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(E/Z)-Rigosertib sodium

CAS号

1225497-78-8

分子式

C21H24NNaO8S

主要靶点

PLK

仅限科研使用

Cat No : CM06040

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Synonyms

(E/Z) ON-01910 sodium|ON 01910|ON01910|ON-01910|N-[2-甲氧基-5-[[[2-(2,4,6-三甲氧基苯基)乙烯基]磺酰]甲基]苯基]甘氨酸钠盐|PLK1

验证数据展示

  • CAS No.: 1225497-78-8

    (E/Z)-Rigosertib sodium
    CAS#: 1225497-78-8

产品信息

CAS号 1225497-78-8
分子式 C21H24NNaO8S
主要靶点 PLK
主要通路 细胞周期
分子量 473.47
纯度 99.82%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 (E/Z) ON-01910 sodium|ON 01910|ON01910|ON-01910|N-[2-甲氧基-5-[[[2-(2,4,6-三甲氧基苯基)乙烯基]磺酰]甲基]苯基]甘氨酸钠盐|PLK1

靶点活性

PDGFR:18 nM(Cell-free assay) |FLK1:42 nM(Cell-free assay) |Src:55 nM(Cell-free assay) |BCR-ABL:32 nM(Cell-free assay) |PLK1:9 nM(Cell-free assay)

体内活性

在体内，该化合物未显示出血液毒性、肝损伤或神经毒性，且在多种异种移植裸鼠模型中均能有效抑制肿瘤生长。ON01910与多种化疗化合物表现出强烈的协同作用，经常引发肿瘤的完全退化[1]。

体外活性

ON01910是一种小分子Plk1活性抑制剂，能够诱导肿瘤细胞由于纺锤体异常而引起的有丝分裂停滞，并最终导致它们的凋亡。该化合物并非与ATP竞争，而是与酶的底物结合位点竞争[1]。

溶解度

DMSO:94 mg/mL (198.53 mM)

参考文献

1.Gumireddy K , Reddy M V R , Cosenza S C , et al. ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent.[J]. Cancer Cell, 2005, 7(3):275-286.
2.Dai, Yi-Han, Lai, et al. ON 01910.Na inhibits growth of diffuse large B-cell lymphoma by cytoplasmic sequestration of sumoylated C-MYB/TRAF6 complex[J]. Translational Research the Journal of Laboratory & Clinical Medicine, 2016.

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