AM211, inhibitor

AM211

Cat. Num. AAA5758544

• Purity: 98.28%
• Synonyms: AM211; AM211 free acid; inhibitor

• Purity/Purification: 98.28%
• Form/Format: Solid. Powder

• Solubility: DMSO: 125mg/mL (249.75mM); Ethanol: 85mg/mL (185.6mM); Water: <1mg/mL; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C27H27F3N2O4
• SMILES: CCN(Cc1cc(C(F)(F)F)ccc1-c1cc(CC(=O)O)ccc1OC)C(=O)NCc1ccccc1
• CAS Number: 1175526-27-8
• Target & IC50: Akt1: ic50 5nM; Akt2: ic50 18nM; Akt3: ic50 8nM; Human DP2: ic50 4.9nM; Mouse DP2: ic50 7.8nM; Guinea pig DP2: ic50 4.9nM; Rat DP2: ic50 10.4nM; prostaglandin D2 receptor
• Cell Research: GDC-0068 is prepared in DMSO and stored, and then diluted with appropriate medium before use[2]. The 384-well plates are seeded with 2,000 cells per well in a volume of 54 uL per well followed by incubation at 37 degree C under 5% CO2 overnight (~16 hours). Compounds (e.g., GDC-0068) are diluted in DMSO to generate the desired stock concentrations then added in a volume of 6 uL per well. All treatment, are tested in quadruplicates. After 4 days incubation, relative numbers of viable cells are estimated using CellTiter-Glo and total luminescence is measured on a Wallac Multilabel Reader. The concentration of drug resulting in IC50 is calculated from a 4-parameter curve analysis (XLfit) and is determined from a minimum of 3 experiments. For cell lines that failed to achieve an IC50, the highest concentration tested (10uM) is listed[2].
• In Vitro: AM211 exhibits good oral bioavailability in rats and dogs and dose-dependently inhibits 13,14-dihydro-15-keto-PGD(2)-induced leukocytosis in a guinea pig pharmacodynamic assay. AM211 demonstrates efficacy in two animal models of allergic inflammation, including an ovalbumin-induced lung inflammation model in guinea pigs and an ovalbumin-induced mouse model of allergic rhinitis. AM211 represents a potent and selective antagonist of DP2 that may be used clinically to evaluate the role of DP2 in T helper 2-driven allergic inflammatory diseases[1].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for AM211, inhibitor

AM211 is a potent and orally bioavailable antagonist of prostaglandin D2 (PGD2) receptor type 2 (DP2)

Product Categories/Family for AM211, inhibitor

Cytoskeletal Signaling; Akt; GPCR/G Protein

References

Lin K. Cancer Res, 2011, 71(8 Supplement), abstract DDT02-01.
Bain G, Lorrain D S, Stebbins K J, et al. Pharmacology of AM211, a Potent and Selective Prostaglandin D2 Receptor Type 2 Antagonist That Is Active in Animal Models of Allergic Inflammation[J]. Journal of Pharmacology and Experimental Therapeutics, 2011, 338(1):290-301.
Bain G, Lorrain D S, Stebbins K J, et al. Pharmacology of AM211, a Potent and Selective Prostaglandin D2 Receptor Type 2 Antagonist That Is Active in Animal Models of Allergic Inflammation[J]. Journal of Pharmacology and Experimental Therapeutics, 2011, 338(1):290-301.
James F. Blake. 2011.
Bain G, King C D, Brittain J, et al. Pharmacodynamics, Pharmacokinetics, and Safety of AM211: A Novel and Potent Antagonist of the Prostaglandin D2 Receptor Type 2[J]. The Journal of Clinical Pharmacology, 2012, 52(10).
Bain G, King C D, Brittain J, et al. Pharmacodynamics, Pharmacokinetics, and Safety of AM211: A Novel and Potent Antagonist of the Prostaglandin D2 Receptor Type 2[J]. The Journal of Clinical Pharmacology, 2012, 52(10).
Tabernero J, et al. Ann Oncol, 2011, 22(suppl 3), abstract IL33.
Heidi M. Savage, et al. Cancer Res, 2012, 72(8 Supplement), 966.
Roel Funke, et al. American Society of Clinical Oncology (ASCO) Annual Meeting, 1-5, 2012.