VLX600

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Chemical Structure| 327031-55-0 同义名 : -
CAS号 : 327031-55-0
货号 : A1107952
分子式 : C17H15N7
纯度 : 95%
分子量 : 317.348
MDL号 : MFCD01305422
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(78.78 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.15mL

0.63mL

0.32mL

15.76mL

3.15mL

1.58mL

31.51mL

6.30mL

3.15mL
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.