RGNCY-0100 (AS2676293 RANKL inhibitor)
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AS2676293 is a small molecule RANKL inhibitor that is effective in treating mouse metastasis in mouse models. AS2676293 is orally bioavailable and inhibited bone metastasis of human breast cancer cells (MDA-MB-231-5a-D-Luc2) and tumor-induced osteolysis. In transwell assays, AS2676293 inhibited bone metastasis of B16F10, a murine cell line that is known not to trigger osteoclast activation. AS2676293 has potential for development as a therapy for treating bone metastasis through the inhibition of both osteoclast bone resorption and tumor migration to bone.
Systematic Name: N-(4-fluoro-2-(trifluoromethyl)benzyl)-5-methoxy-2-(pyridin-2-yl)pyrimidin-4-amine
SMILES: COC(C=N1)=C(NCC2=CC=C(F)C=C2C(F)(F)F)N=C1C3=NC=CC=C3
Formula: C18H14F4N4O
Mol Wt: 378.33
PMID: 22853997
Tags: Cancer, small molecule, RGNCY-0100, AS2676293, RANKL, bone, osteoclast, metastasis, B16F10, MDA-MB-231-5a-D-Luc2