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BMVC-8C3O is a G-quadruplex (G4) stabilizer.1 It increases the melting temperature of human telomeres by 45°C in a potassium solution. BMVC-8C3O binds to G4 structures at the EGFR promoter (Kd = 74.3 and 246.4 nM for QFS1 and QFS2, respectively), reduces EGFR protein levels, and inhibits the growth of several non-small cell lung cancer (NSCLC) cell lines, including those resistant to osimertinib (AZD 9291; Item No. 16237), in a concentration-dependent manner.2 In vivo, BMVC-8C3O (3 mg/kg) reduces tumor volume and weight in an H1975 NSCLC mouse xenograft model. It is also active against several strains of M. tuberculosis (MICs = 5.492-25 µg/ml) and inhibits M. tuberculosis polyketide synthase 13 (Pks13; IC50 = 6.94 µM), an enzyme involved in mycolic acid biosynthesis.3
WARNING This product is not for human or veterinary use.
1. Molecular engineering of G-
2. EGFR suppression contributes to growth inhibitory activity of G-
3. Identification of BMVC-