JB170

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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。

JB170  纯度: 98.40%

JB170 是一种强效且高度特异性的 PROTAC 介导的 AURORA-A 降解剂 (DC50=28 nM)，通过将 Alisertib 连接至 Cereblon配体 Thalidomide 而形成。JB170 优先结合 AURORA-A (EC50=193 nM) 而不是 AURORA-B (EC50=1.4µM)。JB170 介导的 S 期阻滞是由 AURORA-A 耗竭引起的。JB170 对 AURORA-A 激酶的非催化功能具有很好的抑制能力。

JB170

JB170 Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥8480 In-stock
5 mg ￥4800 In-stock
10 mg ￥8000 In-stock
25 mg ￥15500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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生物活性

JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase[1].

IC50 & Target[1]

Aurora A

28 nM (DC50)

Aurora A

99 nM (Kd)

Aurora A

193 nM (EC50)

Cereblon

 

体外研究
(In Vitro)

JB170 (1 μM; 24-72 hours; MV4-11 cells) mediates Aurora-A depletion inhibiting cancer cell survival[1].
JB170 (0.01-10 μM; 6 hours; MV4-11 cells) reduces AURORA-A levels [1].
JB170 (0.5 μM; 12 hours; MV4-11 cells) delays/arrests S-phase progression[1].
JB170 (0.5 μM; 0-72 hours; MV4-11 cells) induces apoptosis is exclusively caused by targeting AURORA-A[1].
JB170 (0.1 µM; 0-9 hours; IMR5 cells) shows rapid AURORA-A depletion. JB170 (0~1 μM; 6 hours; MV4-11 cells) strongly attenuates in mutants with respect to AURORA-A. JB170 (0.1 μM; 18 hours; MV4-11 cells) does not activate AURORA-A. JB170 (0~1 µM; 24 hours; IMR5 cells) largely abrogates AURORA-AT217D depletion. JB170 (1 μM; 4 days; IMR5 cells) mediates Aurora-A depletion inhibiting cancer cell survival. JB170 (IMR5 cells) reduces AURORA-A levels by lowering AURORA-A mRNA levels[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.

Cell Viability Assay[1]

Cell Line: MV4-11 cells
Concentration: 1 µM
Incubation Time: 24-72 hours
Result: After 72 hours, the number of viable cells was 32% of control levels.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.01~10 μM
Incubation Time: 6 hours
Result: Substantial degradation was observed at 100 nM and 1 µM.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.5 µM
Incubation Time: 0~72 hours
Result: Apoptosis was exclusively caused by targeting AURORA-A.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.5 µM
Incubation Time: 12 hours
Result: Delayed or arrested S-phase progression.

分子量

963.36

Formula

C48H44ClFN8O11
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 : 100 mg/mL (103.80 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0380 mL 5.1902 mL 10.3803 mL
5 mM 0.2076 mL 1.0380 mL 2.0761 mL
10 mM 0.1038 mL 0.5190 mL 1.0380 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% corn oil

    Solubility: ≥ 2.5 mg/mL (2.60 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.60 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]. Adhikari B, et al. PROTAC-mediated degradation reveals a non-catalytic function of AURORA-A kinase. Nat Chem Biol. 2020;16(11):1179-1188.

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