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Rigosertib

现货
Catalog No.
B1288
PI3K/PLK1抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,080.00
Ship with 10-15 days
10mg
¥ 1,800.00
Ship with 10-15 days
50mg
¥ 7,200.00
Ship with 10-15 days

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Background

Rigosertib is a dual inhibitor of phosphoinositide 3-kinase (PI3K) and polo-like kinase 1 (PLK1) [1].

In vitro studies show that rigosertib inhibits the PI3K/AKT pathway, down-regulates cyclin D1, induces NOXA and BIM and activates the JNK pathway in human leukemic cells. Rigosertib induces apoptosis of a variety of human tumor cell lines including breast, prostate, ovarian, pancreatic, SCLC, colorectal, melanoma and et al. For instant, it shows anti-tumor efficacy in BT20, MCF-7, BT474, OV-CAR-3, A549 and HCT-116 with IC50 values of 80nM, 75nM, 50nM, 75nM, 90nM and 75nM, respectively. In addition, rigosertib is also effective against the drug resistant tumor cell lines. It potently inhibits tumor growth with IC50 values of 100nM and 50nM against MES-SA/DX5 and CEM/C2, respectively. Moreover, it is reported that rigosertib can affect the cell cycle of both normal cells and tumor cells. Rigosertib leads to a blockade of cell cycle progression in the G1 and G2/M phases in normal diploid human fetal lung cells. When treated with DU145 cells, rigosertib induces cell cycle arrest in G2/M phase [2].

References:
[1] Anderson R T, Keysar S B, Bowles D W, et al. The Dual Pathway Inhibitor Rigosertib Is Effective in Direct Patient Tumor Xenografts of Head and Neck Squamous Cell Carcinomas. Molecular cancer therapeutics, 2013, 12(10): 1994-2005.
[2] Reddy M V R, Venkatapuram P, Mallireddigari M R, 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. Journal of medicinal chemistry, 2011, 54(18): 6254-6276.

Chemical Properties

StorageStore at -20°C
M.Wt451.49
Cas No.592542-59-1
FormulaC21H25NO8S
SolubilitySoluble in DMSO
Chemical Name2-[2-methoxy-5-[[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonylmethyl]anilino]acetic acid
SDFDownload SDF
Canonical SMILESCOC1=C(C=C(C=C1)CS(=O)(=O)C=CC2=C(C=C(C=C2OC)OC)OC)NCC(=O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

质量控制和MSDS

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化学结构

Rigosertib