Lomeguatrib

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Cat.No. 4359 - Lomeguatrib | C10H8BrN5OS | CAS No. 192441-08-0
Description: MGMT inhibitor
Alternative Names: PaTrin-2
Chemical Name: 6-[(4-Bromo-2-thienyl)methoxy]-9H-purin-2-amine
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Inhibitor of O6-methylguanine-DNA methyltransferase (MGMT); (IC50 = 0.009 μM in cell-free extracts from HeLa S3 cells); attenuates MGMT activity in vitro and in vivo. Enhances the antitumor activity of temozolomide (Cat. No. 2706) in both human melanoma and MCF-7 xenografts.

Compound Libraries

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Technical Data

M. Wt 326.17
Formula C10H8BrN5OS
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 192441-08-0
PubChem ID 3025944
InChI Key JUJPKFNFCWJBCX-UHFFFAOYSA-N
Smiles NC1=NC(OCC3=CC(Br)=CS3)=C2C(N=CN2)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 32.62 100

Preparing Stock Solutions

The following data is based on the product molecular weight 326.17. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.07 mL 15.33 mL 30.66 mL
5 mM 0.61 mL 3.07 mL 6.13 mL
10 mM 0.31 mL 1.53 mL 3.07 mL
50 mM 0.06 mL 0.31 mL 0.61 mL

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References

References are publications that support the biological activity of the product.

Reinhard et al (2001) Monosaccharide-linked inhibitors of O6-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships. J.Med.Chem. 44 4050 PMID: 11708909

Barvaux et al (2004) Sensitization of a human ovarian cancer cell line to temozolomide by simultaneous attenuation of the Bcl-2 antiapoptotic protein and DNA repair by O6-alkylguanine-DNA alkyltransferase. Mol.Cancer Ther. 3 1215 PMID: 15486188

Clemons et al (2005) O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumor MCF-7 cells and xenografts. Br.J.Cancer 93 1152 PMID: 16278661


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Keywords: Lomeguatrib, Lomeguatrib supplier, dna, mgmt, o6-methylguanine-dna, methyltransferases, inhibitors, inhibits, psuedosubstrates, epigenetics, PaTrin-2, DNA, Methyltransferases, 4359, Tocris Bioscience

Citations for Lomeguatrib

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Literature in this Area

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Cancer

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Epigenetics Scientific Review

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