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Rigosertib

CAS号

592542-59-1

分子式

C21H25NO8S

主要靶点

PDGFR|Bcr-Abl|Apoptosis|CDK|FLT|PLK|PI3K|Src

仅限科研使用

Cat No : CM06039

Print datasheet

Synonyms

Cdk1|BCR-ABL|BcrAbl|Apoptosis|Fyn|Flt1|瑞格色替|Src|inhibit|Inhibitor|ON 01910|ON01910|ON-01910|PDGFR|Rigosertib|Phosphoinositide 3-kinase|PI3K|Polo-like Kinase (PLK)|PLK1|PLK|PLK2

验证数据展示

  • CAS No.: 592542-59-1

    Rigosertib
    CAS#: 592542-59-1

产品信息

CAS号 592542-59-1
分子式 C21H25NO8S
主要靶点 PDGFR|Bcr-Abl|Apoptosis|CDK|FLT|PLK|PI3K|Src
主要通路 血管生成|蛋白酪氨酸激酶|细胞周期|凋亡|PI3K/Akt/mTOR 信号通路|血管生成|蛋白酪氨酸激酶|血管生成|细胞周期|蛋白酪氨酸激酶|细胞骨架|血管生成|蛋白酪氨酸激酶
分子量 451.49
纯度 97.33%， 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 Cdk1|BCR-ABL|BcrAbl|Apoptosis|Fyn|Flt1|瑞格色替|Src|inhibit|Inhibitor|ON 01910|ON01910|ON-01910|PDGFR|Rigosertib|Phosphoinositide 3-kinase|PI3K|Polo-like Kinase (PLK)|PLK1|PLK|PLK2

靶点活性

Src:155 nM|PLK2:260 nM|PLK1:9 nM|BCR-ABL:32 nM|CDK1:260 nM|Fyn:182 nM|FLK1:42 nM|PDGFR:18 nM

体内活性

Rigosertib (200 mg/kg, i.p.) 在BT20细胞的小鼠异种移植模型中显示出抑制肿瘤生长的活性。Rigosertib (250 mg/kg, i.p.) 在Bel-7402、MCF-7和MIA-PaCa细胞的小鼠异种移植模型中显著抑制肿瘤生长[3][4]。

体外活性

Rigosertib是一种非ATP竞争性PLK1抑制剂（IC50: 9 nM），对94种不同肿瘤细胞株展示出细胞杀伤活性（IC50: 50-250 nM），包括BT27、MCF-7、DU145、PC3、U87、A549、H187、RF1、HCT15、SW480和KB细胞。Rigosertib还能抑制PLK2、PDGFR、Flt1、BCR-ABL、Fyn、Src和CDK1（IC50: 18-260 nM）。在正常细胞如HFL、PrEC、HMEC和HUVEC中，除非Rigosertib浓度大于5-10 μM，否则几乎不产生影响。同时，Rigosertib还能抑制多种耐药肿瘤细胞株，包括MES-SA、MES-SA/DX5a、CEM和CEM/C2a（IC50: 50-100 nM）。Rigosertib（100-250 nM）在HeLa细胞中导致纺锤体异常及细胞凋亡。Rigosertib（0.25-5 μM）在DU145细胞中阻断G2/M期的细胞周期进程，导致含有subG1 DNA含量的细胞累积，并激活凋亡途径。Rigosertib（50 nM-0.5 μM）在A549细胞中诱导生存能力丧失和caspase 3/7激活。Rigosertib（2 μM）在不对T细胞或正常B细胞产生毒性的条件下，诱导慢性淋巴细胞性白血病（CLL）细胞凋亡。Rigosertib（2 μM）还能抑制滤泡树突状细胞对CLL细胞的生存影响，并减少SDF-1诱导的白血病细胞迁移。

溶解度

DMSO:75 mg/mL (166.12 mM)

参考文献

1.Xu F, et al. Rigosertib as a selective anti-tumor agent can ameliorate multiple dysregulated signalingtransduction pathways in high-grade myelodysplastic syndrome. Sci Rep. 2014 Dec 4;4:7310.
2.Hyoda T, et al. Rigosertib induces cell death of a myelodysplastic syndrome-derived cell line by DNA damage-induced G2/M arrest. Cancer Sci. 2015 Mar;106(3):287-93.
3.Gumireddy K, et al. ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent. Cancer Cell. 2005 Mar;7(3):275-86.
4.Reddy MV, et al. Discovery of a clinical stage multi-kinase inhibitor sodium (E)-2-{2-methoxy-5-[(2',4',6'-trimethoxystyrylsulfonyl)methyl]phenylamino}acetate (ON 01910.Na): synthesis, structure-activity relationship, and biological activity. J Med Chem. 2011 Sep 22;54(18):6254-76.
5.Chapman CM, et al. ON 01910.Na is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. Clin Cancer Res. 2012 Apr 1;18(7):1979-91

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