LOXO-292

LOXO-292

CAT N°: 33515
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From 74.00 62.90

LOXO-292 is an inhibitor of the receptor tyrosine kinase RET.{59919} It inhibits the phosphorylation of a KIF5B-RET fusion protein expressed in HEK293 cells (IC50 = 4 nM). LOXO-292 selectively inhibits proliferation of cancer cells containing RET mutations or gene fusions, including RETM918T-containing MZ-CRC-1 medullary thyroid and CCDC6-RET gene fusion-positive TPC-1 thyroid cancer cells, by 20 to 1,700-fold. It improves survival in a CCDC6-RET gene fusion-positive orthotopic patient-derived xenograft (PDX) mouse model of brain cancer when administered at a dose of 30 mg/kg. Formulations containing LOXO-292 have been used in the treatment of RET mutation- or gene fusion-positive lung or thyroid cancers.

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