Rigosertib sodium (Synonyms: 瑞格色替钠; ON-01910 sodium)

目录号: HY-12037 纯度: 99.57%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Rigosertib sodium (ON-01910 sodium) 是一种多激酶抑制剂和选择性抗癌剂，通过抑制 PI3K/Akt 途径诱导细胞凋亡，促进组蛋白 H2AX 的磷酸化并诱导细胞周期中的 G2/M 期停滞。Rigosertib sodium 是一种选择性的非 ATP 竞争性 PLK1 抑制剂，IC₅₀ 值为 9 nM。

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Rigosertib sodium Chemical Structure

CAS No. : 592542-60-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥729	In-stock
1 mg	￥360	In-stock
5 mg	￥700	In-stock
10 mg	￥1200	In-stock
50 mg	￥4400	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

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Customer Review

Other Forms of Rigosertib sodium:

Rigosertib In-stock
(E/Z)-Rigosertib sodium 询价

MCE 顾客使用本产品发表的 5 篇科研文献

Rigosertib sodium 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Polo-like Kinase (PLK) 亚型特异性产品:

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PLK1 PLK2 PLK3 PLK4

查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle^[1]^[2]. Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC₅₀ of 9 nM^[3].

IC₅₀ & Target^[1]

PLK1

9 nM (IC₅₀)

PLK2

260 nM (IC₅₀)

PDGFR

18 nM (IC₅₀)

Src

155 nM (IC₅₀)

BCR-ABL

32 nM (IC₅₀)

Cdk1

260 nM (IC₅₀)

Flt1

42 nM (IC₅₀)

