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Radotinib(IY-5511)Bcl-Abl tyrosine kinase inhibitor

Radotinib(IY-5511)

Catalog No. B5846
Size Price Stock Qty
5mg $70.00 In stock
10mg $120.00 In stock
25mg $210.00 In stock
50mg $320.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Radotinib(IY-5511)

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Chemical Properties

Cas No. 926037-48-1 SDF Download SDF
Chemical Name (Z)-4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-((4-(pyrazin-2-yl)pyrimidin-2-yl)amino)benzimidic acid
Canonical SMILES CC1=C(NC2=NC=CC(C3=CN=CC=N3)=N2)C=C(/C(O)=N/C4=CC(N(C=N5)C=C5C)=CC(C(F)(F)F)=C4)C=C1
Formula C27H21F3N8O M.Wt 530.5
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Radotinib(IY-5511) is a novel and selective Bcl-Abl tyrosine kinase inhibitor. [1]

Bcl-Abl is a constitutively activated chimeric tyrosine kinase which is the genetic abnormality expressed in patient with CML (chronic myeloid leukemia).

In vitro, radotinib couples to Bcr-Abl and reduce the phosphorylation of Bcr-Abl target protein CrkL. The pre-clinical studies shows superiority of radotinib to imatinib in both wild-type and mutant BCR-ABL1 positive CML cell lines. [1]

In a phase I clinical trial, dose up to 1000 mg/day of radotinib exhibits no dose-limiting toxicities. Phase II study proves radotinib to be an effective and well tolerated in chronic phase-chronic myeloid leukemia patients with resistance and/or intolerance to Bcr-Abl1 tyrosine kinase inhibitors. [1]

Reference:
1.  Kim SH, Menon H, Jootar S 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.