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Rigosertib (ON-01910)

Rigosertib (ON-01910) 是一種非ATP競(jìng)爭(zhēng)性PLK1抑制劑，無(wú)細(xì)胞試驗(yàn)中IC50為9 nM，比作用于Plk2選擇性高30倍，對(duì)Plk3沒(méi)有抑制活性。Rigosertib 可抑制 PI3K/Akt 信號(hào)通路并激活氧化應(yīng)激信號(hào)。Rigosertib 可誘導(dǎo)多種癌細(xì)胞的凋亡。Phase 3。

Rigosertib (ON-01910) Chemical Structure

Rigosertib (ON-01910) Chemical Structure

CAS: 1225497-78-8

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買(mǎi)數(shù)量
10mM (1mL in DMSO) 2170 現(xiàn)貨
5mg 1381.36 現(xiàn)貨
50mg 7944.48 現(xiàn)貨
1g 31900 現(xiàn)貨
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Rigosertib (ON-01910)相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

PLK Signaling Pathways

PLK信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類(lèi)型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
A2780 Function assay 0.25 uM 24 hrs Reduction in CDC25C level in human A2780 cells at 0.25 uM after 24 hrs by Western blot analysis 24471873
A2780 Apoptosis assay 0.25 uM 24 hrs Induction of apoptosis in human A2780 cells assessed as caspase-3/7 activation at 0.25 uM after 24 hrs by using Apo-ONE homogeneous caspase-3/7 kit 24471873
A2780 Function assay 0.25 uM 24 hrs Reduction in Mcl1 level in human A2780 cells at 0.25 uM after 24 hrs by Western blot analysis 24471873
MRC5 Function assay 1 uM Metabolic stability of the compound in human MRC5 cells at 1 uM 21463944
MCF7 Function assay 1 uM Metabolic stability of the compound in human MCF7 cells at 1 uM 21463944
LNCAP Antiproliferative assay 72 hrs Antiproliferative activity against AR positive human LNCAP cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.025 μM. 24471873
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.012 μM. 24471873
DU145 Cytotoxicity assay 96 hrs Cytotoxicity against human DU145 cells after 96 hrs by trypan blue exclusion assay, IC50 = 0.075 μM. 21812421
K562 Cytotoxicity assay 96 hrs Cytotoxicity against human K562 cells after 96 hrs by trypan blue exclusion assay, IC50 = 0.0075 μM. 21812421
MRC5 Cytotoxicity assay 72 hrs Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay, GI50 = 0.71 μM. 21463944
MDA468 Cytotoxicity assay 24 hrs Cytotoxicity against human MDA468 cells after 24 hrs by MTT assay, GI50 = 0.601 μM. 21463944
MDA468 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA468 cells after 48 hrs by MTT assay, GI50 = 0.302 μM. 21463944
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, GI50 = 0.05 μM. 21463944
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, GI50 = 0.05 μM. 21463944
MDA468 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA468 cells after 72 hrs by MTT assay, GI50 = 0.02 μM. 21463944
T47D Cytotoxicity assay 72 hrs Cytotoxicity against human T47D cells after 72 hrs by MTT assay, GI50 = 0.01 μM. 21463944
PANC1 Antiproliferative assay 72 hrs Antiproliferative activity against human PANC1 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.039 μM. 24471873
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against ER positive human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.05 μM. 24471873
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.05 μM. 24471873
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against ER negative human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.057 μM. 24471873
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.062 μM. 24471873
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.07 μM. 24471873
DU145 Antiproliferative assay 72 hrs Antiproliferative activity against AR negative human DU145 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.075 μM. 24471873
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生物活性

