KT-333 

KT-333 is a molecular glues that degrades STAT3 protein. KT-333 mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL)^[1].

KT-333 (11.8±2.3 nM，48 h) 对 STAT3 降解后使得 SU-DHL-1 细胞系产生了不可逆的生长抑制并诱导了半胱天冬酶 3/7 的活性，这是细胞凋亡的标志^[1]。
KT-333 显示出了对 STAT3 蛋白的降解作用，并且在细胞表型分析中，对多个 ALCL 细胞系的 GI₅₀ 值范围为 8.1 到 57.4 nM^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

KT-333 ammonium (5，10，15 和 45 mg/kg，iv.；一周一次持续两周) 显示出剂量依赖性的抗肿瘤活性。以 5 mg/kg 给药的小鼠实现了 79.9% 的肿瘤生长抑制 (TGI)，而以10，15 或 45 mg/kg 给药的小鼠实现了完全的肿瘤消退，这些效果一直持续到研究结束^[1]。
KT-333 ammonium (10，20 和 30 mg/kg，iv.；一周一次持续两周) 显示出剂量依赖性的抗肿瘤活性。以 10 mg/kg 给药的小鼠实现了 83.8% 的肿瘤生长抑制 (TGI)，而以 20 或 30 mg/kg 给药的小鼠实现了完全的肿瘤消退，这些效果一直持续到研究结束^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1257.78

C₆₀H₇₄ClN₁₀O₁₄PS

2502186-79-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ding X, et al. Antitumor effect of the novel sphingosine kinase 2 inhibitor ABC294640 is enhanced by inhibition of autophagy and by sorafenib in human cholangiocarcinoma cells. Oncotarget. 2016 Apr 12;7(15):20080-92.  [Content Brief]