MedK Product data sheet MedKoo Cat#: 205990 Name: Radotinib CAS#: 926037-48-1 (free base) F F F Chemical Formula: C27H21F3N8O Exact Mass: 530.1790 O N Molecular Weight: 530.50 H Product supplied as: Powder N N N N N Purity (by HPLC): ≥ 98% H N Shipping conditions Ambient temperature N Storage conditions: Powder: -20°C 3 years; 4°C 2 years. In solvent: -80°C 3 months; -20°C 2 weeks.
1. Product description: Radotinib, also known as IY-5511, is an orally available, a second-generation tyrosine kinase inhibitor of Bcr-Abl fusion protein and the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. Upon administration, radotinib specifically inhibits the Bcr-Abl fusion protein, an abnormal enzyme expressed in Philadelphia chromosome-positive chronic myeloid leukemia (CML) cells. In addition, this agent also inhibits PDGFR thereby blocking PDGFR-mediated signal transduction pathways.
2. CoA, QC data, SDS, and handling instruction SDS and handling instruction, CoA with copies of QC data (NMR, HPLC and MS analytical spectra) can be downloaded from the product web page under “QC And Documents” section. Note: copies of analytical spectra may not be available if the product is being supplied by MedKoo partners. Whether the product was made by MedKoo or provided by its partners, the quality is 100% guaranteed.
3. Solubility data Solvent Max Conc. mg/mL Max Conc. mM DMSO 10.0 18.9
4. Stock solution preparation table: Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg 1 mM 1.89 mL 9.43 mL 18.85 mL 5 mM 0.38 mL 1.89 mL 3.77 mL 10 mM 0.19 mL 0.94 mL 1.89 mL 50 mM 0.04 mL 0.19 mL 0.38 mL
5. Molarity Calculator, Reconstitution Calculator, Dilution Calculator Please refer the product web page under section of “Calculator”
6. Recommended literature which reported protocols for in vitro and in vivo study In vitro study 1. Heo SK, Noh EK, Jeong YK, Ju LJ, Sung JY, Yu HM, Cheon J, Koh S, Min YJ, Choi Y, Jo JC. Radotinib inhibits mitosis entry in acute myeloid leukemia cells via suppression of Aurora kinase A expression. Tumour Biol. 2019 May;41(5):1010428319848612. doi: 10.1177/1010428319848612. PMID: 31074363. 2. Lee S, Kim S, Park YJ, Yun SP, Kwon SH, Kim D, Kim DY, Shin JS, Cho DJ, Lee GY, Ju HS, Yun HJ, Park JH, Kim WR, Jung EA, Lee S, Ko HS. The c-Abl inhibitor, Radotinib HCl, is neuroprotective in a preclinical Parkinson's disease mouse model. Hum Mol Genet. 2018 Jul 1;27(13):2344-2356. doi: 10.1093/hmg/ddy143. PMID: 29897434; PMCID: PMC6005030.
In vivo study 1. Heo SK, Noh EK, Jeong YK, Ju LJ, Sung JY, Yu HM, Cheon J, Koh S, Min YJ, Choi Y, Jo JC. Radotinib inhibits mitosis entry in acute myeloid leukemia cells via suppression of Aurora kinase A expression. Tumour Biol. 2019 May;41(5):1010428319848612. doi: 10.1177/1010428319848612. PMID: 31074363. 2. Lee S, Kim S, Park YJ, Yun SP, Kwon SH, Kim D, Kim DY, Shin JS, Cho DJ, Lee GY, Ju HS, Yun HJ, Park JH, Kim WR, Jung EA, Lee S, Ko HS. The c-Abl inhibitor, Radotinib HCl, is neuroprotective in a preclinical Parkinson's disease mouse model. Hum Mol Genet. 2018 Jul 1;27(13):2344-2356. doi: 10.1093/hmg/ddy143. PMID: 29897434; PMCID: PMC6005030.
MedKoo Biosciences || http://www.medkoo.com || [email protected] 2500 Gateway Centre Blvd Suite 400, Morrisville, NC27560, USA. Tel: 919-636-5577, Fax: 919-980-4831
MedK Product data sheet 7. Bioactivity Biological target: Radotinib (IY-5511) is a BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM.
In vitro activity Radotinib significantly decreased the expression of cyclin-dependent kinase 1 and cyclin B1, the key regulators of G2/M phase, and inhibited the expression of Aurora kinase A and Aurora kinase B in acute myeloid leukemia cells. In addition, radotinib decreased the expression and binding between p-Aurora kinase A and TPX2, which are required for spindle assembly. Furthermore, it reduced Aurora kinase A and polo-like kinase 1 phosphorylation and suppressed the expression of α-, β-, and γ-tubulin in acute myeloid leukemia cells.
Reference: Tumour Biol. 2019 May;41(5):1010428319848612. https://journals.sagepub.com/doi/10.1177/1010428319848612?url_ver=Z39.88- 2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub%20%200pubmed
In vivo activity The neuroprotective efficacy of Radotinib HCl, a brain penetrant c-Abl inhibitor, was evaluated in a pre-clinical model of Parkinson’s disease (PD). Administration of Radotinib HCl inhibited c-Abl activation and prevented dopaminergic neuron loss, neuroinflammation and behavioral deficits following α-synuclein PFF (preformed fibrils)-induced toxicity in vivo.
Reference: Hum Mol Genet. 2018 Jul 1;27(13):2344-2356. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6005030/
Note: The information listed here was extracted from literature. MedKoo has not independently retested and confirmed the accuracy of these methods. Customer should use it just for a reference only.
MedKoo Biosciences || http://www.medkoo.com || [email protected] 2500 Gateway Centre Blvd Suite 400, Morrisville, NC27560, USA. Tel: 919-636-5577, Fax: 919-980-4831