SR18662 - KKL Med Inc.

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SR18662

目录号 : KM7279 纯度 : 98%

Data Sheet 产品使用指南

SR18662 是一种有效的 Kruppel-like factor 5 (KLF5) 的抑制剂， IC₅₀ 为 4.4 nM，ML264 的类似物。SR18662 可用于结直肠癌的相关研究。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

SR18662 is a potent inhibitor of Krüppel-like factor five (KLF5) with an IC₅₀ of 4.4 nM and an analogue of ML264 with improved inhibitory potency against colorectal cancer cells. SR18662 can be used for the study of colorectal cancer.

体外研究

SR18662 (0-10 μM; 24-72 hours) significantly reduces growth and proliferation of CRC cells as compared to treatment with vehicle control, ML264 . It shows improved efficacy in reducing viability of multiple CRC cell lines.
SR18662 (10 μM; 24-72 hours) shows a significant increase in the number of apoptotic cells at both early and late states in DLD-1 and HCT116 cells.
SR18662 (1 μM; 72 hours) reduces the expression of cyclins (cyclins E, A2, and B1) and components of MAPK (p-Erk) and WNT signaling pathways (p-GSK3 β) in cells.

Cell Viability Assay

Cell Line:	CRC cells
Concentration:	0-10 μM
Incubation Time:	24 hours, 48 hours, 72 hours
Result:	Induced anti-tumor activity in colorectal cancer cell lines.

Apoptosis Analysis

Cell Line:	DLD-1 and HCT116 cells
Concentration:	10 μM
Incubation Time:	24 hours, 48 hours, 72 hours
Result:	Increased apoptosis of colorectal cancer cell lines.

Western Blot Analysis

Cell Line:	DLD-1 and HCT116 cells
Concentration:	1 μM
Incubation Time:	72 hours
Result:	Reduced levels of cyclins E, A2, and B1 inhibits activity of MAPK, WNT/β-catenin signaling pathways and decreases the levels of cyclins.

体内研究

SR18662 (intraperitoneal injection; 5-10 mg/kg; daily or twice daily; 5 days injection, days break, and 5 days) significantly reduces the growth of tumors in a mouse xenograft model.

Animal Model:	Nude mice with DLD-1 cells
Dosage:	5 mg/kg; 10 mg/kg; 25 mg/kg
Administration:	Intraperitoneal injection; 5mg/kg daily, 5mg/kg twice a day,10 mg/kg daily, 10 mg/kg twice per day, 25mg/kg daily, and 25 mg/kg twice per day; 5 days of injections, 2 days break, and 5 days of injections
Result:	Caused a significant dose-dependent inhibition of xenograft growth in mice.

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 : 125 mg/mL (297.40 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3792 mL	11.8960 mL	23.7920 mL
5 mM	0.4758 mL	2.3792 mL	4.7584 mL
10 mM	0.2379 mL	1.1896 mL	2.3792 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: 2.08 mg/mL (4.95 mM); Clear solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.95 mM) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.95 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.95 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。