Name | Lomeguatrib |
Synonyms | C521206 Lomeguatrib 6-((4-Bromo-2-thienyl)methoxy)purin-2-amine 6-[(4-BroMo-2-thienyl)Methoxy]-1H-purin-2-aMine 6-[(4-BroMo-2-thienyl)Methoxy]-9H-purin-2-aMine 2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine 2-AMino-6-(4-broMothiophen-2-ylMethoxy)-9H-purine 6-[(4-bromothiophen-2-yl)methoxy]-7H-purin-2-amine |
CAS | 192441-08-0 |
InChI | InChI=1/C10H8BrN5OS/c11-5-1-6(18-3-5)2-17-9-7-8(14-4-13-7)15-10(12)16-9/h1,3-4H,2H2,(H3,12,13,14,15,16) |
Molecular Formula | C10H8BrN5OS |
Molar Mass | 326.17 |
Density | 2.07 |
Boling Point | 683.8±65.0 °C(Predicted) |
Flash Point | 367.3°C |
Solubility | DMSO: soluble10mg/mL, clear |
Vapor Presure | 1.5E-18mmHg at 25°C |
Appearance | powder |
Color | white to beige |
pKa | 9.42±0.10(Predicted) |
Storage Condition | Keep in dark place,Inert atmosphere,2-8°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
Refractive Index | 1.797 |
In vitro study | Lomeguatrib inhibits OLomeguatrib from acting on MCF-7 cells and effectively inhibits MGMT with an IC50 of 6nm. Lomeguatrib (10 μm) significantly increased the growth inhibitory effect of Temozolomide on MCF-7 cells (D60 of 10 μm in combination with Lomeguatrib and 400 μm alone). |
In vivo study | The combination of Lomeguatrib (20 mg/kg/day for 5 days) and Temozolomide (100 mg/kg/day for 5 days) significantly delayed tumor growth, the time to five-fold the mean tumor size was increased by 22 days without any significant increase in cytotoxicity. Treatment of A375M human melanoma xenograft model with Lomeguatrib inhibits ATase activity and enhances the antitumor effect of Temozolomide. The tumor was treated with Lomeguatrib at a dose of 20 mg/kg intraperitoneally alone, and the ATase was completely depleted within 2 hours. Treatment of A375M xenografts with Temozolomide at a dose of 100 g/kg per day significantly delayed tumor growth and prolonged the five-fold change in tumor size to 9.6 days. The addition of Lomeguatrib to Temozolomide significantly enhanced the latter's effect, turning the time it took for the tumor to fivefold in size to 8.7 days. In addition, Lomeguatrib in combination with Temozolomide produced considerably less toxicity (0/9 vs. 2/9 deaths; 6.84 weight loss vs. 9.48%). Lomeguatrib alone had no significant effect on tumor growth. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
WGK Germany | 3 |
RTECS | UO7420000 |
biological activity | Lomeguatrib (PaTrin-2) is an effective O6-alkylguanine-DNA-alkyltransferase inhibitor with IC50 of 5 nM. |
Target | Value |
O6-alkylguanine-DNA-alkyltransferas () | 5 nM |