XZ739 |
| カタログ番号GC61384 |
XZ739、Cereblon 依存性 PROTAC BCL-XL (Bcl-2 ファミリーメンバー) 分解剤で、16 時間処理後の MOLT-4 細胞で 2.5 nM の DC50 値を示します。 XZ739 はまた、カスパーゼを介したアポトーシスを介して細胞死を誘導します。
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Cas No.: 2365172-19-4
Sample solution is provided at 25 µL, 10mM.
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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.
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