XZ739
XZ739是一种基于CRBN的PROTACBCL-XL降解剂，作用于MOLT-4细胞，处理16小时后，DC50值为2.5nM。XZ739还通过caspase介导的凋亡(apoptosis)诱导细胞死亡。
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包装价格促销价数量
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5mg￥16562.0013250.00- +
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10mg￥27250.0021800.00- +
- 货号: ajcx31672
- CAS: 2365172-19-4
- 别名:
- 分子式: C65H76ClF3N8O12S3
- 分子量: 1349.99
- 纯度: ＞98%
- 溶解度: DMSO: 20 mg/mL (14.81 mM)
- 储存: -20°C, stored under nitrogen
- 库存: 现货
Background
XZ739, a CRBN-dependent PROTAC BCL-XL degrader with a DC50 value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediated apoptosis[1].
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
[1]. Xuan Zhang,et al. Discovery of PROTAC BCL-X L Degraders as Potent Anticancer Agents With Low On-Target Platelet Toxicity. Eur J Med Chem. 2020 Apr 15;192:112186.
