XZ739 是一种基于Cereblon的 PROTACBCL-XL(Bcl-2家族成员) 降解剂，作用于 MOLT-4 细胞，处理 16 小时后，DC50值为 2.5 nM。XZ739 还通过 caspase 介导的凋亡 (apoptosis) 诱导细胞死亡。
| 生物活性 | XZ739, aCereblon-dependentPROTACBCL-XL(Bcl-2family member) degrader with aDC50value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediatedapoptosis[1]. |
| IC50& Target[1] | Bcl-xL 2.5 nM (DC50) | Cereblon |
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体外研究
(In Vitro) | XZ739 (0.001-10 μM; 48 hours) potently reduces the viability of T-ALL MOLT-4, B-ALL RS4; 11, SCLC NCI-H146 cells, and platelets after 48 h treatment with IC50s of 10.1, 41.8, 25.3, and 1217 nM, respectively. XZ739 has >100-fold selectivity for MOLT-4 cells over human platelets[1].
XZ739 (1.2-300 nM; 16 hours) induces BCL-XL degradation in MOLT-4 cells[1].
The BCL-XL degradation induced by XZ739 in MOLT-4 is rapid, starting within 2 h; and 8 h after XZ739 treatment, more than 96% of the BCL-XL is degraded with 100 nM of XZ739[1].
Cell Viability Assay[1] | Cell Line: | Human platelets and MOLT-4 cells | | Concentration: | 0.001, 0.01, 0.1, 1, and 10 μM | | Incubation Time: | 48 hours | | Result: | IC50values were 10.1 nM and 1217 nM for MOLT-4 cells and platelets, respectively. |
Western Blot Analysis[1] | Cell Line: | MOLT-4 cells | | Concentration: | 1.2, 3.7, 11, 33, 100, 300 nM | | Incubation Time: | 16 hours | | Result: | Dose-dependently induced BCL-XL degradation. |
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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 : 20 mg/mL(14.81 mM;Need ultrasonic) 配制储备液 | 1 mM | 0.7407 mL | 3.7037 mL | 7.4075 mL | | 5 mM | 0.1481 mL | 0.7407 mL | 1.4815 mL | | 10 mM | 0.0741 mL | 0.3704 mL | 0.7407 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 mg/mL (1.48 mM); Suspended solution; Need ultrasonic
此方案可获得 2 mg/mL (1.48 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 20.0 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。 *以上所有助溶剂都可在本网站选购。
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