Rigosertib (ON-01910)

For research use only. Not for use in humans.

目录号：S1362

Rigosertib (ON-01910) Chemical Structure

CAS No. 1225497-78-8

Rigosertib (ON-01910) 是一种非ATP竞争性PLK1抑制剂，无细胞试验中IC50为9 nM，比作用于Plk2选择性高30倍，对Plk3没有抑制活性。Rigosertib 可抑制 PI3K/Akt 信号通路并激活氧化应激信号。Rigosertib 可诱导多种癌细胞的凋亡。Phase 3。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 2630.22	现货
5mg	RMB 1381.36	现货
50mg	RMB 7944.48	现货
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客户使用Selleck生产的Rigosertib (ON-01910)发表文献25篇：

Nature, 2019, 10.1038/s41586-019-1607-3

PubMed: 31578521 ( click the link to review the publication )

Mol Cell, 2020, 79(1):191-198.e3

PubMed: 32619469 ( click the link to review the publication )

Biology (Basel), 2020, 15;9(5):E99

PubMed: 32429320 ( click the link to review the publication )

J Clin Invest, 2019, 1;129(11):4797-4816

PubMed: 31589169 ( click the link to review the publication )

Clin Cancer Res, 2019, 25(11):3384-3391

PubMed: 30846478 ( click the link to review the publication )

Toxicol Sci, 2019, 10.1093/toxsci/kfz123

PubMed: 31132080 ( click the link to review the publication )

Stem Cells Dev, 2019, 28(7):438-453

PubMed: 30667343 ( click the link to review the publication )

Neuron, 2018, 98(1):142-155

PubMed: 29551489 ( click the link to review the publication )

Pharmacol Res, 2018, 134:166-178

PubMed: 29944980 ( click the link to review the publication )

Sci Rep, 2018, 8(1):9991

PubMed: 29968772 ( click the link to review the publication )

Oncotarget, 2018, 9(3):3605-3618

PubMed: 29423069 ( click the link to review the publication )

Mol Cell, 2017, 68(1):210-223e6

PubMed: 28985505 ( click the link to review the publication )

Oncotarget, 2017, 8(58):97928-97940

PubMed: 29228663 ( click the link to review the publication )

Oncotarget, 2017, 9(13):10920-10933

PubMed: 29541386 ( click the link to review the publication )

Cell Death Dis, 2016, 7:e2207

PubMed: 27124581 ( click the link to review the publication )

Transl Res, 2016, 10.1016/j.trsl.2016.04.001

PubMed: 27150054 ( click the link to review the publication )

Cell Cycle, 2016, 15(15):2009-18

PubMed: 27249336 ( click the link to review the publication )

Exp Hematol, 2016, 44(4):247-56

PubMed: 26724640 ( click the link to review the publication )

J Control Release, 2015, 204:20-9

PubMed: 25681050 ( click the link to review the publication )

J Control Release, 2015, 204:20-29

PubMed: ( click the link to review the publication )

Endocr Relat Cancer, 2014, 13(5):1054-66

PubMed: 24748653 ( click the link to review the publication )

Sci Rep, 2014, 4:7310

PubMed: 25472472 ( click the link to review the publication )

Cancer Res, 2013, 73(20):6310-22

PubMed: 24067506 ( click the link to review the publication )

Stem Cells, 2013, 31(6):1051-63

PubMed: 23404835 ( click the link to review the publication )
PLoS One, 2013, 8(11):e79863

PubMed: 24223200 ( click the link to review the publication )

产品安全说明书

PLK抑制剂选择性比较

生物活性

产品描述

特性

Rigosertib是作用于Polo样激酶（PLK1）的非ATP竞争性抑制剂。

靶点

PLK1 ^[1] (Cell-free assay)	PDGFR ^[1] (Cell-free assay)	Bcr-Abl ^[1] (Cell-free assay)	Flt1 ^[1] (Cell-free assay)	Src ^[1] (Cell-free assay)	点击更多
9 nM	18 nM	32 nM	42 nM	155 nM	点击更多

