Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Lomeguatrib (formerly PaTrin-2) is a novel, potent and selective inhibitor of MGMT (O6-alkylguanine-DNA-alkyltransferase) with anticancer activity. It inhibits MGMT with IC50s of 9 nM and ∼6 nM in cell-free assay and MCF-7 cells, respectively.
ln Vitro |
Lomeguatrib (Compound 10) is an O6-methylguanine methyltransferase (MGMT) inhibitor, with an IC50 of 9 nM in cell-free assay[1] and ∼6 nM in MCF-7 cells. Lomeguatrib (10 μM) considerably improves the growth inhibitory effects of temozolomide in MCF-7 cells (D60=10 μM with Lomeguatrib versus 400 μM without)[2].
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ln Vivo |
In MCF-7 xenografts, memeguatrib (20 mg/kg ip) totally inactivates MGMT in less than two hours, but has no discernible effect on tumor growth[2].
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Animal Protocol |
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References |
[1]. 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.
[2]. 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 |
Molecular Formula |
C10H8BRN5OS
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Molecular Weight |
326.17
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CAS # |
192441-08-0
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Related CAS # |
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SMILES |
BrC1=CSC(COC2=C3N=CNC3=NC(N)=N2)=C1
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InChi Key |
JUJPKFNFCWJBCX-UHFFFAOYSA-N
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InChi Code |
InChI=1S/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)
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Synonyms |
PaTrin-2; Lomeguatrib; PaTrin 2; PaTrin2; 2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.0659 mL | 15.3294 mL | 30.6589 mL | |
5 mM | 0.6132 mL | 3.0659 mL | 6.1318 mL | |
10 mM | 0.3066 mL | 1.5329 mL | 3.0659 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Growth of MCF-7 tumour xenografts in nude mice.Br J Cancer. 2005 Nov 14;93(10):1152-6. |