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.
|Related VEGFR/PDGFR Products|
Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
|Pazopanib HCl (GW786034 )
Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.
|Dovitinib (TKI-258) Dilactic Acid
Dovitinib Dilactic acid (TKI258 Dilactic acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM.
Toceranib(SU 11654; PHA 291639) is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ.
|Nintedanib (BIBF 1120)
Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.