TPX 0005

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TPX 0005 (Ropotrectinib, Repotrectinib, TPX0005) is a novel ALK/ROS1/TRK inhibitor.

TPX 0005 (Ropotrectinib, Repotrectinib, TPX0005) is a novel ALK/ROS1/TRK inhibitor, effectively inhibits a broad spectrum of mutations including solvent front ALK G1202R, ROS1 G2032R and TRKA G595R mutants; potently inhibits WT ALK (IC50=1.01 nM) and mutant ALKs including ALK G1202R (IC50=1.26 nM) and ALK L1196M (IC50=1.08 nM); is also a potent SRC inhibitor (IC50=5.3 nM); shows low nano-molar activities against CD74-ROS1 G2032R (IC50=8.4 nM), LMNA-TRKA G595R (IC50=0.4 nM),TEL-TRKB G639R (IC50=1.9 nM) and TEL-TRKC G623R (IC50=0.4 nM) in Ba/F3 cell proliferation assays; dramatically causes tumor growth inhibition and tumor regression in xenograft tumor model; demonstrates desired druglike properties and good safety profile.Solid Tumors Phase 2 Clinical

Ropotrectinib;Repotrectinib;TPX0005

Angiogenesis

ALK

ALK;Src

Cancer

Solid Tumors

1802220-02-5

355.37

C18H18FN5O2

>98% (HPLC)

DMSO: ≥83.3 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C1NC[C@H](C)OC2=CC=C(F)C=C2[C@@H](C)NC3=NC4=C1C=NN4C=C3

(7S,13R)-11-fluoro-6,7,13,14-tetrahydro-7,13-dimethyl-1,15-etheno-1H-pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one

(-20℃)

With Ice Pack

≥ 2 years