LY2940680 Inhibitor CAS No. 1258861-20-9

Cat. No.	Name	Size	Price
KI0571	LY2940680	5 mg	$432
	LY2940680	10 mg	$592
	LY2940680	50 mg	$1552
	LY2940680	200 mg	$4272

Chemical Characteristic

Product Name	LY2940680
CAS No.	1258861-20-9
Molecular Weight	512.5
Formula	C₂₆H₂₄F₄N₆O
Chemical Name	4-Fluoro-N-methyl-N-[1-[4-(1-methyl-1H-pyrazol-5-yl)-1-phthalazinyl]-4-piperidinyl]-2-(trifluoromethyl)benzamide
Smiles	C(=O)(c1c(cc(cc1)F)C(F)(F)F)N(C1CCN(CC1)c1nnc(c2ccccc12)c1n(ncc1)C)C
Chemical Structure

Biological activities

LY2940680 is a smoothened (SMO) antagonist. LY2940680 inhibits cancer growth in cell lines containing a mutation in the gene encoding SMO.^[1] LY2940680 binds to the SMO receptor and potently inhibits Hedgehog (Hh) signaling in Daoy and C3H10t_{1/2. LY2940680 inhibits the functional activity of resistant SMO mutant (D473H) produced by treatment with GDC-0449. LY2940680 treatment induces Caspase-3 activity and reduces proliferation. LY2940680 inhibits Hh regulated gene expression in the subcutaneous xenograft tumor stroma and produces significant anti-tumor activity. Treatment of Ptch+/??p53????transgenic mice with oral administration of LY2940680 produce remarkable efficacy and significantly improve their survival. ^[2]}

References

[1] Redmond EM, et al. Investigational Notch and Hedgehog inhibitors--therapies for cardiovascular disease. Expert Opin Investig Drugs. 2011, 20(12): 1649-1664. [2] Bender M H, et al. Proffered Oral Presentations - New Small Molecule Therapeutics. Abstract 2819: Identification and characterization of a novel smoothened antagonist for the treatment of cancer with deregulated hedgehog signaling. Cancer Res. 2011, 71 (8 Supplement): 2819.

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