Home DNA Damage/DNA Repair DNA alkylator inhibitor Lomeguatrib For research use only.

Lomeguatrib

Synonyms: PaTrin-2

Lomeguatrib (PaTrin-2) is a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase with IC50 of 5 nM.

Lomeguatrib Chemical Structure

Lomeguatrib Chemical Structure

CAS: 192441-08-0

Selleck's Lomeguatrib has been cited by 8 Publications

2 Customer Reviews

Purity & Quality Control

Batch: S805601 DMSO] 65 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.89%
99.89

Lomeguatrib Related Products

Choose Selective DNA alkylator Inhibitors

Biological Activity

Description Lomeguatrib (PaTrin-2) is a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase with IC50 of 5 nM.
Targets
O6-alkylguanine-DNA-alkyltransferas [1]
5 nM
In vitro
In vitro Lomeguatrib inactivates O6-alkylguanine-DNA-alkyltransferase (ATase) with a IC50 10-fold lower than O6-Benzylguanine. Lomeguatrib inhibits the activity of ATase in Raji cells with IC50 of 10 nM. [1] Lomeguatrib effectively inactivates MGMT in MCF-7 cells with IC50 of ~6nM ). Lomeguatrib (10 μM ) substantially increases the growth inhibitory effects of temozolomide in MCF-7 cells (D60= 10 μM with Lomeguatrib vs 400 μM without). [2]
In Vivo
In vivo Lomeguatrib (20 mg/kg/day for 5 days) combined with temozolomide (100 mg/kg/day for 5 days) produces a substantial tumour growth delay: median tumour quintupling time is increased by 22 days without any significant increase in toxicity, while neither of the two drugs administrated along show any antitumor activity. [2] Lomeguatrib inactivates ATase and enhances the anti-tumour effect of temozolomide in A375M human melanoma xenografts model. Lomeguatrib, at a single dose of 20 mg/kg i.p., produces complete ATase depletion in tumor within 2 hr. Temozolomide (100 g/kg/day) significantly delays growth of the A375M tumour xenograft with an estimated delay in the time for tumour to quintuple in size of 9.6 days. Addition of Lomeguatrib to temozolomide significantly enhances the latter’s effect, delaying the quintupling time a further 8.7 days. Moreover, the Lomeguatrib combination results in considerably less toxicity (0/9 vs. 2/9 deaths; 6.84% weight loss vs. 9.48%). Lomeguatrib alone has no significant effect on tumour growth. [3]

Chemical Information & Solubility

Molecular Weight 326.17 Formula

C10H8BrN5OS
CAS No. 192441-08-0 SDF Download Lomeguatrib SDF
Smiles C1=C(SC=C1Br)COC2=NC(=NC3=C2NC=N3)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 65 mg/mL ( (199.28 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Lomeguatrib | Lomeguatrib supplier | purchase Lomeguatrib | Lomeguatrib cost | Lomeguatrib manufacturer | order Lomeguatrib | Lomeguatrib distributor