[CAS NO. 1550008-55-3]  ML264

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PRODUCTS SPECIFICATIONS [1550008-55-3]

Catalog
HY-19994
Brand
MCE
CAS
1550008-55-3

DESCRIPTION [1550008-55-3]

Overview

MDLMFCD30187519
Molecular Weight384.88
Molecular FormulaC17H21ClN2O4S
SMILESO=C(NCC(N(C)C(CC1)CCS1(=O)=O)=O)/C=C/C2=CC=CC(Cl)=C2

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


Summary

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 (IC 50 =29 nM is a cell-based assay for proliferation of DLD-1 cells, IC 50 =81 nM in a cell-based luciferase assay). ML264 lacks cytotoxicity in the IEC-6 control cell line (IC 50 >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, IC 50 =560 nM; HT29, IC 50 =130 nM; SW620, IC 50 =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] .

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


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] .

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


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 : ≥ 100 mg/mL ( 259.82 mM )

* "≥" 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 available by MCE.