Belizatinib
Belizatinib Basic information
- Product Name:
- Belizatinib
- Synonyms:
-
- Belizatinib
- Belizatinib (TSR011)
- TSR-011
- CS-2493
- TSR011; TSR011; TSR 011; BELIZATINIB
- Benzamide, 4-fluoro-N-[6-[[4-(1-hydroxy-1-methylethyl)-1-piperidinyl]methyl]-1-[cis-4-[[(1-methylethyl)amino]carbonyl]cyclohexyl]-1H-benzimidazol-2-yl]-
- TSR011,Trk Receptor,CD246,ALK tyrosine kinase receptor,Tropomyosin related kinase receptor,TSR 011,inhibit,Cluster of differentiation 246,Belizatinib,Inhibitor,Anaplastic lymphoma kinase,Anaplastic lymphoma kinase (ALK)
- 4-Fluoro-N-(6-((4-(2-hydroxypropan-2-yl)piperidin-1-yl)methyl)-1-(cis-4-(isopropylcarbamoyl)cyclohexyl)-1H-benzo[d]imidazol-2-yl)benzamide
- CAS:
- 1357920-84-3
- MF:
- C33H44FN5O3
- MW:
- 577.73
- Mol File:
- 1357920-84-3.mol
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Belizatinib Chemical Properties
- Density
- 1.27±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF:30.0(Max Conc. mg/mL);51.93(Max Conc. mM)
DMSO:143.33(Max Conc. mg/mL);248.08(Max Conc. mM)
Ethanol:65.0(Max Conc. mg/mL);112.5(Max Conc. mM) - form
- A crystalline solid
- pka
- 12.55±0.43(Predicted)
- color
- White to off-white
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Belizatinib Usage And Synthesis
Description
Belizatinib, also known as TSR-011, is an oral inhibitor of ALK and TRK.
Description
Belizatinib is an inhibitor of anaplastic lymphoma kinase (ALK) and tropomyosin-related kinases A/B/C (IC50s = 0.7 and <3 nM, respectively).
Uses
Belizatinib is used in treating diseases via targeted modulation of gene signaling networks.
in vivo
Belizatinib (TSR-011) exerts sustained potent inhibition of ALK-dependent tumour growth in mouse models[1].
IC 50
TrkA; TrkB; TrkC
References
[1] H. ARKENAU. Phase (Ph) 1/2a study of TSR-011, a potent inhibitor of ALK and TRK, in advanced solid tumors including crizotinib-resistant ALK positive non-small cell lung cancer.[J]. Journal of Clinical Oncology, 2015, 33 1: 8063-8063. DOI: 10.1200/jco.2015.33.15_suppl.8063
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