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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-TOPK-OTS964
OTS964

Chemical Structure : OTS964

CAS No.: 1338545-07-5

OTS964 (OTS964 hydrochloride, OTS-964)

货号: PC-43047Not For Human Use, Lab Use Only.

OTS964 is a dimethylated derivative of OTS514 and potent, selective TOPK inhibitor with IC50 of 28 nM, exhibits excellent in vivo efficacy with liposomal formulation.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

OTS964 is a dimethylated derivative of OTS514 and potent, selective TOPK inhibitor with IC50 of 28 nM, exhibits excellent in vivo efficacy with liposomal formulation.
OTS964 inhibits the growth of TOPK-positive cells with low IC50 values (A549 IC50=31 nM), decreases autophosphorylation of TOPK (Thr9), as well as phosphorylation of histone H3 (Ser10), in both T47D and LU-99 cells.
The liposomal OTS964 causes complete regression of tumors without any detectable toxicity in the xenograft models.
 

物理化学性质&存储条件

分子量 428.9748
分子式 C23H25ClN2O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Thieno[2,3-c]quinolin-4(5H)-one, 9-[4-[(1R)-2-(dimethylamino)-1-methylethyl]phenyl]-8-hydroxy-6-methyl-, hydrochloride (1:1)

参考文献

1. Matsuo Y, et al. Sci Transl Med. 2014 Oct 22;6(259):259ra145.

2. Ikeda Y, et al. Clin Cancer Res. 2016 Dec 15;22(24):6110-6117.

3. Pirovano G, et al. Br J Cancer. 2017 Aug 8;117(4):503-512.

4. Sugimori M, et al. Oncotarget. 2017 Dec 9;9(3):3043-3059.

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