作用于CDK4、Ark5、PDGFRβ、FGFR1、RET和Fyn,IC50分别为3.9、5、26、26、9.2和11 nM。 ON123300是一种多靶点激酶抑制剂。 RTK的信号传导过度激活通常是由EGFR突变/扩增或PDGFR扩增/过表达引起的。 FGFR1信号传导也发生在显示FGFR1激酶结构域获得功能突变的GBM中。 体外:在先前的研究中,用ON123300处理Z138C和Granta 519细胞时,发现ON123300有效抑制Rb家族蛋白的磷酸化。此外,ON123300能够抑制参与PI3K / AKT途径的蛋白质的磷酸化。此外,较低浓度ON123300处理的细胞出现细胞周期停滞,然而,较高的浓度可能导致凋亡诱导。 ON123300是有效的多靶点激酶抑制剂,对CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), Fyn的IC50分别为3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM和11nM。
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ON-123300
Dangerous GoodsCAS number:1357470-29-1 molecular formula:C24H27N7O
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compound introduction
Specs
| Chinese alias | - | ||
| English alias | ON123300 | 1357470-29-1 | ON-123300 | narazaciclib | 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile | QJ8RO3296G | CHEMBL3115681 | Pyrido(2,3-d)pyrimidine-6-carbonitrile, 8-cyclopentyl-7,8 | ||
| CAS number | 1357470-29-1 | molecular formula | C24H27N7O |
| molecular weight | 429.5 g/mol | Exact mass | - |
| PSA | 88.400 Ų | logp | 3.100 |
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physicochemical properties
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Safety information
pictogram:
GHS07
Signal word:
Warning
Hazard Statement:
H302: 吞食有害
Statement of Preventive Measures:
P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
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