LKT Labs

Biochemicals for Life Science Research

Lomeguatrib

Product ID L5750
Cas No. 192441-08-0
Purity ≥98%
Product Unit SizeCostQuantityStock
10 mg $78.60 In stock
25 mg $157.40 In stock
100 mg $503.40 In stock
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Description

Lomeguatrib is an anticancer chemotherapeutic compound that is used as a pseudosubstrate for O6-methylguanine-DNA methyltransferase (MGMT), inactivating the enzyme and inhibiting DNA repair across many cancer cell lines. Lomeguatrib is currently in clinical trials as a co-administered compound that increases the efficacy of chemotherapeutics such as temozolomide and dacarbazine in the treatment of melanoma and other solid tumors. In glioblastoma cells, lomeguatrib decreases activity of MGMT and increases expression of p53, inducing DNA fragmentation and apoptosis.

Product Info

Cas No.

192441-08-0

Purity

≥98%
Formula

C10H8BrN5OS
Formula Wt.

326.17
IUPAC Name

6-[(4-bromothiophen-2-yl)methoxy]-7H-purin-2-amine
Appearance

Yellow to white powder

Shipping and Storage

Store Temp

Ambient
Ship Temp

Ambient

Downloads

MSDS

L5750 MSDS PDF
Info Sheet

L5750 Info Sheet PDF

References

Taspinar M, Ilgaz S, Ozdemir M, et al. Effect of lomeguatrib-temozolomide combination on MGMT promoter methylation and expression in primary glioblastoma tumor cells. Tumour Biol. 2013 Jun;34(3):1935-47. PMID: 23519841.

Tawbi HA, Villaruz L, Tarhini A, et al. Inhibition of DNA repair with MGMT pseudosubstrates: phase I study of lomeguatrib in combination with dacarbazine in patients with advanced melanoma and other solid tumours. Br J Cancer. 2011 Sep 6;105(6):773-7. PMID: 21811257.

Watson AJ, Sabharwal A, Thorncroft M, et al. Tumor O(6)-methylguanine-DNA methyltransferase inactivation by oral lomeguatrib. Clin Cancer Res. 2010 Jan 15;16(2):743-9. PMID: 20068091.

Watson AJ, Middleton MR, McGown G, et al. O(6)-methylguanine-DNA methyltransferase depletion and DNA damage in patients with melanoma treated with temozolomide alone or with lomeguatrib. Br J Cancer. 2009 Apr 21;100(8):1250-6. PMID: 19367283.

Khan O, Middleton MR. The therapeutic potential of O6-alkylguanine DNA alkyltransferase inhibitors. Expert Opin Investig Drugs. 2007 Oct;16(10):1573-84. PMID: 17922622.

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