Lomeguatrib (Synonyms: PaTrin-2)

Name: Lomeguatrib
Brand: MedChemExpress
SKU: HY-13668
Rating: 5.0 (6 reviews)

Cat. No.: HY-13668 Purity: 99.77%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Lomeguatrib is a O⁶-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC₅₀s of 9 nM in cell-free assay and ～6?nM in MCF-7 cells.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Lomeguatrib 화학구조

CAS No. : 192441-08-0

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 6 publication(s) in Google Scholar

6 Publications Citing Use of MCE Lomeguatrib

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DNA Methyltransferase DNMT1 DNMT3 MGMT

Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

Lomeguatrib is a O⁶-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC₅₀s of 9 nM in cell-free assay and ～6?nM in MCF-7 cells.

IC₅₀ & Target^[1]^[2]

MGMT

6 nM (IC₅₀, in MCF-7 cells)

MGMT

9 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	0.009 μM Compound: 10	In vitro inhibition of MGMT using cell free extracts from HeLa S3 cells In vitro inhibition of MGMT using cell free extracts from HeLa S3 cells	[PMID: 11708909]

In Vitro

Lomeguatrib (Compound 10) is a O⁶-methylguanine methyltransferase (MGMT) inhibitor, with an IC₅₀ of 9 nM in cell-free assay^[1] and ～6?nM in MCF-7 cells. 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].

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

In Vivo

Lomeguatrib (20?mg/kg i.p.) completely inactivates MGMT within 2?h, but shows no significant effect on tumor growth in MCF-7 xenografts^[2].

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

분자량

326.17

화학식

C₁₀H₈BrN₅OS

CAS No.

192441-08-0

Appearance

Solid

Color

White to light yellow

SMILES

NC1=NC(OCC2=CC(Br)=CS2)=C3N=CNC3=N1

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

용액&용해도

In Vitro:

DMSO : ≥ 56 mg/mL (171.69 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.0659 mL	15.3294 mL	30.6589 mL
5 mM	0.6132 mL	3.0659 mL	6.1318 mL
10 mM	0.3066 mL	1.5329 mL	3.0659 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

몰농도 계산기
농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.77%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (250 KB) RP-HPLC (248 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Reinhard J, et al. Monosaccharide-linked inhibitors of O(6)-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships. J Med Chem. 2001 Nov 22;44(24):4050-61. [Content Brief]

[2]. Clemons M, et al. O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts. Br J Cancer. 2005 Nov 14;93(10):1152-6. [Content Brief]

Kinase Assay ^[1]	Briefly, 200 μg of extracted cellular protein from HeLaS3 cells in 200 μL of 70 mM HEPES buffer (with 1 mM dithiothreitol (DTT), 5 mM EDTA, pH 7.8) is incubated at 37°C with a defined concentration of Lomeguatrib (added as a DMSO solution). After 30 min an excess of [³H]-methylated DNA (120 000 cpm) is added, and the incubation is continued for an additional 90 min. The reaction is stopped by the addition of 400 μL TCA (13%), and the DNA is hydrolyzed by heating the reaction mixture for 30 min at 98°C. The precipitated protein is washed three times with 400-μL portions of 5% TCA, solubilized in 0.1 N NaOH, and analyzed by liquid scintillation counting using the cocktail Rotiszint eco plus and a TRI-CARB. Enzyme activity is expressed as fmol of [³H]methyl transferred to TCA-insoluble protein material per mg of total cellular protein. Percent inhibition is calculated relative to untreated control samples. Each assay is repeated three times, and IC₅₀ values are determined graphically from plots of percent inhibition vs inhibitor concentration^[1]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
Cell Assay ^[2]	To determine toxicity, the MTT growth inhibition assay is employed. Cells (1000 per well) are plated into a 96-well plate and following a 24 h attachment period, Lomeguatrib is added to the cells. After 2 h incubation with Lomeguatrib (10 μM) at 37°C, 5% CO₂, increasing doses of temozolomide or vehicle are added and the cells are incubated for a further 4-5 days. At the end of the exposure period, 150 μg MTT is added to each well and plates are incubated for 3 h at 37°C, 5% CO₂. The media are removed and the formazan crystals formed in the viable cells are solubilised in 200 μL DMSO. The absorbances at 540 and 690 nm are determined using a ELISA plate reader and growth inhibition calculated as a percentage of the A540-A690 of untreated wells^[2]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
Animal Administration ^[2]	Mice^[2] To assess the ability of Lomeguatrib to sensitise human breast tumour xenografts to the tumour growth inhibitory effects of temozolomide, groups of at least six nude mice are treated as follows: the vehicle control group are given corn oil then 20% DMSO in PBS; the temozolomide only group are given corn oil then temozolomide (100 mg/kg/day); the Lomeguatrib only group are given Lomeguatrib (20 mg/kg/day) then DMSO in PBS, and the Lomeguatrib plus temozolomide group are given Lomeguatrib (20 mg/kg/day) then temozolomide (100 mg/kg/day). Drugs or vehicles are administered i.p. once daily for 5 days with a separation of 1 h. Up to 10 and at least six animals are assigned to each group, and mean tumour volume is standardised across the groups at the start of the experiment: thus the control, Lomeguatrib, temozolomide and Lomeguatrib plus temozolomide groups had mean tumour volumes of 29.8±7.6 (range 19.0-38.7), 33.2±14.7 (range 16.5-58.7), 35.1±10.9 (range 20.9-52.4) and 30.3±10.0 (range 20.7-44.5) mm³, respectively^[2]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
References	[1]. Reinhard J, et al. Monosaccharide-linked inhibitors of O(6)-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships. J Med Chem. 2001 Nov 22;44(24):4050-61. [Content Brief] [2]. Clemons M, et al. O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts. Br J Cancer. 2005 Nov 14;93(10):1152-6. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0659 mL	15.3294 mL	30.6589 mL	76.6471 mL
	5 mM	0.6132 mL	3.0659 mL	6.1318 mL	15.3294 mL
	10 mM	0.3066 mL	1.5329 mL	3.0659 mL	7.6647 mL
	15 mM	0.2044 mL	1.0220 mL	2.0439 mL	5.1098 mL
	20 mM	0.1533 mL	0.7665 mL	1.5329 mL	3.8324 mL
	25 mM	0.1226 mL	0.6132 mL	1.2264 mL	3.0659 mL
	30 mM	0.1022 mL	0.5110 mL	1.0220 mL	2.5549 mL
	40 mM	0.0766 mL	0.3832 mL	0.7665 mL	1.9162 mL
	50 mM	0.0613 mL	0.3066 mL	0.6132 mL	1.5329 mL
	60 mM	0.0511 mL	0.2555 mL	0.5110 mL	1.2775 mL
	80 mM	0.0383 mL	0.1916 mL	0.3832 mL	0.9581 mL
	100 mM	0.0307 mL	0.1533 mL	0.3066 mL	0.7665 mL

Lomeguatrib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lomeguatrib192441-08-0PaTrin-2PaTrin2PaTrin 2DNA MethyltransferaseDNMTsDNA MTasesInhibitorinhibitorinhibit

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Lomeguatrib (Synonyms: PaTrin-2)

고객리뷰

Lomeguatrib Related Antibodies

6 Publications Citing Use of MCE Lomeguatrib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All DNA Methyltransferase Isoform Specific Products:

Biological Activity

Protocol

순도&문서

References

고객리뷰

Lomeguatrib Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Lomeguatrib Related Classifications

Keywords:

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고객리뷰

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SAFETY DATA SHEET (SDS)

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