BAY-593
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BAY-593 is an orally active GGTase-I inhibitor. BAY-593 can block YAP1/TAZ signaling in animals and has antitumor activity.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 2413020-56-9
- Formula: C26H31F3N2O3
- Molecular Weight:476.53
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
Description
IC50 & Target
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GGTase I |
In Vitro
BAY-593 (0.5 nM-10 μM; 72 h) inhibits the proliferation of HT-1080 and MDA-MB-231 cells with the IC50 values of 0.038 and 0.564 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BAY-593 (2.5-20 mg/kg; oral administration; 14 days) shows dose-dependent antitumor activity in HT-1080 fibrosarcoma and MDA-MB-231 triple negative breast cancer xenotransplantation mouse models[1].
Pharmacokinetic Analysis in HT-1080 xenograft mouse models[1]
Pharmacokinetic Analysis in HT-1080 xenograft mouse models[1]
| Route | Dose (mg/kg) | Schedule | T/Cvolume on day 9 | Cmax (μg/L) | 4 days AUC (mg·h/L) | 4 days AUCunbound (μg·h/L) |
| p.o. | 2.5 | BID | 0.44 | 100 | 2.6 | 37 |
| p.o. | 5 | QD | 0.43 | 76 | 2.8 | 39 |
| p.o. | 10 | Q2D | 0.069 | 350 | 5.4 | 76 |
| p.o. | 20 | Q4D | 0.063 | 2262 | 16.0 | 224 |
| p.o. | 5 | BID | 0.056 | 275 | 8.0 | 112 |
| p.o. | 10 | QD | 0.021 | 321 | 14.0 | 196 |