Supinoxin(Synonyms: RX-5902)

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Supinoxin (Synonyms: RX-5902) 纯度: 99.90%

Supinoxin (RX-5902) 是磷酸化 p68 RNA 解旋酶 (P-p68) 的强效口服活性抑制剂，并且是首创的抗肿瘤试剂 (anti-cancer agent)。Supinoxin 与 Y593 磷酸化的 p68 相互作用并减弱 β-catenin 的核穿梭性。 Supinoxin 诱导细胞凋亡 (apoptosis) 并抑制 TNBC 癌细胞系的生长，IC50 的范围为 10 nM 至 20 nM。

Supinoxin(Synonyms: RX-5902)

Supinoxin Chemical Structure

CAS No. : 888478-45-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3960 In-stock
5 mg ￥3600 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

Supinoxin 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library

生物活性

Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM[1][2].

IC50 & Target

IC50: phosphorylated-p68 RNA helicase; apoptosis[1]
体外研究
(In Vitro)

RX-5902 (0-10 μM; 72 hours) is active against cell lines of all TNBC molecular subtypes and is active against cell lines with mutations in p53, RB1, CDKN2A, and loss of PTEN[1].
RX-5902 (20-100 nM; 24 hours) treatment results in a dose-dependent increase in tetraploid cells, consistent with induction of G2–M cell-cycle arrest[1].
RX-5902 (0-100 nM; 72 hours) exhibits no significant induction of apoptosis in cell lines resistant to the antiproliferative effects of RX5902. But in sensitive cells, the observed activation of apoptosis begins at 24–48 hours and reaches a peak at 72 hours. The induced apoptosis is greasted with a dose of 100 nM[1].
RX-5902 (0-100 nM; 24 or 48 hours) decreases MCL-1 expression as a dose-dependent manner in TNBC cell lines sensitive to RX-5902[1].
RX-5902 inhibits cell growth, MDA-MB-231, Caki-1, UMRC2, PANC-1, A549, MKN-45, HepG2, HCT116, HT29, PC-3, U251, HeLa, SK-MEL-28 and OVCAR-3 with IC50 values range from 0.01 μM to 0.021 μM in the growth inhibition of cancer cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MDA-MB-231, HCC1806, Hs578t, CAL-85-1, HCC38, HCC1187, MDA-MB-436, CAL-51, HCC38, BT549, MDAMB-157, HDQ-P1, HCC1395, MDA-MB-436, HCC1937, CAL-120, BT20 cells
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Displayed the average IC50 of the cell lines sensitive to RX-5902 treatment is 56 nM.

Cell Cycle Analysis[1]

Cell Line: Sensitive (MDA-MB-231 and HCT1806) and two resistant (MDA-MB-436 and CAL-120) cell lines
Concentration: 20 nM; 100 nM
Incubation Time: 24 hours
Result: Led to G2-M cell-cycle arrest at sensitive cells.

Apoptosis Analysis[1]

Cell Line: Sensitive (MDA-MB-231 and HCT1806) and two resistant (MDA-MB-436 and CAL-120) cell lines
Concentration: 0-100 nM
Incubation Time: 24-72 hours
Result: Induced cell apoptosis in sensitive cell lines and peaks at 72 hours.

Western Blot Analysis[1]

Cell Line: Cal-51, HCC-1806, and MDA-MB-468 cells
Concentration: 20 nM; 100 nM
Incubation Time: 24 hours
Result: Induced inhibition of MCL-1 expression in Cal-51, HCC-1806, and MDA-MB-468 cells.

体内研究
(In Vivo)

RX-5902 (oral administration; 160/320/600 mg/kg; once weekly for 3 weeks) significant dose-dependent tumor growth inhibition (TGI) in the MDA-MB-231 model, exhibits TGI of 55.7%, 80.29% and 94.58% at 160 mg/kg, 320 mg/kg and 600 mg/kg, respectively. It is more efficacious than the chemotherapy control arm of nab-paclitaxel (TGI 45%)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MDAMD-231 xenograft model in mice[1]
Dosage: 160 mg/kg; 320 mg/kg; 600 mg/kg
Administration: Oral administration; once weekly for 3 weeks
Result: Decreased tumor volume as a dose-dependent manner.

Clinical Trial

分子量

441.46

Formula

C22H24FN5O4
CAS 号

888478-45-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (226.52 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2652 mL 11.3261 mL 22.6521 mL
5 mM 0.4530 mL 2.2652 mL 4.5304 mL
10 mM 0.2265 mL 1.1326 mL 2.2652 mL

*

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。-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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.66 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.66 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Kost GC, et al. A Novel Anti-Cancer Agent, 1-(3,5-Dimethoxyphenyl)-4-[(6-Fluoro-2-Methoxyquinoxalin-3-yl)Aminocarbonyl] Piperazine (RX-5902), Interferes With β-Catenin Function Through Y593 Phospho-p68 RNA Helicase.J Cell Biochem. 2015 Aug;116(8):1595-601.

    [2]. Capasso A, et al. First-in-Class Phosphorylated-p68 Inhibitor RX-5902 Inhibits β-Catenin Signaling and Demonstrates Antitumor Activity in Triple-Negative Breast Cancer.Nov;18(11):1916-1925.

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