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Technical Data
| Formula | C10H8BrN5OS |
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| Molecular Weight | 326.17 | CAS No. | 192441-08-0 | |
| Solubility (25°C)* | In vitro | DMSO | 65 mg/mL (199.28 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Lomeguatrib (PaTrin-2) is a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase with IC50 of 5 nM. | ||
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| In vitro | Lomeguatrib inactivates O6-alkylguanine-DNA-alkyltransferase (ATase) with a IC50 10-fold lower than O6-Benzylguanine. Lomeguatrib inhibits the activity of ATase in Raji cells with IC50 of 10 nM. [1] Lomeguatrib effectively inactivates MGMT in MCF-7 cells with IC50 of ~6nM ). Lomeguatrib (10 μM ) substantially increases the growth inhibitory effects of temozolomide in MCF-7 cells (D60= 10 μM with Lomeguatrib vs 400 μM without). [2] | ||
| In vivo | Lomeguatrib (20 mg/kg/day for 5 days) combined with temozolomide (100 mg/kg/day for 5 days) produces a substantial tumour growth delay: median tumour quintupling time is increased by 22 days without any significant increase in toxicity, while neither of the two drugs administrated along show any antitumor activity. [2] Lomeguatrib inactivates ATase and enhances the anti-tumour effect of temozolomide in A375M human melanoma xenografts model. Lomeguatrib, at a single dose of 20 mg/kg i.p., produces complete ATase depletion in tumor within 2 hr. Temozolomide (100 g/kg/day) significantly delays growth of the A375M tumour xenograft with an estimated delay in the time for tumour to quintuple in size of 9.6 days. Addition of Lomeguatrib to temozolomide significantly enhances the latter’s effect, delaying the quintupling time a further 8.7 days. Moreover, the Lomeguatrib combination results in considerably less toxicity (0/9 vs. 2/9 deaths; 6.84% weight loss vs. 9.48%). Lomeguatrib alone has no significant effect on tumour growth. [3] |
Protocol (from reference)
References
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Customer Product Validation
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, , Mol Cancer Ther, 2015, 14(5):1236-46.
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Data from [Data independently produced by , , Onco Targets Ther, 2018, 11:3671-3684]
Selleck's Lomeguatrib has been cited by 8 publications
| MGMT function determines the differential response of ATR inhibitors with DNA-damaging agents in glioma stem cells for GBM therapy [ Neurooncol Adv, 2024, 6(1):vdad165] | PubMed: 38213834 |
| Epigenetic Activation of TUSC3 Sensitizes Glioblastoma to Temozolomide Independent of MGMT Promoter Methylation Status [ Int J Mol Sci, 2023, 24(20)15179] | PubMed: 37894860 |
| Heat Shock Protein Inhibitor 17-Allyamino-17-Demethoxygeldanamycin, a Potent Inductor of Apoptosis in Human Glioma Tumor Cell Lines, Is a Weak Substrate for ABCB1 and ABCG2 Transporters [ Pharmaceuticals (Basel), 2021, 14(2)107] | PubMed: 33573093 |
| Prolonged unfolded protein reaction is involved in the induction of chronic myeloid leukemia cell death upon oprozomib treatment [ Cancer Sci, 2020, 112(1):133-143] | PubMed: 33067904 |
| MutT homologue 1 (MTH1) catalyzes the hydrolysis of mutagenic O6-methyl-dGTP. [ Nucleic Acids Res, 2018, 46(20):10888-10904] | PubMed: 30304478 |
| Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] | PubMed: 30135193 |
| CAT3, a prodrug of 13a(S)-3-hydroxyl-6,7-dimethoxyphenanthro[9,10-b]-indolizidine, circumvents temozolomide-resistant glioblastoma via the Hedgehog signaling pathway, independently of O6-methylguanine DNA methyltransferase expression [Ji M Onco Targets Ther, 2018, 11:3671-3684] | PubMed: 29983575 |
| MGMT Expression Predicts PARP-Mediated Resistance to Temozolomide. [Erice O, et al. Mol Cancer Ther, 2015, 14(5):1236-46] | PubMed: 25777962 |
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.