Supinoxin - CAS:888478-45-3

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Supinoxin (Synonyms:RX-5902)

目录号 : KM9586 CAS No. : 888478-45-3 纯度 : 98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
5mg		In-stock
10mg	询价	In-stock
50mg	询价	In-stock

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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.

体外研究

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.
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.
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.
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.
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.

Cell Viability Assay

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

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

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

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

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%).

Animal Model:	MDAMD-231 xenograft model in mice
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.

分子式

C₂₂H₂₄FN₅O₄

分子量

441.46

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。
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。

临床试验

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

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

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

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浓度

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