CGP52421 is a FLT3 inhibitor, which is also an metabolite of midostaurin (PKC412).
|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.
Dose- and time-dependent pharmacokinetics of midostaurin in patients with diabetes mellitus.
Wang Y, et al. J Clin Pharmacol. 2008 Jun;48(6):763-75. PMID: 18508951.
A highly sensitive method for the detection of PKC412 (CGP41251) and its metabolites by high-performance liquid chromatography.
Illmer T, et al. J Pharmacol Toxicol Methods. 2007 Jul-Aug;56(1):23-7. PMID: 17395497.
|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.
UNC-2025 is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.
TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM.
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