| 规格 | 价格 | 库存 | 数量 |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| 靶点 |
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)
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| 体外研究 (In Vitro) |
Rigosertib 的 IC50 为 9 nM，以非 ATP 竞争性方式抑制 PLK1。此外，rigosertib 还可抑制 PLK2、PDGFR、Flt1、BCR-ABL、Fyn、Src 和 CDK1，IC50 为 18–260 nM。 94 种不同的肿瘤细胞系，包括 BT27、MCF-7、DU145、PC3、U87、A549、H187、RF1、HCT15、SW480 和 KB 细胞，对 rigosertib 表现出细胞杀伤活性，IC50 为 50–250 nM 。然而，Rigosertib 对正常细胞（例如 HFL、PrEC、HMEC 和 HUVEC）几乎没有影响，直到浓度高于 5–10 μM。 Rigosertib (100-250 nM) 会导致 HeLa 细胞纺锤体畸变和细胞凋亡[3]。此外，MES-SA、MES-SA/DX5a、CEM 和 CEM/C2a 属于 rigosertib 抑制的多重耐药肿瘤细胞系，IC50 为 50-100 nM。在 DU145 细胞中，rigosertib (0.25–5 μM) 抑制细胞周期的 G2/M 期，导致 subG1 区域 DNA 含量的细胞积聚，并触发细胞凋亡途径。在 A549 细胞中，rigosertib (50 nM-0.5 μM) 会导致 caspase 3/7 激活和活力丧失[4]。 rigosertib 钠 (2 μM) 可诱导慢性淋巴细胞白血病 (CLL) 细胞凋亡，不会对 T 细胞或健康 B 细胞造成伤害。此外，rigosertib 钠 (2 μM) 消除了滤泡树突状细胞对 CLL 细胞的促生存作用，这也减少了 SDF-1 产生的白血病细胞的迁移[5]。
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| 体内研究 (In Vivo) |
rigosertib（250 mg/kg，腹腔注射）可显着抑制 Bel-7402、MCF-7 和 MIA-PaCa 细胞的小鼠异种移植模型中的肿瘤生长[3]。 rigosertib（200 mg/kg，腹腔注射）可抑制小鼠异种移植模型中的 BT20 细胞肿瘤生长[4]。
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| 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. [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 |
| 分子式 |
C21H24NNAO8S
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|---|---|
| 分子量 |
473.47
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| CAS号 |
592542-60-4
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| 相关CAS号 |
Rigosertib;592542-59-1;(E/Z)-Rigosertib sodium;1225497-78-8
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| SMILES |
COC1=CC=C(C=C1NCC([O-])=O)CS(/C=C/C2=C(C=C(C=C2OC)OC)OC)(=O)=O.[Na+]
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| 溶解度 (体外) |
DMSO : 150 mg/mL (316.81 mM)
H2O : ≥ 52 mg/mL (109.83 mM) |
|---|---|
| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 5.25 mg/mL (11.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 52.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5.25 mg/mL (11.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 52.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5.25 mg/mL (11.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (5.28 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (5.28 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: 50 mg/mL (105.60 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 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 |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
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。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
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