Chemical Structure : AMX12006
货号: PC-20852Not For Human Use, Lab Use Only.
AMX12006 (AMX-12006) is a potent, selective, orally active antagonist of prostaglandin E2 (PGE2) receptor 4 (EP4) with IC50 of 4.3 nM in cAMP assays, shows no activity against EP1, EP2, EP3 receptors.
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AMX12006 (AMX-12006) is a potent, selective, orally active antagonist of prostaglandin E2 (PGE2) receptor 4 (EP4) with IC50 of 4.3 nM in cAMP assays, shows no activity against EP1, EP2, EP3 receptors.
AMX12006 inhibits the cancer cells in breast cancer cell lines MCF-7 and 4T1 with IC50 of 46.73 and 79.47 μM respectively, and IC50 41.39 and >100 μM in colon cancer cell lines CT-26 WT and HCA-7, and IC50 > 100 μM in lung cancer cell lines.
AMX12006 (75 mg/kg, 150 mg/kg) demonstrated antitumor efficacy in a CT-26 colon cancer xenograft (BALB/c) mouse model, with no significant body weight loss.
Combination of AMX12006 with capecitabine significantly suppressed tumor growth (TGI up to 94.26%) in mouse models.
分子量 | 481.48 | |
分子式 | C26H22F3N3O3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Debasis Das, et al. ACS Medicinal Chemistry Letters, 2023.
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