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ML264 KLF inhibitor

Name: ML264
SKU: S8196
Availability: InStock
Rating: 5 (10 reviews)

Cat.No.S8196

ML264 (CID-51003603), a selectively inhibitor of kruppel-like factor 5 (KLF5), potently inhibits growth of colorectal cancer.

Chemical Structure

Molecular Weight: 384.88

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.75%

99.75

Related Targets	Ras ERK p38 MAPK Raf JNK MEK S6 Kinase MAP4K TAK1 Mixed Lineage Kinase ASK MNK MAPKAPK2 TOPK
Related Products	SR18662 KLF4 Antibody [K21G5]

Chemical Information, Storage & Stability

Molecular Weight	384.88	Formula	C₁₇H₂₁ClN₂O₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1550008-55-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CID-51003603			Smiles	CN(C1CCS(=O)(=O)CC1)C(=O)CNC(=O)C=CC2=CC(=CC=C2)Cl

Solubility

In vitro
Batch:

DMSO : 200 mg/mL (519.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.800mg/ml (9.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 76 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	KLF5 ^[1] (Cell-based assay for proliferation of DLD-1 cells) 29 nM
In vitro	ML264 potently halts DLD-1 viability (IC50 = 29 nM) with high maximal effect (>90%). DLD-1 cells are human colorectal adenocarcinoma cells. This compound has significant effects at submicromolar doses on other cell types as well, including HCT116 (human colorectal carcinoma), HT29 (human colorectal adenocarcinoma), and SW620 (human colorectal adenocarcinoma). The IEC-6 anti-target (a nontransformed rat intestinal epithelial cell line) is largely unaffected, with inhibition below 50% at the highest dose^[1].This compound potently inhibits proliferation of CRC cells in vitro through modifications of the cell cycle profile^[2].
In vivo	In an established xenograft mouse model of colon cancer, ML264 efficiently inhibits growth of the tumor within five days of treatment. This effect is caused by a significant reduction in proliferation and that this compound potently inhibits the expression of KLF5 and EGR1, a transcriptional activator of KLF5^[2].
References	[1] https://pubmed.ncbi.nlm.nih.gov/23762940/ [2] https://pubmed.ncbi.nlm.nih.gov/26621868/

Tech Support

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