TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM.
|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.|
|Incubation time||72 hours|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Related FLT3 Products|
Gilteritinib is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
AMG 925 is a potent and orally bioavailable dual FLT3/CDK4 inhibitor with IC50 of 1 nM and 3 nM, respectively.
G-749 is a novel and potent FLT3 inhibitor with IC50 of 0.4 nM, 0.6 nM and 1 nM for FLT3 (WT), FLT3 (D835Y), and Mer, respectively, showing lower potency against other tyrosine kinases.
CGP52421 is a FLT3 inhibitor, which is also an metabolite of midostaurin (PKC412).
Tandutinib (MLN518), previously known as CT53518, is an orally active multitargeted tyrosine kinase inhibitor of FLT3, PDGFR and c-Kit.
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