PROTAC AR Degrader-4 包含IAP配体结合基团,linker 和雄激素受体 (AR) 配体结合基团。基于 cIAP1 的降解剂也被称为SNIPER。
生物活性 | PROTACAR Degrader-4 comprises aIAPligand binding group, a linker and anAndrogen Receptor(AR) binding group.PROTACAR Degrader-4 is anARdegrader. Degradation inducers based oncIAP1are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1]. |
IC50& Target[1] | |
体外研究 (In Vitro) | Specific and Nongenetic IAPs-dependent Protein Erasers (SNIPERs) are bifunctional compounds which are designed by conjugating an IAPs-recognition structure with a target protein-recognition structure. Targeting proteins for degradation involves three steps. 1, its two recognition structures allow SNIPER to form a complex linking IAPs, which have E3 ligase activity, with the target protein. 2, the target protein is polyubiquitinated by IAPs. 3, the polyubiquitinated protein is degraded by proteasome.
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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 : 200 mg/mL(226.24 mM;Need ultrasonic) 配制储备液 1 mM | 1.1312 mL | 5.6559 mL | 11.3118 mL | 5 mM | 0.2262 mL | 1.1312 mL | 2.2624 mL | 10 mM | 0.1131 mL | 0.5656 mL | 1.1312 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: ≥ 5 mg/mL (5.66 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (5.66 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 50.0 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% (20%SBE-β-CDin saline) Solubility: 5 mg/mL (5.66 mM); Suspended solution; Need ultrasonic
此方案可获得 5 mg/mL (5.66 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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