Radotinib

Modify Date: 2024-01-08 17:48:59

Radotinib Structure
Radotinib structure
Common Name Radotinib
CAS Number 926037-48-1 Molecular Weight 530.504
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C27H21F3N8O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Radotinib


Radotinib(IY-5511) is a novel and selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM for wild-type BCR-ABL1 kinase.IC50 value: 34 nM [1]Target: BCR-ABL1 inhibitorRadotinib is a BCR-ABL1 specific 2nd-generation tyrosine kinase inhibitor. According to recently conducted in vitro kinase assays, the IC50 value for radotinib against wild-type BCR-ABL1 kinase was 34 nM, which is relatively lower compared with the IC50 levels of c-kit (1,324 nM), PDGFR (PDGFRα, 75.5 nM; PDGFRβ, 130 nM) and src (>2,000 nM). Also, radotinib effectively inhibited the proliferation of common mutant clones of BCR-ABL1, with the exception of T315I. In an off-target kinase assay to assess safety, DDR, EPHB, LYN, and PDGFR kinases were inhibited below the 180 nM level.

 Names

Name 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyrazin-2-ylpyrimidin-2-yl)amino]benzamide
Synonym More Synonyms

 Radotinib Biological Activity

Description Radotinib(IY-5511) is a novel and selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM for wild-type BCR-ABL1 kinase.IC50 value: 34 nM [1]Target: BCR-ABL1 inhibitorRadotinib is a BCR-ABL1 specific 2nd-generation tyrosine kinase inhibitor. According to recently conducted in vitro kinase assays, the IC50 value for radotinib against wild-type BCR-ABL1 kinase was 34 nM, which is relatively lower compared with the IC50 levels of c-kit (1,324 nM), PDGFR (PDGFRα, 75.5 nM; PDGFRβ, 130 nM) and src (>2,000 nM). Also, radotinib effectively inhibited the proliferation of common mutant clones of BCR-ABL1, with the exception of T315I. In an off-target kinase assay to assess safety, DDR, EPHB, LYN, and PDGFR kinases were inhibited below the 180 nM level.
Related Catalog
References

[1]. Kim SH, et al. Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors. Haematologica. 2014 Jul;99(7):1191-6.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Molecular Formula C27H21F3N8O
Molecular Weight 530.504
Exact Mass 530.179016
PSA 114.00000
LogP 4.29
Index of Refraction 1.665
Storage condition -20℃

 Synonyms

Benzamide, 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(2-pyrazinyl)-2-pyrimidinyl]amino]-
Radotinib
4-Methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-{[4-(2-pyrazinyl)-2-pyrimidinyl]amino}benzamide
UNII-I284LJY110
IY-5511
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Price: ¥922/10 mM * 1 mL in DMSO

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