產(chǎn)品描述 Rigosertib (ON-01910) 是一種非ATP競(jìng)爭(zhēng)性PLK1抑制劑，無(wú)細(xì)胞試驗(yàn)中IC50為9 nM，比作用于Plk2選擇性高30倍，對(duì)Plk3沒(méi)有抑制活性。Rigosertib 可抑制 PI3K/Akt 信號(hào)通路并激活氧化應(yīng)激信號(hào)。Rigosertib 可誘導(dǎo)多種癌細(xì)胞的凋亡。Phase 3。
特性 Rigosertib是作用于Polo樣激酶（PLK1）的非ATP競(jìng)爭(zhēng)性抑制劑。
靶點(diǎn)
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)		 點(diǎn)擊更多
9 nM 18 nM 32 nM 42 nM 155 nM
體外研究(In Vitro)
體外研究活性 Rigosertib是PLK1的非ATP競(jìng)爭(zhēng)性抑制劑，IC50為9 nM。Rigosertib也抑制 PLK2,PDGFR,Flt1,BCR-ABL,Fyn,Src和CDK1, IC50為18-260 nM。Rigosertib具有使細(xì)胞死亡的活性，作用于94種不同腫瘤細(xì)胞系，IC50為50-250 nM,包括BT27,MCF-7,DU145,PC3,U87,A549,H187,RF1,HCT15,SW480,和KB細(xì)胞。Rigosertib作用于正常細(xì)胞,如 HFL,PrEC,HMEC,和HUVEC沒(méi)有效果，除非作用濃度高于5-10 μM。100-250 nM Rigosertib作用于HeLa 細(xì)胞，誘導(dǎo)紡錘體變異和凋亡。[1] Rigosertib也抑制一些多重耐藥的的腫瘤細(xì)胞系，包括 MES-SA, MES-SA/DX5a, CEM, 和 CEM/C2a, IC50為50-100 nM。0.25-5 μM Rigosertib作用于DU145細(xì)胞, 抑制細(xì)胞周期，使細(xì)胞停在G2/M 期,和激活凋亡通路。50 nM-0.5 μM Rigosertib作用于A549細(xì)胞,誘導(dǎo)存活力和caspase 3/7激活的喪失。[2]最新研究顯示, Rigosertib作用于慢性淋巴細(xì)胞性白血病 (CLL)細(xì)胞，誘導(dǎo)凋亡，且作用于T細(xì)胞或正常B細(xì)胞沒(méi)有毒性。Rigosertib 慢性淋巴細(xì)胞性白血病(CLL)細(xì)胞，也抑制濾泡樹(shù)突狀細(xì)胞的促生存效果，作用于白血病細(xì)胞，降低SDF-1誘導(dǎo)的遷移 。[3]
激酶實(shí)驗(yàn) 體外測(cè)定PLK1的酶實(shí)驗(yàn)
10 ng 重組PLK1和不同濃度Rigosertib在15 μL反應(yīng)混合物(50 mM HEPES,10 mM MgCl2,1 mM EDTA,2 mM二硫蘇糖醇,0.01% NP-40,pH 為7.5)中在室溫下反應(yīng)30分鐘。激酶反應(yīng)在20 μL反應(yīng)混合物［15 μL 酶 + 抑制劑, 2 μL 1 mM ATP, 2 μL γ32P ATP (40 μci), 和1 μL 重組Cdc25C (100 ng)或酪蛋白 (1 μg) 底物］在30oC下進(jìn)行20分鐘。在20 μL 2× Laemmli buffer中沸騰2分鐘終止反應(yīng)。通過(guò)18% SDS-PAGE分離磷酸化的底物。烘干凝膠柱，用X-射線處理3-10分鐘。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 多種腫瘤細(xì)胞系,包括 BT20,MCF-7,DU145,PC3,U87,A549,H187,RF1,HCT15,HeLa,和Raji細(xì)胞
濃度 1 nM-10 μM, 溶于DMSO，作為儲(chǔ)存液
孵育時(shí)間 96小時(shí)
方法 細(xì)胞生長(zhǎng)在含10%FBS和1 unit/mL青霉素-鏈霉親和素溶液的DMEM或RPMI培養(yǎng)基中。腫瘤細(xì)胞按每孔1×105個(gè)細(xì)胞接種在6孔板上，24小時(shí)后，加入不同濃度Rigosertib。處理96小時(shí)后，測(cè)定每孔細(xì)胞數(shù)。通過(guò)臺(tái)酚藍(lán)染色測(cè)定全部存活細(xì)胞數(shù)。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot pAbl / Abl / PCrk-L / Crk-L / Cleaved caspase3 / Cleaved PARP / pHistone H2A.X 26008977
Immunofluorescence p-ATF / COX IV 27764820
Growth inhibition assay GI50 Cell viability 29108241
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 Rigosertib按250 mg/kg劑量作用于攜帶Bel-7402,MCF-7,和MIA-PaCa細(xì)胞的鼠移植瘤模型,明顯抑制腫瘤生長(zhǎng)。[1]Rigosertib按200 mg/kg劑量作用于攜帶BT20細(xì)胞的鼠移植瘤模型，也抑制腫瘤生長(zhǎng)。[2]
動(dòng)物實(shí)驗(yàn) Animal Models 攜帶Bel-7402,MCF-7,和MIA-PaCa細(xì)胞的雌性無(wú)胸腺NCR-nu/nu鼠
Dosages 250 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04177498 Recruiting
Recessive Dystrophic Epidermolysis Bullosa
Thomas Jefferson University|Traws Pharma Inc.
 August 24 2021 Early Phase 1
NCT02075034 Withdrawn
Myelodysplastic Syndrome
Traws Pharma Inc.
 May 2014 Phase 1
NCT02030639 Completed
Healthy
Traws Pharma Inc.
 January 2014 Phase 1
NCT01928537 Completed
Myelodysplastic Syndromes|Refractory Anemia With Excess Blasts|Chronic Myelomonocytic Leukemia|Cytopenia
Traws Pharma Inc.
 August 2013 Phase 3
NCT01807546 Completed
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
Traws Pharma Inc.
 March 2013 Phase 2
NCT01168011 Completed
Solid Tumor
Traws Pharma Inc.
 July 2010 Phase 1

化學(xué)信息&溶解度

分子量 473.47 分子式

C21H24NNaO8S
CAS號(hào) 1225497-78-8 SDF Download Rigosertib (ON-01910) SDF
Smiles COC1=C(C=C(C=C1)CS(=O)(=O)C=CC2=C(C=C(C=C2OC)OC)OC)NCC(=O)[O-].[Na+]
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 95 mg/mL ( (200.64 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : 95 mg/mL (200.64 mM)

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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