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。^[1] 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。^[2]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。^[3]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
T47D	NFnlWWREgXSxdH;4bYNqfHliYYPzZZk>		NWrHO4xnPzJiaILz	MYjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGdKPTBiPTCwMlAyKM7:TT6=	NWLxXph7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OlM6PDRpPkKxOFY{QTR2PD;hQi=>
MDA468	M1nHN2N6fG:2b4jpZ4l1gSCjc4PhfS=>		NEm0doY4OiCqcoO=	NGj2Z2tEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEF2NkigZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NEA:KDBwMEKg{txONg>?	MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR4M{m0OEc,OjF2NkO5OFQ9N2F-
MCF7	M3PUcGN6fG:2b4jpZ4l1gSCjc4PhfS=>		MnK2O\|IhcHK\|	M{\NSmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhT0l3MDC9JFAvODVizszNMi=>	NIfzPJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUS2N\|k1PCd-MkG0OlM6PDR:L3G+
HCT116	NWPoWZlPS3m2b4TvfIlkcXS7IHHzd4F6		MUW3NkBpenN?	NGrVdGdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NEA:KDBwMEWg{txONg>?	MkjGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2NkO5OFQoRjJzNE[zPVQ1RC:jPh?=
MDA468	NUTk[2VXS3m2b4TvfIlkcXS7IHHzd4F6		NHXzdW41QCCqcoO=	NGPteHREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEF2NkigZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiR1m1NEA:KDBwM{CyJO69VS5?	MkTlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2NkO5OFQoRjJzNE[zPVQ1RC:jPh?=
MDA468	M4ewUWN6fG:2b4jpZ4l1gSCjc4PhfS=>		MXSyOEBpenN?	MljBR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCPDZ6IHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEeLNUCgQUAxNjZyMTFOwG0v	NVuzWFA2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OlM6PDRpPkKxOFY{QTR2PD;hQi=>
MRC5	Mnv1R5l1d3SxeHnjbZR6KGG\|c3H5		NYDuSWdzPzJiaILz	NWnPdZg6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVKFNTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwJF0hOC55MTFOwG0v	NWTsV3pmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OlM6PDRpPkKxOFY{QTR2PD;hQi=>
MCF7	NX7aUXVFTnWwY4Tpc44h[XO\|YYm=	MnvENUB2VQ>?		MUfN[ZRi[m:uaXOgd5Ri[mmuaYT5JI9nKHSqZTDjc41xd3WwZDDpckBpfW2jbjDNR2Y4KGOnbHzzJIF1KDFidV2=	M1yyflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNE[zPVQ1Lz5{MUS2N\|k1PDxxYU6=
MRC5	MX7GeY5kfGmxbjDhd5NigQ>?	M1nLTVEhfU1?		NIftc3FO\XSjYn;sbYMhe3SjYnnsbZR6KG:oIITo[UBkd22yb4Xu[EBqdiCqdX3hckBOWkN3IHPlcIx{KGG2IEGgeW0>	MlW3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2NkO5OFQoRjJzNE[zPVQ1RC:jPh?=
K562	MWXDfZRwfG:6aXPpeJkh[XO\|YYm=		MVm5OkBpenN?	MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IEm2JIhzeyCkeTD0dplx[W5iYnz1[UBmgGOudYPpc44h[XO\|YYmsJGlEPTBiPTCwMlAxPzVizszNMi=>	Mki3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF6MUK0NlEoRjJzOEGyOFIyRC:jPh?=
DU145	NWPSOWZWS3m2b4TvfIlkcXS7IHHzd4F6		Ml\ZPVYhcHK\|	MlXwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[W[2ZYKgPVYhcHK\|IHL5JJRzgXCjbjDicJVmKGW6Y3z1d4lwdiCjc4PhfUwhUUN3MDC9JFAvODd3IN88UU4>	NGLNdHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUixNlQzOSd-MkG4NVI1OjF:L3G+
HeLa	NH3NbGZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MmjXO\|IhcHK\|	MmP1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKZVzhJINmdGy\|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NEA:KDBwMEGyJO69VS5?	NHHYfZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES3NVg4Oyd-MkS0O\|E5PzN:L3G+
LNCAP	MnLxRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MXq3NkBpenN?	M{KyTGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRXIheG:\|aYTpeoUhcHWvYX6gUG5ESVBiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG\|c3H5MEBIUTVyIE2gNE4xOjVizszNMi=>	NGLBSYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES3NVg4Oyd-MkS0O\|E5PzN:L3G+
PANC1	NXHkWIhxSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MnvsO\|IhcHK\|	NWnHVmVvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQRW5EOSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGdKPTBiPTCwMlA{QSEQvF2u	M{TxOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEexPFc{Lz5{NES3NVg4OzxxYU6=
MCF7	MVnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NEWzd4E4OiCqcoO=	NUf4eXk{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBGWiCyb4PpeIl3\SCqdX3hckBOS0Z5IHPlcIx{KGG\|c3Xzd4VlKGG\|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhT0l3MDC9JFAvODVizszNMi=>	NFP5VFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES3NVg4Oyd-MkS0O\|E5PzN:L3G+
