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 Experiment | |
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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. |
Concentrations | 0~100 μM |
Incubation time | 72 h |
Animal Experiment | |
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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 |
Administration | intraperitoneally |
Molecular Weight | 443.54 |
Formula | C26H29N5O2 |
CAS Number | 670220-88-9 |
Solubility (25°C) | DMSO |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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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