Risvodetinib (IkT-148009) | c-Abl inhibitor | Probechem Biochemicals

Chemical Structure : IkT-148009

CAS No.: 2031185-00-7

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IkT-148009 (Risvodetinib, IkT09)

货号: PC-20144Not For Human Use, Lab Use Only.

IkT-148009 (Risvodetinib, IkT09) is a potent, selective, orally bioavailable and brain-penetrant c-Abl inhibitor with IC50 of 33 and 14 nM for c-Abl (Abl1) and its closely related isoform c-Abl2 (Arg), respectively.

规格	价格	库存
1 mg	￥1280	In stock
5 mg	￥2980	In stock
10 mg	￥4880	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

IkT-148009 (Risvodetinib, IkT09) is a potent, selective, orally bioavailable and brain-penetrant c-Abl inhibitor with IC50 of 33 and 14 nM for c-Abl (Abl1) and its closely related isoform c-Abl2 (Arg), respectively.
IkT-148009 shows little to know inhibition against the other members of the c-Abl family, c-Kit, PDGFRα, and PDGFRβ with IC50 of 2975, 1009 and 881 nM, respectively.
IkT-148009 (100 mg/kg per day) suppressed c-Abl activation in the mouse brains of MPTP-treated mice.
IkT-148009 showed protection from degeneration of nigrostriatal DA neurons in mouse brain in MPTP neurotoxicity mouse model of parkinson's disease (PD), significantly reduced the MPTP-induced loss of dopamine and the loss of the DA metabolites, 3-4-dihydroxyphenylacetic acid (DOPAC), homovanillic acid (HVA), and 3-methoxytyramine (3MT).
IkT-148009 (100 mg/kg per day, 1% HPMC (hydroxypropyl methylcellulose), 1% Tween 80, and 10% PEG 400 in sterile water, oral gavage) rescued DA neuron loss, reduced pathological α-synuclein inmouse model of inherited and sporadic PD.

物理化学性质&存储条件

分子量	574.69
分子式	C33H34N8O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-[4-Methyl-3-[[4-[5-(4-methyl-5-isoxazolyl)-3-pyridinyl]-2-pyrimidinyl]amino]phenyl]-4-[(4-methyl-1-piperazinyl)methyl]benzamide

参考文献

1. Patent US9828370B2.

2. Karuppagounder SS, et al. Sci Transl Med. 2023 Jan 18;15(679):eabp9352.

IkT-148009 (Risvodetinib, IkT09)

生物&药学活性

物理化学性质&存储条件

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IkT-148009 (Risvodetinib, IkT09)

生物&药学活性

物理化学性质&存储条件

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