Risvodetinib free base

Risvodetinib is an orally active, selective and brain-penetrant protein tyrosine kinase inhibitor.

For research use only. Not for human or veterinary use.

Target c-Met/HGFR Bcr-Abl

Research area Neurological Disease Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Risvodetinib structure

CAS No.: 2031185-00-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 1,700.00	BP-02289-100mg	In stock	Get quote
250 mg	USD 2,880.00	BP-02289-250mg	In stock	Get quote
500 mg	USD 4,380.00	BP-02289-500mg	Inquire	Get quote
1 g	Inquire	BP-02289-1g	Inquire	Inquire

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Description

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 .

Biological activity

In Vivo Risvodetinib (100 mg/kg, p.o., daily for 10 days) performs robust functional rescue and significant protection of dopaminergic (DA) neurons in the MPTP acute neurotoxicity mouse model. Risvodetinib (50 or 100 mg/kg, p.o., daily for 8 or 20 weeks) recovers nigrostriatal neurodegeneration and reduces phosphorylated α-synuclein in the mouse model of inherited PD. Risvodetinib (100 mg/kg, p.o., once a day, 5 times per week for 6 months) has an effective neuroprotection and reduces α-synuclein pathology in mouse model of sporadic PD.

Identifiers

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
InChIKey: ADGOPPKEIZXKAZ-UHFFFAOYSA-N

Specifications

MW (average): 574.6755
Formula: C₃₃H₃₄N₈O₂
CAS No.: 2031185-00-7
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : 100 mg/mL

Documents

References

[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.

[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.

Same target

Search c-Met/HGFR

Same research area

Search Neurological Disease