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ML264 

Cat. No.: HY-19994 Purity: 99.67%
Handling Instructions

ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.

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

ML264 Chemical Structure

ML264 Chemical Structure

CAS No. : 1550008-55-3

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 440 In-stock
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100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.

IC50 & Target

KLF5[1]

In Vitro

ML264 is highly active (IC50=29 nM is a cell-based assay for proliferation of DLD-1 cells, IC50=81 nM in a cell-based luciferase assay). ML264 lacks cytotoxicity in the IEC-6 control cell line (IC50>50 μM, <50% inhibition is observed at 100 μM). Robust activity is also seen in several other KLF5-expressing cell types as well (e.g., HCT116, IC50=560 nM; HT29, IC50=130 nM; SW620, IC50=430 nM). Western blot analysis shows that ML264 significantly reduces KLF5 expression[1]. The effects of ML264 are tested on the rate of cell proliferation of colon cancer cells lines DLD-1 and HCT116 over 72 hours. ML264 efficiently inhibits the rate of proliferation of both cell lines. A significant decrease in proliferation is evident within 24 hours of treatment and by 72 hours the live cell numbers of ML264-treated and vehicle-treated cells differed by 15- to 30- fold. An MTS assay that allows the quantification of metabolically active cells is performed. ML264 treatment significantly reduces the number of cells undergoing mitosis in DLD-1 cells at 24, 48 and 72 hours[2].

In Vivo

Single daily injections of ML264 at 10 mg/kg do not significantly affect tumor growth. However, twice daily injections of ML264 at 10 mg/kg or 25 mg/kg result in significant reductions in tumor growth, and this effect can be detected as early as two days after the first injection. The data also show that there is a concentration-dependent effect of ML264 on the tumor volume. Statistical analysis of tumor growth reveals significant tumor size reduction in mice treated twice daily with ML264 compared to those receiving only vehicle at day 5 and 10[2].

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 : ≥ 100 mg/mL (259.82 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5982 mL 12.9911 mL 25.9821 mL
5 mM 0.5196 mL 2.5982 mL 5.1964 mL
10 mM 0.2598 mL 1.2991 mL 2.5982 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 3.25 mg/mL (8.44 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

For cell proliferation experiments, DLD-1 and HCT116 cells are treated with 10 μM ML264 or with vehicle (DMSO). Live cells are collected at 24, 48 and 72 hours post treatment and their numbers are determined by counting using a Coulter counter. Each experiment is done in triplicate. In MTS assay, DLD-1 and HCT116 cells are treated with 10 μM ML264 or with vehicle (DMSO). After 24, 48, and 72 hours of incubations, 20 μL of MTS solution is added to each well and an analysis is performed. The measurement of the control (cells with medium and DMSO) is defined as 100% and the results from other measurements are calculated accordingly. Each experiment is done in sextuplicate. A cell cycle progression assay is performed. Each experiment is done in triplicate. The apoptosis rate is determined using the Alexa Fluor 488 Annexin V/Dead Cell Apoptosis Kit with analysis by flow cytometry. Each experiment is done in triplicate[2].

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

Animal Administration
[2]

Mice[2]
Nude mice are housed under specific pathogen-free conditions in ventilated and filtered cages under positive pressure. Xenograft tumors are generated by injecting subcutaneously 5×106 DLD-1 human colorectal cells into the right flank of 6-7 week old male nude mice. Tumor volume is determined by caliper measurement and calculated by established methods. When tumors reach a volume of about 100 mm6, mice are treated intraperitoneally (i.p.) with varying doses of ML264: 10 mg/kg daily, 10 mg/kg twice per day and 25 mg/kg twice per day, with each treatment regimen lasting for a duration of 10 days. The vehicle solution is used as the control treatment. Mice are monitored and weighed every two days. Experiments are terminated when the tumor’s greatest measurement reaches 2 cm. Tumors are excised and retained for further analyses[2].

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

References
Molecular Weight

384.88

Formula

C₁₇H₂₁ClN₂O₄S

CAS No.

1550008-55-3

SMILES

O=C(NCC(N(C)C(CC1)CCS1(=O)=O)=O)/C=C/C2=CC=CC(Cl)=C2

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
ML264
Cat. No.:
HY-19994
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ML264

Cat. No.: HY-19994