Repotrectinib(TPX-005)
Cat. No.: DC10463
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Chemical Structure
1802220-02-5
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Field of application
Repotrectinib(TPX-005) is a multi-target macrocycle inhibitor of anaplastic lymphoma kinase (ALK), c-ros proto-oncogene 1 receptor tyrosine kinase (ROS1), and neurotrophic tyrosine kinase receptor (TRK)
| Cas No.: |
1802220-02-5 |
| Chemical Name: |
Repotrectinib |
| Synonyms: |
TPX-0005;Repotrectinib;Ropotrectinib;08O3FQ4UNP;Repotrectinib (USAN);Repotrectinib [USAN];GTPL10316;TPX0005;TPX 0005 [WHO-DD];BDBM374727;US10246466 |
| SMILES: |
FC1C=CC2=C(C=1)[C@@H](C)NC1C=CN3C(=C(C=N3)C(NC[C@H](C)O2)=O)N=1 |
| Formula: |
C18H18FN5O2 |
| M.Wt: |
355.3662 |
| Sotrage: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| 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. |
| In Vivo: |
Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts[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]. |
MSDS
COA
| LOT NO. |
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| 2018-0101 |
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