KT-333 diammonium

CAS: 2502186-80-1 F: C60H80ClN12O14PS W: 1291.84

KT-333 diammonium is a molecular glues that degrades STAT3 protein. KT-333 diammonium mediates the selective degradation

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Bioactivity	KT-333 diammonium is a molecular glues that degrades STAT3 protein. KT-333 diammonium 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 diammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 diammonium 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].
Invitro	KT-333 ammonium (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 ammonium 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. 0 --> KT-333 diammonium 相关抗体:
In Vivo	KT-333 diammonium (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 diammonium (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.
CAS	2502186-80-1
Formula	C60H80ClN12O14PS
Molar Mass	1291.84
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

Volanesorsen sodium