Chemical Structure : AMX12006
CAS No.:
2639775-01-0
AMX12006
(AMX 12006, AMX-12006)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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481.48
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Formula
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C26H22F3N3O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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CN1C2=CC=CC=C2C(NC3=CC(C(F)(F)F)=CC=C3)=C1C(N[C@H](C4=CC=C(C(O)=O)C=C4)C)=O
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References
1. Debasis Das, et al. ACS Medicinal Chemistry Letters, 2023.
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