NCGC00378430|cas:920650-00-6|西域试剂

NCGC00378430,99.76%

产品编号：Bellancom-138657| CAS NO：920650-00-6| 分子式：C₂₂H₂₃N₃O₅S| 分子量：441.50

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-138657	￥2500.00	杭州北京（现货）
Bellancom-138657	￥4000.00	杭州北京（现货）
Bellancom-138657	￥8500.00	杭州北京（现货）
Bellancom-138657	￥13500.00	杭州北京（现货）
Bellancom-138657	￥19500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

NCGC00378430

产品介绍

NCGC00378430 是一种有效的 SIX1/EYA2 相互作用抑制剂。NCGC00378430 部分逆转 SIX1 过表达介导的转录和代谢谱，并逆转 SIX1 诱导的 TGF-β 信号传导和上皮-间质转化 (EMT)。NCGC00378430 在小鼠模型中抑制 SIX1 介导的乳腺癌转移。

生物活性

NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model.

体外研究

NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor with an IC₅₀ of 52 μM in the Alphascreen assay.
NCGC00378430 (20 μM; 3 days) blocks TGF-β induced activation of p-Smad3, upregulation of FN1, and downregulation of E-CAD in T47D cells.
NCGC00378430 (10 μM; 3 days) reverses the Sine oculis homeobox homolog 1 (SIX1)-induced increase in p-SMAD3 and does not alter total E-CAD levels. NCGC00378430 restores membranous E-CAD in MCF7-SIX1 cells, along with inhibiting FN1 expression.
NCGC00378430 (10 or 20 μM) disrupts SIX1-EYA2 interaction in breast cancer cells (MCF7, T47D, MDA-MB-231 cells).
NCGC00378430 (10 μM; for 3 days) partially reverses SIX1-mediated transcriptional and metabolic signatures in MCF7 breast tumor cells.

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

Western Blot Analysis

Cell Line:	T47D cells
Concentration:	20 μM
Incubation Time:	3 days
Result:	Blocked TGF-β induced activation of p-Smad3, upregulation of FN1, and downregulation of E-CAD.

体内研究
(In Vivo)

NCGC00378430 (25 mg/kg; local injection to the site of tumor; every other day; from day 3 until the day 21) dramatically decreases distant metastatic burden compared to vehicle treatment.
NCGC00378430 (20 mg/kg; IV) has a T_1/2α of 0.25 hours.

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

Animal Model:	6-8 week old NSG mice with MCF7 tumor cells
Dosage:	25 mg/kg
Administration:	Local Injection to the site of tumor; every other day; from day 3 until the day 21
Result:	Dramatically decreased distant metastatic burden compared to vehicle treatment. Had no growth inhibitory effect.

Animal Model:	Mice
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	IV
Result:	Had a T_1/2α of 0.25 hours, a CL of 6.19 L/hr•kg, a V_ss of 4.08 L/kg, a C_max of 6703 ng/mL and an AUC of 3234 ng/mL•hr.

体内研究

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

Animal Model:	6-8 week old NSG mice with MCF7 tumor cells
Dosage:	25 mg/kg
Administration:	Local Injection to the site of tumor; every other day; from day 3 until the day 21
Result:	Dramatically decreased distant metastatic burden compared to vehicle treatment. Had no growth inhibitory effect.

Animal Model:	Mice
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	IV
Result:	Had a T_1/2α of 0.25 hours, a CL of 6.19 L/hr•kg, a V_ss of 4.08 L/kg, a C_max of 6703 ng/mL and an AUC of 3234 ng/mL•hr.

体内研究

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

Animal Model:	6-8 week old NSG mice with MCF7 tumor cells
Dosage:	25 mg/kg
Administration:	Local Injection to the site of tumor; every other day; from day 3 until the day 21
Result:	Dramatically decreased distant metastatic burden compared to vehicle treatment. Had no growth inhibitory effect.

Animal Model:	Mice
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	IV
Result:	Had a T_1/2α of 0.25 hours, a CL of 6.19 L/hr•kg, a V_ss of 4.08 L/kg, a C_max of 6703 ng/mL and an AUC of 3234 ng/mL•hr.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (226.50 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2650 mL	11.3250 mL	22.6501 mL
5 mM	0.4530 mL	2.2650 mL	4.5300 mL
10 mM	0.2265 mL	1.1325 mL	2.2650 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 40% PEG300 5% Tween-80 45% 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 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
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。