Rhosin hydrochloride is a rho GTPase inhibitor (Kd = 354 nM). Inhibits binding of RhoA to guanine nucleotide exchange factors (GEFs) including LARG, DBL, LBC, p115 RhoGEF and PDZ RhoGEF. Has no effect on the binding of Rac1 or Cdc42 to their respective GEFs. Suppresses RhoA/C-mediated breast cancer cell migration and invasion in vitro. Also induces neurite outgrowth in synergy with NGF.
| Molecular Weight | 394.86 |
| Formula | C20H18N6O.HCl |
| CAS Number | 1281870-42-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 80 mg/mL Water 35 mg/mL |
| 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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