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192441-08-0,MFCD23703756
Catalog No.:AA002FVW

192441-08-0 | Lomeguatrib

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5mg
≥98%
in stock  
$55.00   $38.00
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10mg
≥98%
in stock  
$96.00   $67.00
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25mg
≥98%
in stock  
$209.00   $146.00
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50mg
≥98%
in stock  
$393.00   $275.00
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  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA002FVW
Chemical Name:
Lomeguatrib
CAS Number:
192441-08-0
Molecular Formula:
C10H8BrN5OS
Molecular Weight:
326.1724
MDL Number:
MFCD23703756
SMILES:
Brc1csc(c1)COc1nc(N)nc2c1nc[nH]2
Properties
Computed Properties
 
Complexity:
299  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
18  
Hydrogen Bond Acceptor Count:
6  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
3  
XLogP3:
2  

Downstream Synthesis Route

[1]JournalofMedicinalChemistry,2001,vol.44,p.4050-4061

[2]Patent:CN106083854,2016,A.Locationinpatent:Paragraph0056-0061;0081-0086;0106-0111;0131-0136;0156

Literature

Title: 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.

Journal: British journal of cancer 20110906

Title: Towards more specific O6-methylguanine-DNA methyltransferase (MGMT) inactivators.

Journal: Bioorganic & medicinal chemistry 20110301

Title: A phase I trial of lomeguatrib and irinotecan in metastatic colorectal cancer.

Journal: Cancer chemotherapy and pharmacology 20101001

Title: Tumor O(6)-methylguanine-DNA methyltransferase inactivation by oral lomeguatrib.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20100115

Title: A phase I study of extended dosing with lomeguatrib with temozolomide in patients with advanced melanoma.

Journal: British journal of cancer 20090421

Title: O(6)-methylguanine-DNA methyltransferase depletion and DNA damage in patients with melanoma treated with temozolomide alone or with lomeguatrib.

Journal: British journal of cancer 20090421

Title: A phase II trial of lomeguatrib and temozolomide in metastatic colorectal cancer.

Journal: British journal of cancer 20080520

Title: MGMT inhibitors--The Trinity College-Paterson Institute experience, a chemist's perception.

Journal: DNA repair 20070801

Title: Novel role of triazenes in haematological malignancies: pilot study of Temozolomide, Lomeguatrib and IL-2 in the chemo-immunotherapy of acute leukaemia.

Journal: DNA repair 20070801

Title: Randomized trial of the combination of lomeguatrib and temozolomide compared with temozolomide alone in chemotherapy naive patients with metastatic cutaneous melanoma.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20070620

Title: O6-(4-bromothenyl)guanine (PaTrin-2), a novel inhibitor of O6-alkylguanine DNA alkyl-transferase, increases the inhibitory activity of temozolomide against human acute leukaemia cells in vitro.

Journal: Pharmacological research 20060401

Title: The P140K mutant of human O(6)-methylguanine-DNA-methyltransferase (MGMT) confers resistance in vitro and in vivo to temozolomide in combination with the novel MGMT inactivator O(6)-(4-bromothenyl)guanine.

Journal: The journal of gene medicine 20060101

Title: O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts.

Journal: British journal of cancer 20051114

Title: Quantitative trait locus analysis reveals two intragenic sites that influence O6-alkylguanine-DNA alkyltransferase activity in peripheral blood mononuclear cells.

Journal: Carcinogenesis 20050801

Title: 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.

Journal: Molecular cancer therapeutics 20041001

Title: Effect of O6-(4-bromothenyl)guanine on different temozolomide schedules in a human melanoma xenograft model.

Journal: International journal of cancer 20020810

Title: Monosaccharide-linked inhibitors of O(6)-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships.

Journal: Journal of medicinal chemistry 20011122

Title: Reinhard J, et al. Monosaccharide-linked inhibitors of O(6)-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships. J Med Chem. 2001 Nov 22;44(24):4050-61.

Title: Clemons M, et al. O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts. Br J Cancer. 2005 Nov 14;93(10):1152-6.

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