Lomeguatrib

Lomeguatrib Basic information
Product Name:Lomeguatrib
Synonyms:Lomeguatrib;2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine;6-[(4-bromothiophen-2-yl)methoxy]-7H-purin-2-amine;6-((4-Bromo-2-thienyl)methoxy)purin-2-amine;C521206;2-AMino-6-(4-broMothiophen-2-ylMethoxy)-9H-purine;6-[(4-BroMo-2-thienyl)Methoxy] -1H-purin-2-aMine;6-[(4-BroMo-2-thienyl)Methoxy]-9H-purin-2-aMine
CAS:192441-08-0
MF:C10H8BrN5OS
MW:326.17
EINECS:
Product Categories:Inhibitors;Inhibitor of MGMT.;Epigenetics
Mol File:192441-08-0.mol
Lomeguatrib Structure
Lomeguatrib Chemical Properties
Boiling point 683.8±65.0 °C(Predicted)
density 2.07
storage temp. Keep in dark place,Inert atmosphere,2-8°C
solubility DMSO: soluble10mg/mL, clear
form powder
pka9.42±0.10(Predicted)
color white to beige
Stability:Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Safety Information
Hazard Codes Xn
Risk Statements 22
WGK Germany 3
RTECS UO7420000
MSDS Information
Lomeguatrib Usage And Synthesis
DescriptionLomeguatrib (192441-08-0) is a potent (IC50?= 9 nM) inhibitor of O6-Methylguanine-DNA Methyltransferase (MGMT), an important DNA repair protein.1?It is currently being investigated in cancers that have acquired resistant to the chemotherapeutic temozolomide2-5, as well as other chemotherapeutics6,7.
UsesO6-Methylguanine-DNA methyltransferase (MGMT) is a DNA repair protein which removes an alkyl group from the O6 position on guanine in an autoinactivating reaction. Although important in normal DNA repair, this reaction confers resistance to treatments that use O6-alkylating agents to produce cytotoxicity, e.g., in cancer. Lomeguatrib is a modified quanine base which acts as a pseudosubstrate inactivator of MGMT (IC50 = ~3 nM). A non-toxic compound, lomeguatrib completely inactivates MGMT in human prostate and colorectal tumors when given as a single 120 mg oral dose and in primary central nervous system cancers at 160 mg.
UsesLomeguatrib is an inhibitor of O6-methylguanine-DNA methyltransferase (MGMT). Lomeguatrib attenuates MGMT activity in vitro and in vivo. Lomeguatrib enhances the antitumor activity of temozolomide in both human melanoma and MCF-7 xenografts.
storage+4°C
References1) 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 2) 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 3) Gumbrell?et al.?(2006),?Lomeguatrib, a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase: phase I safety, pharmacodynamic, and pharmacokinetic trial and evaluation in combination with temozolomide in patients with advanced solid tumors: Clin. Cancer Res.?12?1577 4) Watson?et al.?(2009),?O(6)-methylguanine-DNA methyltransferase depletion and DNA damage in patients with melanoma treated with temozolomide alone or with lomeguatrib: Br. J. Cancer?100?1250 5) Taspinar?et al.?(2013),?Effect of lomeguatrib-temozolomide combination of MGMT promoter methylation and expression in primary glioblastoma tumor cells: Tumour Biol.?34?1935 6) Sabharwal?et al.?(2010),?A phase I trial of lomeguatrib and irinotecan in metastatic colorectal cancer: Cancer Chemother. Pharmacol.?66?829 7) Tawbi?et al.?(2011),?Inhibition of DNA repair with MGMT pseudosubstrates: phase I study of lomeguatrib in combination with dacarbazine in patients with advanced melanoma and other solid tumors: Br. J. Cancer?105?773
Lomeguatrib Preparation Products And Raw materials
Lomeguatrib Lomefloxacin Methoxy ALTRENOGEST POLY(ETHYLENE GLYCOL) METHYL ETHER ACRYLATE Anisole (Trifluoromethoxy)benzene 6-Aminocaproic acid Glycine Lomefloxacin hydrochloride Purine p-Anisic acid p-Anisidine Methoxyacetic acid p-Anisaldehyde Bromine Tris(hydroxymethyl)aminomethane AMINO ACIDS

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