Rigosertib (ON-01910)

中文名	Rigosertib (ON-01910)
英文名	sodium (E)-2-((2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)phenyl)amino)acetate
别名	ON 01910 钠盐 RIGOSERTIB钠盐(RANDOM CONFIGURATION) (2-甲氧基-5-(((2,4,6-三甲氧基苯乙烯基)磺酰基)甲基)苯基)甘氨酸钠盐 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
英文别名	Estybon ESTYBON ON-01910 ON 01910 sodium salt Rigosertib (ON-01910) sodium (E)-2-((2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)phenyl)amino)acetate N-[2-Methoxy-5-[[[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl]methyl]phenyl]glycine sodium salt N-[2-Methoxy-5-[[[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl]methyl]phenyl]glycine sodium salt Rigosertib (ON-01910)
CAS	1225497-78-8
化学式	C21H24NNaO8S
分子量	473.47193
熔点	>256oC (dec.)
溶解度	甲醇 (微溶) 、水 (微溶)
存储条件	Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
外观	固体
颜色	Pale Yellow to Pale Green
靶点	PLK1
体外研究	Rigosertib是PLK1的非ATP竞争性抑制剂，IC50为9 nM。Rigosertib也抑制 PLK2,PDGFR,Flt1,BCR-ABL,Fyn,Src和CDK1, IC50为18-260 nM。Rigosertib具有使细胞死亡的活性，作用于94种不同肿瘤细胞系，IC50为50-250 nM,包括BT27,MCF-7,DU145,PC3,U87,A549,H187,RF1,HCT15,SW480,和KB细胞。Rigosertib作用于正常细胞,如 HFL,PrEC,HMEC,和HUVEC没有效果，除非作用浓度高于5-10 µM。100-250 nM Rigosertib作用于HeLa 细胞，诱导纺锤体变异和凋亡。 Rigosertib也抑制一些多重耐药的的肿瘤细胞系，包括 MES-SA, MES-SA/DX5a, CEM, 和 CEM/C2a, IC50为50-100 nM。0.25-5 µM Rigosertib作用于DU145细胞, 抑制细胞周期，使细胞停在G2/M 期,和激活凋亡通路。50 nM-0.5 µM Rigosertib作用于A549细胞,诱导存活力和caspase 3/7激活的丧失。最新研究显示, Rigosertib作用于慢性淋巴细胞性白血病 (CLL)细胞，诱导凋亡，且作用于T细胞或正常B细胞没有毒性。Rigosertib 慢性淋巴细胞性白血病(CLL)细胞，也抑制滤泡树突状细胞的促生存效果，作用于白血病细胞，降低SDF-1诱导的迁移。
体内研究	Rigosertib按250 mg/kg剂量作用于携带Bel-7402,MCF-7,和MIA-PaCa细胞的鼠移植瘤模型,明显抑制肿瘤生长。Rigosertib按200 mg/kg剂量作用于携带BT20细胞的鼠移植瘤模型，也抑制肿瘤生长。
参考资料展开查看	1: Lucas CD, Dorward DA, Tait MA, Fox S, Marwick JA, Allen KC, Robb CT, Hirani N, Haslett C, Duffin R, Rossi AG. Downregulation of Mcl-1 has anti-inflammatory pro-resolution effects and enhances bacterial clearance from the lung. Mucosal Immunol. 2013 Nov 27. doi: 10.1038/mi.2013.102. [Epub ahead of print] PubMed PMID: 24280938. 2: Dolman ME, den Hartog IJ, Molenaar JJ, Schellens JH, Beijnen JH, Sparidans RW. Liquid chromatography-tandem mass spectrometric assay for the cyclin-dependent kinase inhibitor AT7519 in mouse plasma. J Pharm Biomed Anal. 2014 Jan 25;88:216-20. doi: 10.1016/j.jpba.2013.08.051. Epub 2013 Sep 12. PubMed PMID: 24080524. 3: Alessandri AL, Duffin R, Leitch AE, Lucas CD, Sheldrake TA, Dorward DA, Hirani N, Pinho V, de Sousa LP, Teixeira MM, Lyons JF, Haslett C, Rossi AG. Induction of eosinophil apoptosis by the cyclin-dependent kinase inhibitor AT7519 promotes the resolution of eosinophil-dominant allergic inflammation. PLoS One. 2011;6(9):e25683. doi: 10.1371/journal.pone.0025683. Epub 2011 Sep 30. PubMed PMID: 21984938; PubMed Central PMCID: PMC3184151. 4: Mahadevan D, Plummer R, Squires MS, Rensvold D, Kurtin S, Pretzinger C, Dragovich T, Adams J, Lock V, Smith DM, Von Hoff D, Calvert H. A phase I pharmacokinetic and pharmacodynamic study of AT7519, a cyclin-dependent kinase inhibitor in patients with refractory solid tumors. Ann Oncol. 2011 Sep;22(9):2137-43. doi: 10.1093/annonc/mdq734. Epub 2011 Feb 16. PubMed PMID: 21325451. 5: Squires MS, Cooke L, Lock V, Qi W,

Rigosertib (ON-01910) - 配置溶液浓度参考

	1mg	5mg	10mg
1 mM	2.112 ml	10.56 ml	21.121 ml
5 mM	0.422 ml	2.112 ml	4.224 ml
10 mM	0.211 ml	1.056 ml	2.112 ml
5 mM	0.042 ml	0.211 ml	0.422 ml

最后更新：2024-01-02 23:10:35

Rigosertib (ON-01910) - 细胞实验

Cells are grown in either DMEM or RPMI supplemented with 10% fetal bovine serum and 1 unit/mL penicillin-streptomycin solution. Tumor cells are plated into six-well dishes at a density of 1 × 105cells/mL/well, and Rigosertib is added 24 hours later at various concentrations. Cell counts are determined from duplicate wells after 96-hour of treatment. The total number of viable cells is determined by trypan blue exclusio(Only for Reference) Cell lines: A number of tumor cell lines, including BT20, MCF-7, DU145, PC3, U87, A549, H187, RF1, HCT15, HeLa, and Raji cells

最后更新：2023-08-16 21:32:38

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产品名: Rigosertib 去供应商网站查看询盘
CAS: 1225497-78-8
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价格: 25mg-249,5mg-171,1ml-1160
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产品名: (2-甲氧基-5-(((2,4,6-三甲氧基苯乙烯基)磺酰基)甲基)苯基)甘氨酸钠盐去供应商网站查看询盘
CAS: 1225497-78-8
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产品名: Rigosertib钠盐(随机配置) 去供应商网站查看询盘
CAS: 1225497-78-8
产地: 中国上海
包装: 50mg
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产品描述: 中文名：Rigosertib钠盐(随机配置) 英文名:Rigosertib Sodium(Random Configuration) CAS:1225497-7 更多

上海源叶生物科技有限公司

现货供应

产品名: Rigosertib (ON-01910) 去供应商网站查看询盘
CAS: 1225497-78-8
产地: 上海
规格: 95%
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