1. MAPK/ERK Pathway
  2. KLF
  3. SR18662

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

For research use only. We do not sell to patients.

SR18662 Chemical Structure

SR18662 Chemical Structure

CAS No. : 2505001-62-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 200 In-stock
25 mg USD 400 In-stock
50 mg USD 640 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

SR18662 is a potent inhibitor of Krüppel-like factor five (KLF5) with an IC50 of 4.4 nM and 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

CAS No.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (297.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (4.95 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.08 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3792 mL 11.8960 mL 23.7920 mL 59.4799 mL
5 mM 0.4758 mL 2.3792 mL 4.7584 mL 11.8960 mL
10 mM 0.2379 mL 1.1896 mL 2.3792 mL 5.9480 mL
15 mM 0.1586 mL 0.7931 mL 1.5861 mL 3.9653 mL
20 mM 0.1190 mL 0.5948 mL 1.1896 mL 2.9740 mL
25 mM 0.0952 mL 0.4758 mL 0.9517 mL 2.3792 mL
30 mM 0.0793 mL 0.3965 mL 0.7931 mL 1.9827 mL
40 mM 0.0595 mL 0.2974 mL 0.5948 mL 1.4870 mL
50 mM 0.0476 mL 0.2379 mL 0.4758 mL 1.1896 mL
60 mM 0.0397 mL 0.1983 mL 0.3965 mL 0.9913 mL
80 mM 0.0297 mL 0.1487 mL 0.2974 mL 0.7435 mL
100 mM 0.0238 mL 0.1190 mL 0.2379 mL 0.5948 mL
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SR18662 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SR18662
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