bs-60261C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 317.35

Formula: C17 H15 N7

CAS Number: 327031-55-0

InChi Key: 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+

Smiles: CC(=NNC1N=NC2=C(NC3=C2C=CC=C3C)N=1)C1C=CC=CN=1

Purity: 98.0

Solubility: DMSO up to 50 mM

Appearance: Solid Power.

Shelf Life: 1.0 years

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.