1802220-02-5
1802220-02-5 structure
- Name: Repotrectinib
- Chemical Name: TPX-0005
- CAS Number: 1802220-02-5
- Molecular Formula: C18H18FN5O2
- Molecular Weight: 355.366
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK ALK
- Create Date: 2018-03-17 02:59:56
- Modify Date: 2024-01-02 07:16:26
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Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively.
| Name | TPX-0005 |
|---|---|
| Synonyms |
1,15-Etheno-1H-pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one, 11-fluoro-6,7,13,14-tetrahydro-7,13-dimethyl-, (7S,13R)-
08O3FQ4UNP (3R,11S)-6-Fluoro-3,11-dimethyl-10-oxa-2,13,17,18,21-pentaazatetracyclo[13.5.2.04,9.018,22]docosa-1(21),4,6,8,15(22),16,19-heptaen-14-one Repotrectinib |
| Description | Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively. |
|---|---|
| Related Catalog | |
| Target |
IC50: 5.3 nM (SRC), 1.01 nM (WT ALK), 1.26 nM (ALK G1202R), 1.08 nM (ALK L1196M)[1] |
| In Vitro | Repotrectinib (TPX-0005) effectively overcomes this primary resistance (IC50 100 nM in cell proliferation assay) with strong inhibition of the phosphorylation of EML4-ALK (IC50 13 nM) and the SRC substrate paxillin (IC50 107 nM). Repotrectinib inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib[1]. |
| In Vivo | Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts[1]. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Molecular Formula | C18H18FN5O2 |
| Molecular Weight | 355.366 |
| Exact Mass | 355.144440 |
| LogP | 1.71 |
| Index of Refraction | 1.694 |
| Storage condition | -20℃ |
| Hazard Codes | N |
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