PROTAC B-Raf degrader 1 (compound 2) 是基于Cereblon配体的一种B-RafPROTAC。有抗肿瘤活性。
生物活性 | PROTACB-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation ofB-Rafbased onCereblonligand with anti-cancer activity[1]. |
IC50& Target[1] | |
体外研究 (In Vitro) | The IC50values of PROTAC B-Raf degrader 1 (compound 2) towards MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM, respectively[1]. PROTAC B-Raf degrader 1 (5 or 10 μM) can accelerate the degradation of B-Raf by recruiting ubiquitin-proteasome system, and further affects the expression of Mcl-1, a downstream protein of B-Raf[1]. MCF-7 cells achieve an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation of PROTAC B-Raf degrader 1 with the concentration of 20 μM[1]. PROTAC B-Raf degrader 1 arrests cell cycle at the G2/M phase[1].
Cell Cytotoxicity Assay[1] Cell Line: | Human MCF-7 breast cancer cell line, MDA-MB-231 breast cancer cells, human HepG2 hepatoma cells, human normal LO2 liver cells, B16 cells. | Concentration: | 0-200 μM. | Incubation Time: | 72 hours. | Result: | The IC50values are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM in MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells, respectively. |
Western Blot Analysis[1] Cell Line: | Human MCF-7 breast cancer cell line. | Concentration: | 5 or 10 μM. | Incubation Time: | 24 hours. | Result: | Effectively induced the degradation of B-Raf and impacted the expression of Mcl-1. |
Apoptosis Analysis[1] Cell Line: | Human MCF-7 breast cancer cell line. | Concentration: | 2.7-20 μM. | Incubation Time: | 24 hours. | Result: | Achieved an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation with the concentration of 20 μM. |
Cell Cycle Analysis[1] Cell Line: | Human MCF-7 breast cancer cell line. | Concentration: | 20 μM. | Incubation Time: | 24 hours. | Result: | 1.94% cells were arrested at G1 phase, 8.20% at S phase, and 89.86% at G2/M phase. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
溶解性数据 | In Vitro: DMSO : 25 mg/mL(32.73 mM;Need ultrasonic) 配制储备液 1 mM | 1.3093 mL | 6.5465 mL | 13.0929 mL | 5 mM | 0.2619 mL | 1.3093 mL | 2.6186 mL | 10 mM | 0.1309 mL | 0.6546 mL | 1.3093 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℃, 6 months; -20℃, 1 month (stored under nitrogen)。-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 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 (3.27 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.27 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。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (3.27 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.27 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本网站选购。
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