All AbMole products are for research use only, cannot be used for human consumption.
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 (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 | |
|---|---|
| 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 ≥ 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 |
|---|
| Conbercept
Conbercept (KH902) is a monoclonal antibody targeting VEGFRA fused to the IGHG1 Fc fragment. Conbercept is produced by the fusion of the second C-LIKE of FLT1 and the third and fourth C-LIKE of KDR with IGHG1 Fc. |
| SU5208
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2). |
| VEGFR-IN-1
VEGFR-IN-1 is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively. |
| (Z)-Orantinib
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. |
| (Rac)-SAR131675
(Rac)-SAR131675 is the racemate of SAR131675. |
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