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SR18662 

Cat. No.: HY-136530 Purity: 98.09%
Handling Instructions

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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1400 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
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 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].

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
*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 provided by MCE.
References
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Keywords:

SR18662SR 18662SR-18662KLFKrüppel-like factorcolorectal cancerDLD-1HCT116SW620HT29ML264analogueInhibitorinhibitorinhibit

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SR18662
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