Repotrectinib (TPX-0005) - 98%, high purity , CAS No.1802220-02-5, Inhibitor of ALK receptor tyrosine kinase;Inhibitor of c-ros oncogene 1; receptor tyrosine kinase;Inhibitor of Janus kinase 2;Inhibitor of neurotrophic receptor tyrosine kinase 1;Inhibitor of neurotrophic receptor tyrosine kinase 2;Inhibitor of neurotroph

Item Number

R414071

• Synonyms: Repotrectinib|TPX-0005|1802220-02-5|Ropotrectinib|08O3FQ4UNP|Repotrectinib [USAN]|TPX0005|(3R,11S)-6-fluoro-3,11-dimethyl-10-oxa-2,13,17,18,21-pentazatetracyclo[13.5.2.04,9.018,22]docosa-1(21),4(9),5,7,15(22),16,19-heptaen-14-one|Repotrectinib(TPX-005)|TR
• Specifications & Purity: Moligand™, ≥98%
• Biochemical and Physiological Mechanisms: Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of ALK receptor tyrosine kinase;Inhibitor of c-ros oncogene 1; receptor tyrosine kinase;Inhibitor of Janus kinase 2;Inhibitor of neurotrophic receptor tyrosine kinase 1;Inhibitor of neurotrophic receptor tyrosine kinase 2;Inhibitor of neurotroph

Product Description

Information

Repotrectinib (TPX-0005) Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).

Targets

ROS1 ; Trk receptor ; WT ALK (Cell-free assay); ALK(L1196M) (Cell-free assay); ALK(G1202R) (Cell-free assay) 27980,; 1.01 nM; 1.08 nM; 1.26 nM

In vitro

TPX-0005 is an orally available and potent ATP-competitive inhibitor against ALK, ROS1, TRKA, TRKB and TRKC recombinant kinases and their corresponding clinical resistant mutants. TPX-0005 demonstrates potent anti-proliferative activity in the range of sub-nanomolar to low nanomolar in a number of human cancer cell lines and engineered stable cell lines expressing the targeted oncogenes or their solvent front mutants, accompanied by inhibition of target phosphorylation and concomitant inactivation of downstream effectors such as ERK, AKT and STAT3. TPX-0005 inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib. TPX-0005 is able to not only inhibit the wild-type and a broad spectrum of mutant ALKs, but also overcome primary resistance and suppress metastatic features by inhibiting SRC.

In vivo

In patient derived xenograft tumor models, TPX-0005 treatment results in significant regression of tumors harboring the oncogenic ALK, ROS1 and TRKC fusions. Moreover, in a series of mouse xenograft tumor models, TPX-0005 exhibits marked anti-tumor activity not only in tumors harboring the wildtype oncogenic targets but also in tumors harboring the oncogenes with the solvent front mutations via inhibition of the target phosphorylation.