Entrectinib

CAT#: H206181

CAS#: 1108743-60-7

Description: Entrectinib, also known as RXDX-101 and NMS-E628, is an oral small molecule inhibitor of TrkA, TrkB and TrkC, as well as ROS1 and ALK, with high potency and selectivity. RXDX-101 has demonstrated potent pharmacological activity in preclinical studies and has the potential to be first-in-class against the Trk family of kinases. PXDX-101 has been well tolerated in patients with advanced solid tumors. PXDX-101 is currently in clinical trials, and is being developed by Ignyta.

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Synthetic Routes

Entrectinib - Synthetic Route 1

Entrectinib route01

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Entrectinib - Synthetic Route 2

Entrectinib route02

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Entrectinib - Synthetic Route 3

Entrectinib route03

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Lombardi Borgia, Andrea; Menichincheri, Maria; Orsini, Paolo; Panzeri, Achille; Perrone, Ettore; Vanotti, Ermes; Nesi, Marcella; Marchionni, Chiara. Preparation of substituted indazole derivatives for use as kinase inhibitors (Assignee Nerviano Medical Sciences S.r.l., Italy) WO 2009013126 (2009).