Crenolanib (CP-868596) is an orally bioavailable, selective small molecule inhibitor of PDGFRα and PDGFRβ with IC50 of 0.9 and 1.8 nM respectively. Crenolanib (CP-868596) is a 100-500-fold more potent inhibitor of PDGFRα and PDGFRβ than other commercially available TKIs.
|Cell lines||MV4-11, MOLM-13, PL-21, OCI-AML3, THP-1 and U937 cell line|
|Preparation method||Measurement of cell viability
The effects of a 72-h drug treatment on AML cell line viability were determined by the WST-1 cell proliferation reagent (Roche Applied Science; Indianapolis, IN); cell viability was determined in Ba/F3 cells using the MTT cell proliferation reagent (Roche Applied Science) according to the manufacturer’s instructions.
|Incubation time||72 h|
|Animal models||FLT3-ITD−positive MV4-11 cells tumour xenograft mouse model|
|Formulation||formulated in 5% glycerol formal (Sigma-Aldrich, St. Louis, MO)|
|Dosages||15 mg/kg once daily (Monday to Friday) for 3 consecutive weeks beginning 10 days after cell injection|
|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.
Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia.
Zimmerman EI, et al. Blood. 2013 Nov 21;122(22):3607-15. PMID: 24046014.
Crenolanib Inhibits the Drug-Resistant PDGFRA D842V Mutation Associated with Imatinib-Resistant Gastrointestinal Stromal Tumors.
Heinrich et al. Clin Cancer Res. 2012 Aug 15;18(16):4375-84. PMID: 22745105.
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