Repotrectinib CAS# 1802220-02-5
Repotrectinib (TPX-0005) is a compact, next-generation tyrosine kinase inhibitor targeting ROS1, ALK, and TRK with sub-nanomolar potency (IC₅₀ ~0.3–2.0 nM across ROS1/ALK/TRK) and broad activity against resistance mutations, including solvent-front and gatekeeper variants. In cell-based assays, it potently suppressed phosphorylation of ROS1/ALK/TRK and downstream signaling, inhibiting proliferation of fusion-positive cancer cell lines at low nanomolar concentrations. In xenograft models of ROS1-, ALK-, and NTRK-driven tumors, repotrectinib induced tumor regressions at well-tolerated oral doses. Pharmacokinetic studies demonstrated favorable oral bioavailability, robust tumor exposure, and sustained target engagement, supporting its development for fusion-positive solid tumors.
📌 参考资料/链接：
Preparation of fluorodimethyltetrahydroethenopyrazolobenzoxatriazacyclotridecinone derivatives for use as antitumor agentsAssignee: TP Therapeutics, Inc.Inventors: Cui, Jingrong J.; et alWorld Intellectual Property OrganizationPatent#WO2017007759 A1
Preparation of fluorodimethyltetrahydroethenopyrazolobenzoxatriazacyclotridecinone derivatives for use as antitumor agentsAssignee: TP Therapeutics, Inc.Inventors: Cui, Jingrong J.; et alWorld Intellectual Property OrganizationPatent#WO2017007759 A1
📄 详细内容
CAS No. 1802220-02-5 Repotrectinib synthetic routes
Preparation of fluorodimethyltetrahydroethenopyrazolobenzoxatriazacyclotridecinone derivatives for use as antitumor agentsAssignee: TP Therapeutics, Inc.Inventors: Cui, Jingrong J.; et alWorld Intellectual Property OrganizationPatent#WO2017007759 A1
产品链接: CAS No. 1802220-02-5 ››
Preparation of fluorodimethyltetrahydroethenopyrazolobenzoxatriazacyclotridecinone derivatives for use as antitumor agentsAssignee: TP Therapeutics, Inc.Inventors: Cui, Jingrong J.; et alWorld Intellectual Property OrganizationPatent#WO2017007759 A1
产品链接: CAS No. 1802220-02-5 ››