Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
Molecular Weight | 611.51 |
Formula | C26H29F3N5O7P |
CAS Number | 2088852-47-3 |
Form | Solid |
Solubility (25°C) | DMSO 5 mg/mL (Need ultrasonic and warming) |
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.
[2] No authors listed. Cold Spring Harb Protoc. Phosphate-Limited Chemostat Medium
[3] Marc G Vervloet, et al. Nat Rev Nephrol. The role of phosphate in kidney disease
[4] Eleanor Lederer. J Physiol. Regulation of serum phosphate
[5] O Susan Iheagwara, et al. Hemodial Int. Phosphorus, phosphorous, and phosphate
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