VLX600

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

VLX600 是一种铁螯合氧化磷酸化 (OXPHOS) 抑制剂，是一种细胞渗透性抗癌剂。

VLX600 is an iron-chelating oxidative phosphorylation (OXPHOS) inhibitor, is a cell-permeable anticancer agent.?It acts by reducing mitochondrial oxidative phosphorylation in tumor cells.VLX600 as a drug that is preferentially active against quiescent cells in colon cancer 3-D microtissues.?The anticancer activity is associated with reduced mitochondrial respiration, leading to bioenergetic catastrophe and tumour cell death.?VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation.?Importantly, VLX600 displays tumour growth inhibition in vivo.?(In Vivo):VLX600 (16?mg/kg; i.v.; every third day for 16 days) shows anti-tumor activity in human tumor xenografts.

VLX600 (6?μM; 72 hours) induces an autophagic response.VLX600 is cytotoxic to HCT116 spheroids. VLX600 induces a HIF-1α-dependent glycolytic response. VLX600 inhibits oxygen consumption in HCT116 cells. VLX600 inhibits phosphorylation of the mTOR downstream effectors 4EBP1 and p70-S6K by an HIF-1α-independent mechanism. VLX600 preferentially leads to decreased ATP levels in cancer but not normal cells.Cell Proliferation Assay Cell Line:HCT116, HT29, SW620, HT8, DLD and RKO cells Concentration:0.1, 1, 10, 100μM Incubation Time:72 hours Result:Inhibited the proliferation of these cells.Western Blot Analysis Cell Line:HCT116 cells Concentration:6?μM Incubation Time:72?hoursResult:LC3-II was induced.

VLX600 (16?mg/kg; i.v.; every third day for 16 days) shows anti-tumor activity in human tumor xenografts. Animal Model:NMRI nu/nu mice (HCT116 and HT29 colon cancer xenografts)Dosage:16?mg/kg Administration:Intravenously; every third day for 16 days Result:Anti-tumor activity was observed in both HCT116 and HT29 colon cancer xenografts.

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Others

Other Targets

oxidative phosphorylation (OXPHOS)

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327031-55-0

317.35

C17H15N7

>98% (HPLC)

DMSO:8 mg/ml(25.21 mM)

C\C(=N/Nc1nnc2c(n1)[nH]c1c(C)cccc21)c1ccccn1

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(-20℃)

With Ice Pack

≥ 2 years