GJG057 is a LTC4S inhibitor. GJG057 exhibits potent cytotoxic effects against various human cancer cell lines, including SGC-7901, HGC-27, and MCF-7, with IC₅₀ values of 20.5 ± 5.93 μM, 3.3 ± 2.53 μM, and 16.6 ± 0.75 μM, respectively. Notably, GJG057 shows high selectivity towards cancer cells over normal cells. Mechanistic investigations revealed that GJG057 induces apoptosis in a concentration-dependent manner and downregulates the expression of HIF-1α, VEGF, and PKM2, leading to decreased lactate production. Furthermore, GJG057 effectively inhibits tubulin assembly, suggesting its potential as a multi-target anti-tumor agent.
MedKoo Cat#: 556393
Name: GJG057 free base
CAS#: 2761767-18-2 (free base)
Chemical Formula: C21H21F5N4O2
Exact Mass: 456.1585
Molecular Weight: 456.42
Elemental Analysis: C, 55.26; H, 4.64; F, 20.81; N, 12.28; O, 7.01
The following data is based on the product molecular weight 456.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
