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。
| 生物活性 | JB170 is a potent and highly specificPROTAC-mediatedAURORA-A(Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to theCereblon-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 |
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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-AT217Ddepletion. 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].
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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(103.80 mM;Need ultrasonic) 配制储备液 | 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 |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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
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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。
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