[CAS NO. 2505001-62-5]  SR18662

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PRODUCTS SPECIFICATIONS [2505001-62-5]

Catalog
HY-136530
Brand
MCE
CAS
2505001-62-5

DESCRIPTION [2505001-62-5]

Overview

MDL-
Molecular Weight420.31
Molecular FormulaC16H19Cl2N3O4S
SMILESClC1=CC(/C=C/C(NCC(N2CCN(CC2)S(C)(=O)=O)=O)=O)=CC=C1Cl

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

Summary

SR18662 is a potent inhibitor of Krüppel-like factor five (KLF5) with an IC 50 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] .

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] .

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.

Appearance

Solid


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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.