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Crenolanib

Cat. No. M1723
Crenolanib Structure
Synonym:

CP-868596

Size Price Availability Quantity
10mg USD 180 In stock
50mg USD 450 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 443.54
Formula C26H29N5O2
CAS Number 670220-88-9
Purity >98%
Solubility DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Crenolanib, CP-868596 supplier, VEGFR/PDGFR, inhibitors

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