BAY-593 is an orally active inhibitor of geranylgeranyltransferase-I (GGTase-I) that effectively blocks the activation of Rho-GTPases, leading to the inactivation of YAP1/TAZ signaling pathways and demonstrating significant antitumor activity. In cellular assays, BAY-593 exhibits potent antiproliferative effects, with an IC₅₀ of 38.4 nM in HT-1080 fibrosarcoma cells and 564 nM in MDA-MB-231 breast cancer cells. Mechanistically, it promotes YAP1 inactivation by facilitating its cytoplasmic translocation with an IC₅₀ of 44 nM and downregulates YAP1/TAZ target genes, including ANKRD1, CTGF, CYR61, CDC6, and DKK1. In vivo studies further support its therapeutic potential, as oral administration at doses of 5 mg/kg (once or twice daily) and 10 mg/kg (once daily) significantly reduces tumor growth in MDA-MB-231 human breast cancer xenografts in female NMRI nu/nu mice
MedKoo Cat#: 128202
Name: BAY-593 HCl
CAS#: 2413020-57-0 (HCl)
Chemical Formula: C26H32ClF3N2O3
Exact Mass: 0.0000
Molecular Weight: 513.00
Elemental Analysis: C, 60.87; H, 6.29; Cl, 6.91; F, 11.11; N, 5.46; O, 9.36
The following data is based on the product molecular weight 513.00 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 |
