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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 | |
|---|---|
| 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; cell viability was determined in Ba/F3 cells using the MTT cell proliferation reagent according to the manufacturer’s instructions. |
| Concentrations | 0~100 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | FLT3-ITD−positive MV4-11 cells tumour xenograft mouse model |
| Formulation | formulated in 5% glycerol formal |
| 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 ≥ 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related VEGFR/PDGFR Products |
|---|
| ABT-869
ABT-869 (Linifanib) is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of VEGFR and PDGFR. |
| Tivozanib (AV-951)
Tivozanib (AV-951) is a potent VEGFR-1, 2 and 3, c-Kit and PDGFR inhibitor with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM respectively. |
| Axitinib
Axitinib (AG013736) inhibits multiple targets including VEGFR, PDGFR and cKit. |
| Regorafenib
Regorafenib (BAY 73-4506) is a novel oral multikinase inhibitor of c-KIT, VEGFR2, B-Raf with IC50s of 17, 40 and 69 nM respectively. |
| Nintedanib
Nintedanib (BIBF1120) is a novel, potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively. |
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