|6-甲基-3-(2-(1-(吡啶-2-基)亚乙基)肼基)-5H-[1,2,4]三嗪环并[5,6-b]吲哚|CsnPharm

CAS No.: 327031-55-0

VLX600 Catalog No. CSN25874

VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation, potentiated the effect of radiation in tumor spheroids in a synergistic manner. VLX600 is preferentially active against quiescent cells in colon cancer 3-D microtissues. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation and displays tumour growth inhibition in vivo.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述VLX600 as a drug that is preferentially active against quiescent cells in colon cancer 3-D microtissues. VLX600 at 0.1 μM -10 μM inhibited the proliferation of HCT116, five additional human colon carcinoma cell lines and two mouse cell lines (T1 breast carcinoma; B16F10 melanoma) in monolayer culture over 72 h, which is associated with induction of autophagy. After exposure of monolayer cells to VLX600, the expression of COX-1, essential for mitochondrial OXPHOS decreased, which was also observed in multicellular spheroids (MCS) core regions. VLX600 induces a HIF-1α-dependent glycolytic response^[1]. In vitro, imatinib plus VLX600 at doses higher than 1μM decreased GIST-T1 (Gastrointestinal stromal tumor-T1) cell viability when compared to imatinib or VLX600 alone. In vivo, VLX600 (4.5mg/kg, IV q3–4 days) treatment alone resulted in a significant decrease in GIST-T1 tumor volume compared to vehicle controls^[2].
参考文献

[1] Zhang X, Fryknäs M, Hernlund E, et al. Induction of mitochondrial dysfunction as a strategy for targeting tumour cells in metabolically compromised microenvironments. Nat Commun. 2014;5:3295.
[2] Vitiello GA, Medina BD, Zeng S, et al. Mitochondrial Inhibition Augments the Efficacy of Imatinib by Resetting the Metabolic Phenotype of Gastrointestinal Stromal Tumor. Clin Cancer Res. 2018;24(4):972-984.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1511 mL
- 15.7556 mL
- 31.5112 mL
- 5 mM
- 0.6302 mL
- 3.1511 mL
- 6.3022 mL
- 10 mM
- 0.3151 mL
- 1.5756 mL
- 3.1511 mL

技术信息

CAS号

327031-55-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H15N7

运输

蓝冰

分子量

317.35

别名

溶解度

DMSO	13.0 mg/mL (41.0 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

VLX600 Catalog No. CSN25874

靶点选择性

请登录您的专属账户

确认信息