MCF7	NXHWXYJXSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MnfiO\|IhcHK\|	MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwJF0hOC5yNTFOwG0v	MkW1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{G4O\|MoRjJ2NEexPFc{RC:jPh?=
MDA-MB-231	MVrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		M2TLU\|czKGi{cx?=	NGjQPFZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGVTKG6nZ3H0bZZmKGi3bXHuJG1FSS2PQj2yN\|Eh[2WubIOgZZN{\XO\|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDHTVUxKD1iMD6wOVch\|ryPLh?=	NGfaTHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES3NVg4Oyd-MkS0O\|E5PzN:L3G+
A2780	M4LHW2FvfGmycn;sbYZmemG2aY\lJIF{e2G7		NHHmXIM4OiCqcoO=	M33vR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZZN{\XO\|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDHTVUxKD1iMD6wOlIh\|ryPLh?=	M3HYdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEexPFc{Lz5{NES3NVg4OzxxYU6=
HCT116	M3zYVmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MkPlO\|IhcHK\|	NYfNUJFzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG\|c3H5MEBIUTVyIE2gNE4xPyEQvF2u	NVW5SmozRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0O\|E5PzNpPkK0OFcyQDd\|PD;hQi=>
DU145	M{jIUGFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NFfP[GQ4OiCqcoO=	NVLZdmpkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBCWiCwZXfheIl3\SCqdX3hckBFXTF2NTDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUCgQUAxNjB5NTFOwG0v	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR5MUi3N{c,OjR2N{G4O\|M9N2F-
A2780	MkPuSpVv[3Srb36gZZN{[Xl?	MWOwMlI2KHWP	MYiyOEBpenN?	M2nwdHJm\HWldHnvckBqdiCFRFOyOWMhdGW4ZXygbY4hcHWvYX6gRVI4QDBiY3XscJMh[XRiMD6yOUB2VSCjZoTldkAzPCCqcoOgZpkhX2W\|dHXyckBjdG:2IHHuZYx6e2m\|	MoTwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{G4O\|MoRjJ2NEexPFc{RC:jPh?=
A2780	MnPJRZBweHSxc3nzJIF{e2G7	NGXMU5ExNjJ3IIXN	MWWyOEBpenN?	NEXsSW1KdmS3Y4Tpc44hd2ZiYYDvdJRwe2m\|IHnuJIh2dWGwIFGyO\|gxKGOnbHzzJIF{e2W\|c3XkJIF{KGOjc4Dhd4UuOy95IHHjeIl3[XSrb36gZZQhOC5{NTD1UUBi\nSncjCyOEBpenNiYomgeZNqdmdiQYDvMW9PTSCqb33v[4Vv\W:3czDjZZNx[XOnLUOvO{BscXR?	MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR5MUi3N{c,OjR2N{G4O\|M9N2F-
A2780	MlTVSpVv[3Srb36gZZN{[Xl?	MVuwMlI2KHWP	MWSyOEBpenN?	NVyyN2RpWmWmdXP0bY9vKGmwIF3jcFEhdGW4ZXygbY4hcHWvYX6gRVI4QDBiY3XscJMh[XRiMD6yOUB2VSCjZoTldkAzPCCqcoOgZpkhX2W\|dHXyckBjdG:2IHHuZYx6e2m\|	NXexfHk6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0O\|E5PzNpPkK0OFcyQDd\|PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	pAbl / Abl / PCrk-L / Crk-L / Cleaved caspase3 / Cleaved PARP / pHistone H2A.X; PubMed: 26008977 Oncotarget Ba/F3 T315I cells were treated with rigosertib at the indicated concentrations for 24 h. Total extracts were examined via immunoblotting with anti-phospho ABL, phospho-Crk-L, phosphohistone H2A.X, cleaved caspase 3, cleaved-PARP, ABL, Crk-L, and β-actin antibodies (abs). ABL, Abelson; PARP, poly (ADP-ribose) polymerase; abs, antibodies.	26008977
Immunofluorescence	p-ATF / COX IV; PubMed: 27764820 Oncotarget Representative confocal microscopy images of FaDu, UMSCC 47 and D-HMVEC cells treated with rigosertib (1.0 μM) or ON 01911.Na (1.0 μM) for 24 h before fixing, staining with indicated antibodies, and capturing images. Green: p-ATF; Red: Cox IV (mitochondrial marker); Blue: DAPI (nuclear marker).	27764820
Growth inhibition assay	GI50; PubMed: 29108241 Oncotarget The GI50 values of BI2536, rigosertib, and poloxin were determined in both parental and volasertib-resistant R-MOLM14 and R-HL-60. Error bars represent the mean values ± S.D. of at least three independent experiments. Cell viability; PubMed: 27764820 Oncotarget Cell viability as measured by MTS. FaDu, Detroit 562, UMSCC 1, UMSCC 47 and UMSCC 104 cells were treated with increasing concentrations of rigosertib for 48 h, and cell viability was assessed. 50% growth inhibition (IC50) is recorded for each cell line in μM in the legend. Untreated cells were considered 100% viable and percent viability of cells treated with rigosertib was calculated vs. this control. Data represent the mean +/− SD of 3 independent experiments.	29108241 27764820

