM for Src and Lck, respectively[1]. Src-I1, is found to be a potent inhibitor of Src (IC50=0.18 μM), but also inhibited other Src family members, such as Lck, Csk and Yes with similar potency to Src, and RIP2 (IC50=0.026 μM) with even greater potency. In addition, it inhibited CHK2 with similar potency to Src, and Aurora B with slightly lower potency[2].

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

373.40

Formula

C22H19N3O3

CAS 号

179248-59-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -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 : 9.09 mg/mL (24.34 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6781 mL 13.3905 mL 26.7809 mL
5 mM 0.5356 mL 2.6781 mL 5.3562 mL
10 mM 0.2678 mL 1.3390 mL 2.6781 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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.91 mg/mL (2.44 mM); Clear solution

    此方案可获得 ≥ 0.91 mg/mL (2.44 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 9.1 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
  • 2.

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

    Solubility: ≥ 0.91 mg/mL (2.44 mM); Clear solution

    此方案可获得 ≥ 0.91 mg/mL (2.44 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 9.1 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]. Tian G, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91.

    [2]. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.

Kinase Assay
[2]

Assays (25.5 μL volume) are carried out robotically at room temperature (21°C) and are linear with respect to time and enzyme concentration under the conditions used. Assays are performed for 30 min using Multidrop Micro reagent dispensers in a 96-well format. The concentration of magnesium acetate in the assays is 10 mM and [γ-33P]ATP (800 c.p.m./pmol) is used at 5, 20 or 50 μM as indicated, in order to be at or below the Kmfor ATP for each enzyme.The assays are initiated with MgATP, stopped by the addition of 5 μL of 0.5 M orthophosphoric acid and spotted on to P81 filter plates using a unifilter harvester. The IC50 values of inhibitors are determined after carrying out assays at ten different concentrations of each compound[2].

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]. Tian G, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91.

    [2]. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务