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SR18662 

目录号: HY-136530 纯度: 98.09%
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 (HY-19994) 的类似物。SR18662 可用于结直肠癌治疗的相关研究。

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SR18662 Chemical Structure

SR18662 Chemical Structure

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Size Price Stock Quantity
10 mM * 1  mL in DMSO ¥3300 In-stock
5 mg ¥3000 In-stock
10 mg ¥4800 In-stock
50 mg ¥14000 In-stock
100 mg ¥21000 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

SR18662 is a potent inhibitor of Krüppel-like factor five (KLF5) with an IC50 of 4.4 nM, an analogue of ML264 (HY-19994) with improved inhibitory potency against colorectal cancer cells. SR18662 can be used for the study of colorectal cancer[1].

IC50 & Target

IC50: 4.4 nM (KLF5)[1]

In Vitro

SR18662 (0-10 μM; 24-72 hours) significantly reduces growth and proliferation of CRC cells as compared to treatment with vehicle control, ML264 (HY-19994). It shows improved efficacy in reducing viability of multiple CRC cell lines[1].
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[1].
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[1].

Cell Viability Assay[1]

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[1]

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[1]

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.
In Vivo

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[1].

Animal Model: Nude mice with DLD-1 cells[1]
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.
Molecular Weight

420.31

Formula

C₁₆H₁₉Cl₂N₃O₄S

SMILES

ClC1=CC(/C=C/C(NCC(N2CCN(CC2)S(C)(=O)=O)=O)=O)=CC=C1Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 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。

    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: ≥ 2.08 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。

*以上所有助溶剂都可在 MCE 网站选购。
References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

SR18662SR 18662SR-18662Otherscolorectal cancerDLD-1HCT116SW620HT29ML264analogueInhibitorinhibitorinhibit

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