Fyn

182 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
2008	IC₅₀	0.15 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human 2008 cells assessed as cell viability after 96 hrs by trypan blue exclusion Cytotoxicity against human 2008 cells assessed as cell viability after 96 hrs by trypan blue exclusion	[PMID: 21812421]
A2780	GI₅₀	0.04 μM Compound: Rigosertib Sodium	Antiproliferative activity against human A2780 cells measured after 72 hrs by MTT assay Antiproliferative activity against human A2780 cells measured after 72 hrs by MTT assay	[PMID: 27815119]
A549	IC₅₀	0.09 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human A549 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human A549 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
AGS	IC₅₀	0.08 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human AGS cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human AGS cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
Bel-7402	IC₅₀	0.1 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human Bel7402 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human Bel7402 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
BT-20	IC₅₀	0.08 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human BT20 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human BT20 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
BT-474	IC₅₀	0.05 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human BT474 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human BT474 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
BXPC-3	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human BxPC3 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human BxPC3 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
CCRF-CEM	IC₅₀	0.1 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human CEM cells assessed as cell viability after 96 hrs by trypan blue exclusion Cytotoxicity against human CEM cells assessed as cell viability after 96 hrs by trypan blue exclusion	[PMID: 21812421]
CEM/C2	IC₅₀	0.05 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against multidrug-resistant human CEM/C2 cells assessed as cell viability after 96 hrs by trypan blue exclusion Cytotoxicity against multidrug-resistant human CEM/C2 cells assessed as cell viability after 96 hrs by trypan blue exclusion	[PMID: 21812421]
COLO 205	IC₅₀	0.15 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human COLO205 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human COLO205 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
COLO 320	IC₅₀	0.06 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human COLO320 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human COLO320 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
Daudi	IC₅₀	0.15 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human Daudi cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human Daudi cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
DLD-1	IC₅₀	0.15 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human DLD1 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human DLD1 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
DU-145	IC₅₀	0.1 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human DU145 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human DU145 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
Granta-519	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human GRANTA-519 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human GRANTA-519 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HCC70	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human HCC70 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human HCC70 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HCT-116	GI₅₀	0.06 μM Compound: Rigosertib Sodium	Antiproliferative activity against human HCT116 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells measured after 72 hrs by MTT assay	[PMID: 27815119]
HCT-116	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human HCT116 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human HCT116 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HCT-15	IC₅₀	0.09 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human HCT15 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human HCT15 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HEL	IC₅₀	0.05 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human HEL cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human HEL cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HeLa	IC₅₀	0.1 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human HeLa cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human HeLa cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HL-60	IC₅₀	0.02 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human HL60 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human HL60 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HUVEC	IC₅₀	> 100 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against HUVEC after 96 hrs by trypan blue exclusion assay Cytotoxicity against HUVEC after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
K562	IC₅₀	0.015 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human K562 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human K562 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
KB	IC₅₀	0.07 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human KB cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human KB cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
KG-1a	IC₅₀	0.03 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human KG1a cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human KG1a cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
LP-1	IC₅₀	0.03 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human LP-1 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human LP-1 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
MCF7	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human MCF7 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human MCF7 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
MDA-MB-157	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human MDA-MB-157 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human MDA-MB-157 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
MDA-MB-231	IC₅₀	0.025 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human MDA-MB-231 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human MDA-MB-231 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
MES-SA	IC₅₀	0.1 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human MES-SA cells assessed as cell viability after 96 hrs by trypan blue exclusion Cytotoxicity against human MES-SA cells assessed as cell viability after 96 hrs by trypan blue exclusion	[PMID: 21812421]
MES-SA/Dx5	IC₅₀	0.1 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against multidrug-resistant human MES-SA/Dx5 cells assessed as cell viability after 96 hrs by trypan blue exclusion Cytotoxicity against multidrug-resistant human MES-SA/Dx5 cells assessed as cell viability after 96 hrs by trypan blue exclusion	[PMID: 21812421]
MIA PaCa-2	IC₅₀	0.05 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human MIAPaCa2 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human MIAPaCa2 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
MOLT-4	IC₅₀	0.04 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human MOLT4 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human MOLT4 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
NAMALVA	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human NAMALWA cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human NAMALWA cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
NCI-H157	IC₅₀	0.08 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human NCI-H157 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human NCI-H157 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
NCI-H187	IC₅₀	0.08 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human NCI-H187 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human NCI-H187 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
NCI-H1975	IC₅₀	0.09 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human NCI-H1975 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human NCI-H1975 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
NCI-H417	IC₅₀	0.08 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human NCI-N417 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human NCI-N417 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
OPM-2	IC₅₀	0.015 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human OPM2 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human OPM2 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
OVCAR-3	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human OVCAR3 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human OVCAR3 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
PANC-1	IC₅₀	0.04 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human PANC1 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human PANC1 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
PC-3	IC₅₀	0.15 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human PC3 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human PC3 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
Raji	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human Raji cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human Raji cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
RPMI-7951	IC₅₀	0.025 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human RPMI7951 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human RPMI7951 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
SK-BR-3	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human SKBR3 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human SKBR3 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
SW480	IC₅₀	0.06 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human SW480 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human SW480 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
T47D	IC₅₀	0.17 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human T47D cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human T47D cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
U-266	IC₅₀	0.025 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human U266 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human U266 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
U-87MG ATCC	IC₅₀	0.08 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human U87 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human U87 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
U-937	IC₅₀	0.01 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human U937 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human U937 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
WM793	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human WM793 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human WM793 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]

体外研究
(In Vitro)

Rigosertib 是 PLK1 的非 ATP 竞争性抑制剂，IC₅₀ 为 9 nM。Rigosertib 还表现出对 PLK2、PDGFR、Flt1、BCR-ABL、Fyn、Src 和 CDK1 的抑制作用，IC₅₀ 为 18-260 nM。Rigosertib 显示出对 94 种不同肿瘤细胞系的细胞杀伤活性，IC₅₀ 为 50-250 nM，包括 BT27、MCF-7、DU145、PC3、U87、A549、H187、RF1、HCT15、SW480、和 KB 细胞。而在 HFL、PrEC、HMEC 和 HUVEC 等正常细胞中，Rigosertib 几乎没有作用，除非其浓度大于 5-10 μM。在 HeLa 细胞中，Rigosertib (100-250 nM) 诱导纺锤体异常和细胞凋亡^[3]。Rigosertib 还抑制多种多药耐药肿瘤细胞系，包括 MES-SA、MES-SA/DX5a、CEM 和 CEM/C2a，IC₅₀ 为 50-100 nM。在 DU145 细胞中，Rigosertib (0.25-5 μM) 在 G2/M 期阻断细胞周期进程，导致含有 subG1 含量 DNA 的细胞积累，并激活凋亡途径。在 A549 细胞中，Rigosertib (50 nM-0.5 μM) 诱导细胞活力丧失和半胱天冬酶 3/7 激活^[4]。Rigosertib sodium (2 μM) 诱导慢性淋巴细胞白血病 (CLL) 细胞凋亡，对 T 细胞或正常 B 细胞无毒性。Rigosertib sodium (2 μM) 还可消除滤泡树突状细胞对 CLL 细胞的促存活作用，并减少 SDF-1 诱导的白血病细胞迁移^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Rigosertib (250 mg/kg，腹腔注射) 显著抑制小鼠 Bel-7402、MCF-7 和 MIA-PaCa 细胞异种移植模型中的肿瘤生长^[3]。Rigosertib (200 mg/kg，腹腔注射) 在小鼠 BT20 细胞异种移植模型中显示出对肿瘤生长的抑制作用^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

