JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50 of 18 nM.
Molecular Weight | 398.89 |
Formula | C21H23ClN4O2 |
CAS Number | 1610536-69-0 |
Form | Solid |
Solubility (25°C) | DMSO ≥ 250 mg/mL (ultrasonic and warming and heat to 60°C) |
Storage | 4°C, dry, sealed |
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.
[1] Chuangchuang Xu, et al. Org Biomol Chem. Metal-free and regiospecific synthesis of 3-arylindoles
[3] No authors listed. Carteolol
[5] S Groszkowski, et al. Pol J Pharmacol Pharm. 1-Haloacylpiperazines
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