In vitro: GNE-477 (Compound 8) has improved potency in the MCF7.1 cell proliferation assay with an EC50 of 143 nM.
In vivo: GNE-477 also exhibits stasis in a PC3 tumor growth inhibition study. In an experiment evaluating the tumor growth inhibition of a PC3 tumor xenograft over 14 days, stasis is achieved at a 20 mg/kg QD dose and significant inhibition is observed with doses as low as 1 mg/kg QD. GNE-477 is generally well tolerated during this study as demonstrated by acceptable levels of weight loss comparable to that observed with the animals in the vehicle cohort.
Cell Experiment | |
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Cell lines | |
Preparation method | |
Concentrations | |
Incubation time |
Animal Experiment | |
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Animal models | Rats |
Formulation | 0.5% methylcellulose/0.2% Tween-80 |
Dosages | 1 mg/kg |
Administration | orally |
Molecular Weight | 504.63 |
Formula | C21H28N8O3S2 |
CAS Number | 1032754-81-6 |
Solubility (25°C) | 9.2 mg/mL in DMSO |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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