473.47

Formula

C₂₁H₂₄NNaO₈S

CAS 号

592542-60-4

性状

固体

颜色

White to yellow

中文名称

瑞格色替钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 150 mg/mL (316.81 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : ≥ 52 mg/mL (109.83 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1121 mL	10.5603 mL	21.1207 mL
5 mM	0.4224 mL	2.1121 mL	4.2241 mL
10 mM	0.2112 mL	1.0560 mL	2.1121 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5.25 mg/mL (11.09 mM); 澄清溶液

此方案可获得 ≥ 5.25 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 52.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5.25 mg/mL (11.09 mM); 澄清溶液

此方案可获得 ≥ 5.25 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 52.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 5.25 mg/mL (11.09 mM); 澄清溶液

此方案可获得 ≥ 5.25 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 52.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案四

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (5.28 mM); 悬浊液
方案五

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.28 mM); 澄清溶液

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： PBS
Solubility: 50 mg/mL (105.60 mM); 澄清溶液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 99.57%

选择批次：

Data Sheet (650 KB) SDS (252 KB)

COA (192 KB) LCMS (95 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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 [Content Brief]

Cell Assay ^[2]	Tumor cells are plated into six-well dishes at a density of 1×10⁵ cells/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 exclusion. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Bel-7402 tumor models: twenty female athymic (NCR-nu/nu) nude mice are injected with 1 × 10⁷ Bel-7402 tumor cells subcutaneously, and 10-14 days later, when the tumor volumes reach 200-250 mm, the mice are divided into four groups such that each group harbors tumors of the same volume. Rigosertib (ON01910, 250 mg/kg) dissolved in PBS is administered alone or in combination with NSC 266046 (100 mg/kg) intraperitonially on alternate days. Tumor measurements are done two times/week using traceable digital vernier calipers. Body weight is determined during each measurement. The animals are observed for signs of toxicity^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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 [Content Brief]

Rigosertib sodium 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.1121 mL	10.5603 mL	21.1207 mL	52.8017 mL
	5 mM	0.4224 mL	2.1121 mL	4.2241 mL	10.5603 mL
	10 mM	0.2112 mL	1.0560 mL	2.1121 mL	5.2802 mL
	15 mM	0.1408 mL	0.7040 mL	1.4080 mL	3.5201 mL
	20 mM	0.1056 mL	0.5280 mL	1.0560 mL	2.6401 mL
	25 mM	0.0845 mL	0.4224 mL	0.8448 mL	2.1121 mL
	30 mM	0.0704 mL	0.3520 mL	0.7040 mL	1.7601 mL
	40 mM	0.0528 mL	0.2640 mL	0.5280 mL	1.3200 mL
	50 mM	0.0422 mL	0.2112 mL	0.4224 mL	1.0560 mL
	60 mM	0.0352 mL	0.1760 mL	0.3520 mL	0.8800 mL
	80 mM	0.0264 mL	0.1320 mL	0.2640 mL	0.6600 mL
	100 mM	0.0211 mL	0.1056 mL	0.2112 mL	0.5280 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rigosertib592542-60-4ON-01910瑞格色替钠ON01910ON 01910Polo-like Kinase (PLK)PI3KApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Rigosertib sodium (Synonyms: 瑞格色替钠; ON-01910 sodium)

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Rigosertib sodium (Synonyms: 瑞格色替钠; ON-01910 sodium)

Customer Review

Other Forms of Rigosertib sodium:

Rigosertib sodium 相关抗体

MCE 顾客使用本产品发表的 5 篇科研文献

Rigosertib sodium 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Polo-like Kinase (PLK) 亚型特异性产品:

查看 PI3K 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Rigosertib sodium 相关抗体:

摩尔计算器

稀释计算器

Rigosertib sodium 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

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