Product Name :
VLX600, Mitochondrial OXPHOS Inhibitor
Description:
VLX600 is a potent and selective mitochondrial OXPHOS inhibitor. It is preferentially active against quiescent cells in colon cancer 3-D microtissues (low micromole activity). 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. It induces the expression of genes associated with hypoxia, glycolysis, and p53 signaling, stimulates autophagy, and triggers mitochondrial dysfunction in MCs. It displays antitumor activity against colon cancer xenografts with minimal systemic toxicity in mice. Right now it is in phase I clinical trials for patients with refractory advanced solid tumors.
CAS:
327031-55-0
Molecular Weight:
317.35
Formula:
C17H15N7
Chemical Name:
2-[1-(2-{6-methyl-5H-[1,2,4]triazino[5,6-b]indol-3-yl}hydrazin-1-ylidene)ethyl]pyridine
Smiles :
CC(=NNC1N=C2NC3=C(C=CC=C3C)C2=NN=1)C1=CC=CC=N1
InChiKey:
UQOSBPRTQFFUOA-SRZZPIQSSA-N
InChi :
InChI=1S/C17H15N7/c1-10-6-5-7-12-14(10)19-16-15(12)22-24-17(20-16)23-21-11(2)13-8-3-4-9-18-13/h3-9H,1-2H3,(H2,19,20,23,24)/b21-11+
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
VLX600 is a potent and selective mitochondrial OXPHOS inhibitor. It is preferentially active against quiescent cells in colon cancer 3-D microtissues (low micromole activity). 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.{{Eprenetapopt} medchemexpress|{Eprenetapopt} Activator|{Eprenetapopt} Epigenetics|{Eprenetapopt} Technical Information|{Eprenetapopt} References|{Eprenetapopt} supplier} It induces the expression of genes associated with hypoxia, glycolysis, and p53 signaling, stimulates autophagy, and triggers mitochondrial dysfunction in MCs.{{Isosorbide mononitrate} web|{Isosorbide mononitrate} Autophagy|{Isosorbide mononitrate} Purity & Documentation|{Isosorbide mononitrate} In Vitro|{Isosorbide mononitrate} manufacturer|{Isosorbide mononitrate} Cancer} It displays antitumor activity against colon cancer xenografts with minimal systemic toxicity in mice.PMID:24324376 Right now it is in phase I clinical trials for patients with refractory advanced solid tumors.|Product information|CAS Number: 327031-55-0|Molecular Weight: 317.35|Formula: C17H15N7|Chemical Name: 2-[1-(2-{6-methyl-5H-[1,2,4]triazino[5,6-b]indol-3-yl}hydrazin-1-ylidene)ethyl]pyridine|Smiles: CC(=NNC1N=C2NC3=C(C=CC=C3C)C2=NN=1)C1=CC=CC=N1|InChiKey: UQOSBPRTQFFUOA-SRZZPIQSSA-N|InChi: InChI=1S/C17H15N7/c1-10-6-5-7-12-14(10)19-16-15(12)22-24-17(20-16)23-21-11(2)13-8-3-4-9-18-13/h3-9H,1-2H3,(H2,19,20,23,24)/b21-11+|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO up to 50 mM|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|VLX600 was used at 6 µM final concentration in various in vitro assays.|In Vivo:|VLX600 was dosed intravenously to mice at 16 mg/kg every third day for 16 days in xenografts models.|References:|Zhang X, et al. Induction of mitochondrial dysfunction as a strategy for targeting tumour cells in metabolically compromised microenvironments. (2014) Nat Commun. 5:3295.Products are for research use only. Not for human use.|Documents||