LY2940680

• Catalog No.: S2157
• CAS Number: 1258861-20-9
• M. F.: C26H24F4N6O
• M. W.: 512.5019728
• Storage: -20°C

SYNONYMS

• IUPAC name: 4-fluoro-N-methyl-N-{1-[4-(1-methyl-1H-pyrazol-5-yl)phthalazin-1-yl]piperidin-4-yl}-2-(trifluoromethyl)benzamide
• IUPAC Traditional name: 4-fluoro-N-methyl-N-{1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl}-2-(trifluoromethyl)benzamide

DATABASE IDS

• CAS Number: 1258861-20-9

PROPERTIES

• Target: Hedgehog
• Salt Data: Free Base
• Storage Condition: -20°C

DETAILS

Description (English)

Biological Activity

• Description: LY2940680 binds to the Smo receptor and potently inhibits Hh signaling.
• Targets: Smo
• In Vitro: LY2940680 inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib. ^[1]
• In Vivo: LY2940680 has excellent pharmacokinetic properties in rodent and non-rodent species. LY2940680 administrated orally treats Ptch^+/- p53^-/- transgenic mice which spontaneously develop medulloblastoma, produces remarkable efficacy and significantly improves their survival. LY2940680 reveals rapid kinetics of anti-tumor activity through magnetic resonance imaging of these mice, and LY2940680 induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. LY2940680 inhibits Hh regulated gene expression in the subcutaneous xenograft tumor stroma and produces significant anti-tumor activity. ^[2]
• Clinical Trials: LY2940680 is currently being tested in phase 1 trials for people with a range of solid tumors.

Combination Therapy

• Description: LY2940680 inhibits the functional activity of resistant Smo mutant (D473H) produced by treatment with GDC-0449 (a Smo antagonist). sup>[2]

References

• References: [1] Redmond EM et al. Expert Opin Investig Drugs, 2011, 20(12),1649-1664.
• References: [2] Mark H. Bender, Cancer Research, 2011, Volume 71, Issue 8, Supplement1

REFERENCES

• Redmond EM et al. Expert Opin Investig Drugs, 2011, 20(12),1649-1664.
• Mark H. Bender, Cancer Research, 2011, Volume 71, Issue 8, Supplement1