2031185-00-7
Chemical Structure
Risvodetinib
Synonym(s): IkT-148009
- CAS No.: 2031185-00-7
- Formula:C33H34N8O2
- Molecular Weight:574.68
IUPAC Name: N-(4-methyl-3-((4-(5-(4-methylisoxazol-5-yl)pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide
InChIKey: ADGOPPKEIZXKAZ-UHFFFAOYSA-N
SMILES: O=C(C1=CC=C(CN2CCN(CC2)C)C=C1)NC3=CC=C(C)C(NC4=NC(C5=CN=CC(C6=C(C)C=NO6)=C5)=CC=N4)=C3
Biological Activity: Risvodetinib (IkT-148009) is an orally active, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying excellent target efficacy against c-Abl1, c-Abl2/Arg with IC50 values of 33 nM, 14 nM, respectively. Risvodetinib suppresses c-Abl activation and substantially protects dopaminergic neurons from degeneration in mouse models of both inherited and sporadic Parkinson’s disease (PD), which is promising for research in the field of PD[1][2][3][4].
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Risvodetinib | 99.15% | Risvodetinib (IkT-148009) is an orally active, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying excellent target efficacy against c-Abl1, c-Abl2/Arg with IC50 values of 33 nM, 14 nM, respectively. Risvodetinib suppresses c-Abl activation and substantially protects dopaminergic neurons from degeneration in mouse models of both inherited and sporadic Parkinson’s disease (PD), which is promising for research in the field of PD. | ||||||||||||||||||||
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- [1]. Karuppagounder SS, et al. The c-Abl inhibitor IkT-148009 suppresses neurodegeneration in mouse models of heritable and sporadic Parkinson's disease. Sci Transl Med. 2023 Jan 18;15(679):eabp9352. [Content Brief]
- [2]. Werner MH, et al. Preparation of N-[3-[[4-(2-pyridyl)pyrimidin-2-yl]amino]phenyl]-4-[(piperazin-1-yl)methyl]benzamide derivatives as inhibitors of kinases: World Intellectual Property Organization, WO2016172528. 2016-10-27.
- [3]. WHO Drug Information-World Health Organization (WHO).
- [4]. Werner MH, Olanow CW. Parkinson's Disease Modification Through Abl Kinase Inhibition: An Opportunity[J]. Mov Disord. 2022 Jan;37(1):6-15. [Content Brief]
Keywords