Free shipping on all orders over $ 500

Crenolanib

Cat. No. M1723
Crenolanib Structure
Synonym:

CP-868596

Size Price Availability Quantity
10mg USD 160  USD160 In stock
25mg USD 260  USD260 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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 (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Zimmerman EI, et al. Blood. Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia.

[2] Heinrich et al. Clin Cancer Res. Crenolanib Inhibits the Drug-Resistant PDGFRA D842V Mutation Associated with Imatinib-Resistant Gastrointestinal Stromal Tumors.

Related VEGFR/PDGFR Products
Isolinderalactone

Isolinderalactone suppresses human glioblastoma growth and angiogenic activity through the inhibition of VEGFR2 activation in endothelial cells. Isolinderalactone suppressed the expression of B-cell lymphoma 2 (BCL-2), as well as of survivin and X-linked inhibitor of apoptosis protein (XIAP).

Oglufanide

Oglufanide (H-Glu-Trp-OH) is a dipeptide immunomodulator isolated from calf thymus.

KLTWQELYQLKYKGI

KLTWQELYQLKYKGI (QK) is a VEGF mimicking peptide, binds to the VEGF receptors and competes with VEGF.

Protein LMWP

Protein LMWP is a cell-penetrating peptide with vascular endothelial growth factor (VEGF) inhibitory activity.

CBO-P11

CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis.

  Catalog
Abmole Inhibitor Catalog




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


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.