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。^[1]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。^[2]

激酶实验：^[1]	- 合并体外测定PLK1的酶实验: 10 ng 重组PLK1和不同浓度Rigosertib在15 µL反应混合物(50 mM HEPES,10 mM MgCl₂,1 mM EDTA,2 mM二硫苏糖醇,0.01% NP-40,pH 为7.5)中在室温下反应30分钟。激酶反应在20 µL反应混合物［15 µL 酶 + 抑制剂, 2 µL 1 mM ATP, 2 µL γ³²P ATP (40 μci), 和1 µL 重组Cdc25C (100 ng)或酪蛋白 (1 μg) 底物］在30^oC下进行20分钟。在20 µL 2× Laemmli buffer中沸腾2分钟终止反应。通过18% SDS-PAGE分离磷酸化的底物。烘干凝胶柱，用X-射线处理3-10分钟。
细胞实验：^[2]	- 合并 Cell lines: 多种肿瘤细胞系,包括 BT20,MCF-7,DU145,PC3,U87,A549,H187,RF1,HCT15,HeLa,和Raji细胞 Concentrations: 1 nM-10 µM, 溶于DMSO，作为储存液 Incubation Time: 96小时 Method: 细胞生长在含10%FBS和1 unit/mL青霉素-链霉亲和素溶液的DMEM或RPMI培养基中。肿瘤细胞按每孔1×10⁵个细胞接种在6孔板上，24小时后，加入不同浓度Rigosertib。处理96小时后，测定每孔细胞数。通过台酚蓝染色测定全部存活细胞数。 (Only for Reference)
动物实验：^[1]	- 合并 Animal Models: 携带Bel-7402,MCF-7,和MIA-PaCa细胞的雌性无胸腺NCR-nu/nu鼠 Dosages: 250 mg/kg Administration: 腹腔注射 (Only for Reference)

参考文献

溶解度 (25°C)

体外	DMSO	95 mg/mL (200.64 mM)
	Water	95 mg/mL (200.64 mM)
	Ethanol	Insoluble
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： water	95mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Rigosertib (ON-01910) SDF

分子量	473.47
化学式	C₂₁H₂₄NNaO₈S
CAS号	1225497-78-8
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2020-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04177498	Not yet recruiting	Drug: Rigosertib Sodium\|Other: Quality-of-Life Assessment	Recessive Dystrophic Epidermolysis Bullosa	Thomas Jefferson University\|Onconova Therapeutics Inc.	January 1 2021	Early Phase 1
NCT02075034	Withdrawn	Drug: rigosertib	Myelodysplastic Syndrome	Onconova Therapeutics Inc.	May 2014	Phase 1
NCT02030639	Completed	Drug: rigosertib	Healthy	Onconova Therapeutics Inc.	January 2014	Phase 1
NCT01928537	Completed	Drug: rigosertib sodium	Myelodysplastic Syndromes\|Refractory Anemia With Excess Blasts\|Chronic Myelomonocytic Leukemia\|Cytopenia	Onconova Therapeutics Inc.	August 2013	Phase 3
NCT01807546	Completed	Drug: rigosertib	Head and Neck Squamous Cell Carcinoma\|Anal Squamous Cell Carcinoma\|Lung Squamous Cell Carcinoma\|Cervical Squamous Cell Carcinoma\|Esophageal Squamous Cell Carcinoma\|Skin Squamous Cell Carcinoma\|Penile Squamous Cell Carcinoma	Onconova Therapeutics Inc.	March 2013	Phase 2
NCT01168011	Completed	Drug: rigosertib	Solid Tumor	Onconova Therapeutics Inc.	July 2010	Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

PLK Signaling Pathway Map

PLK Inhibitors with Unique Features

泛Plk抑制剂

BI 2536 : Pan-Plk1, Plk1, IC50=0.83 nM; Plk2, IC50=3.5 nM; Plk3, IC50=9 nM.
活性最强的Plk抑制剂

BI 2536 : Plk1, IC50=0.83 nM.
用于临床的Plk抑制剂

Volasertib (BI 6727) : Phase III for acute myeloid leukaemia.
最新的Plk抑制剂

Ro3280 ^New : Potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.

研究领域

产品类型

定制您的化合物库

Rigosertib (ON-01910)

客户使用Selleck生产的Rigosertib (ON-01910)发表文献25篇：

产品安全说明书

PLK抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Rigosertib (ON-01910) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2020-01-06)

技术支持

PLK Signaling Pathway Map

PLK Inhibitors with Unique Features

相关PLK产品