Neurotinib | c-Abl inhibitor | Probechem Biochemicals

Chemical Structure : Neurotinib

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Neurotinib (NCATS-SM1976)

货号: PC-22467Not For Human Use, Lab Use Only.

Neurotinib (NCATS-SM1976) is a potent, selective c-Abl allosteric inhibitor, reduces c-Abl phosphorylation and the activation of CRKII, shows potential to prevent epileptic-like seizure.

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生物&药学活性

Neurotinib (NCATS-SM1976) is a potent, selective c-Abl allosteric inhibitor, reduces c-Abl phosphorylation and the activation of CRKII, shows potential to prevent epileptic-like seizure.
Neurotinib binds c-Abl more strongly than GNF2, binds to c-Abl myristoyl pocket, the same as GNF2.
Neurotinib inhibits CRKII-GST phosphorylation in the 0.1-1 μM concentration range in an in vitro phosphorylation assay incubating CRKII (a c-Abl cellular target).
Neurotinib inhibits cell proliferation of K562 cells with IC50 of 2 uM, which depends on BCR-ABL activity.
Neurotinib reduces c-Abl phosphorylation and the activation of CRKII, exerts a protective effect against 100 μM NMDA toxicity in neurons at 1 uM.
Neurotinib displays improved selectivity and CNS pharmacokinetics in comparison to other c-Abl inhibitors.
Neurotinib (5 mg/kg) for 3 days inhibits the increase in c-Abl phosphorylation in pilocarpine-induced SE mice, protecting mice against seizures and improving survival.
Neurotinib ameliorates the convulsive state in kainic-acid-induced SE mice.
Neurotinib has been shown to be effective in Niemann-Pick A (NPA) and Alzheimer's mice models.

物理化学性质&存储条件

分子量	456.43
分子式	C23H19F3N4O3
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	2-(2-(piperazin-1-yl)pyridin-4-yl)-8-(trifluoromethoxy)dibenzo[b,f][1,4]oxazepin-11(10H)-one

参考文献

1. Chandía-Cristi A, et al. Cell Rep. 2024 May 28;43(5):114144.

2. Martinez A, et al. Antioxidants (Basel). 2023 Nov 16;12(11):2007.

Neurotinib (NCATS-SM1976)

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物理化学性质&存储条件

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Neurotinib (NCATS-SM1976)

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