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AMX12006

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

M.Wt 481.48
Formula C26H22F3N3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Debasis Das, et al. ACS Medicinal Chemistry Letters, 2023.

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