Lomeguatrib , 98% , 192441-08-0

Synonym(s):
2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine;O6-(4-bromothenyl)guanine

CAS NO.：192441-08-0

Empirical Formula: C10H8BrN5OS

Molecular Weight: 326.17

MDL number: MFCD23703756

PRODUCT 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
• pka: 9.42±0.10(Predicted)
• form: powder
• 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.

Description and Uses

Lomeguatrib (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.

O6-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.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P280-P305+P351+P338
• Hazard Codes: Xn
• Risk Statements: 22
• WGK Germany: 3
• RTECS: UO7420000