TPX-0005 (Repotrectinib) is an orally available and potent ATP-competitive inhibitor against ALK/ROS1/pan-TRK and their corresponding constitutively active clinical resistant mutants [1] TPX-0005 inhibits cell proliferation in neuroblastoma cells and exhibits strong antitumor effects in xenograft models of neuroblastoma [2]. Clinical trial studies in patients with advanced solid tumors harboring ALK, ROS1, or NTRK1-3 rearrangements are in progress as single agent as well as in combinatory therapy [3].
Technical information:
| Chemical Formula: | C18H18FN5O2 | |
| CAS #: | 1802220-02-5 | |
| Molecular Weight: | 355.37 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | (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 | |
| Solubility: | Up to 200 mM in DMSO | |
| Synonyms: | Repotrectinib , Ropotrectinib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.
Reference:
| 1. | Drilon A., et al. Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent-Front Mutations. Cancer Discov. 2018; 8(10); 122736. ©2018 AACR. Pubmed ID: DOI: 10.1158/2159-8290.CD-18-0484 |
| 2. | Cervantes-Madrid D. et al. Repotrectinib (TPX-0005), effectively reduces growth of ALK driven neuroblastoma cells. Sci Rep. 2019; 9: 19353 Pubmed ID: 31852910 |
| 3. | Cui JJ, et al. Repotrectinib Increases Effectiveness of KRAS-G12C Inhibitors in KRASG12C Mutant Cancer Models via Simultaneous SRC/FAK/JAK2 Inhibition. Cancer Res 2020; 80(16 Suppl):Abstract nr 1958 Pubmed ID: DOI: 10.1158/1538-7445 |
| 4. | Murray B, et al. Repotrectinib Increases Effectiveness of MEK Inhibitor Trametinib in KRAS Mutant Cancer Models Via Simultaneous SRC/FAK/JAK2 Inhibition. Cancer Res 2020; 80(16 Suppl):Abstract nr 1957 Pubmed ID: 31852910 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.