TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM.
Cell Experiment | |
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Cell lines | MV4-11 |
Preparation method | Plating MV4-11 cells at 10,000 cells per well in 100 μL of in RPMI media containing penn/strep, 10% FBS, and 0.2 ng/mL GM-CSF. Compound dilutions or 0.1% DMSO (vehicle control) is added to cells which are allowed to grow for 72 h at standard cell growth conditions.An equal volume of CellTiterGlo reagent is added to each well and luminescence is quantified in order to measure total cell growth . Total cell growth is quantified as the difference in luminescent counts of cell number at Day 0 compared to total cell number at Day 3 (72 h of growth and/or compound treatment).Calculated all IC50 values in GraphPadPrism using non-linear regression analysis with a multiparameter (variable slope) equation. |
Concentrations | ~5 μM |
Incubation time | 72 hours |
Animal Experiment | |
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Animal models | |
Formulation | |
Dosages | |
Administration |
Molecular Weight | 360.43 |
Formula | C18H20N2O4S |
CAS Number | 301305-73-7 |
Solubility (25°C) | DMSO |
Storage | 2-8°C, protect from light |
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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GTP-14564
GTP-14564 is a tyrosine kinase inhibitor targeting to internal tandem duplication (ITD) and FLT3. |
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