Lomeguatrib

Research use only, not for human use.

Lomeguatrib, a modified guanine base, inhibits the activity of DNA repair protein O(6)-alkylguanine-DNA alkyltransferase (MGMT) .

Lomeguatrib, also known as PaTrin-2, is a potent Inhibitor of O6-Alkylguanine-DNA-Alkyltransferase. Lomeguatrib is also a nontoxic low-molecular weight pseudosubstrate that has the ability to inactivate MGMT. Lomeguatrib can be used with temozolomide (TMZ) for GBM treatment.(In Vitro):Lomeguatrib (Compound 10) is a O6-methylguanine methyltransferase (MGMT) inhibitor, with an IC50 of 9 nM in cell-free assay 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).(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.

Lomeguatrib (Compound 10) is a O6-methylguanine methyltransferase (MGMT) inhibitor, with an IC50 of 9 nM in cell-free assay 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).

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

PaTrin 2 | PaTrin2 | PaTrin-2 | Lomeguatrib

Microbiology/Virology

Antifungal

O6-alkylguanine-DNA-alkyltransferas

Cancer

——

192441-08-0

326.17

C10H8BrN5OS

>98% (HPLC)

DMSO : ≥ 56 mg/mL; 171.69 mM

Nc1nc2c([nH]cn2)c(OCc2cc(Br)cs2)n1

2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine

(-20℃)

With Ice Pack

≥ 2 years