Repotrectinib
Based on 7 publication(s) in Google Scholar
Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 1802220-02-5
- Formula: C18H18FN5O2
- Molecular Weight:355.37
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Repotrectinib
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
Biological Activity
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TrkA |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.7 nM
Compound: TPX-0005
|
Cytotoxicity against mouse BaF3 cells transfected with TrKA F589L mutant assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with TrKA F589L mutant assessed as reduction in cell viability by MTT assay
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[PMID: 34253025] |
| BaF3 | IC50 |
1.8 nM
Compound: TPX-0005
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Cytotoxicity against mouse BaF3 cells transfected with TrKA assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with TrKA assessed as reduction in cell viability by MTT assay
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[PMID: 34253025] |
| BaF3 | IC50 |
2.2 nM
Compound: TPX-0005
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Cytotoxicity against mouse BaF3 cells transfected with SLC34A2-Ros1 assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with SLC34A2-Ros1 assessed as reduction in cell viability by MTT assay
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[PMID: 34253025] |
| BaF3 | IC50 |
4.8 nM
Compound: TPX-0005
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Cytotoxicity against mouse BaF3 cells transfected with TrKA G623R mutant assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with TrKA G623R mutant assessed as reduction in cell viability by MTT assay
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[PMID: 34253025] |
| BaF3 | IC50 |
8 nM
Compound: TPX-0005
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Cytotoxicity against mouse BaF3 cells transfected with TrKA G595R mutant assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with TrKA G595R mutant assessed as reduction in cell viability by MTT assay
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[PMID: 34253025] |
| BaF3 | IC50 |
<0.2 nM
Compound: Repotrectinib
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Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as cell growth inhibition
Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as cell growth inhibition
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[PMID: 36395392] |
| BaF3 | IC50 |
208 nM
Compound: TPX-0005
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Antiproliferative activity against EML4-ALK-L1196M/G1202R mutated mouse BaF3 cells assessed as cell growth inhibition by CCK-8 assay
Antiproliferative activity against EML4-ALK-L1196M/G1202R mutated mouse BaF3 cells assessed as cell growth inhibition by CCK-8 assay
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[PMID: 37127101] |
| BaF3 | IC50 |
0.66 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
0.88 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
0.98 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
1.14 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
1.39 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
1.61 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
1.9 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
10.67 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
10.83 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
12.28 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
15.66 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
158.95 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
17.04 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
19.3 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
2.15 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
23.07 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
3.32 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
4.59 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
5.4 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
5.75 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
78.32 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
8.12 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
892.25 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| BaF3 | IC50 |
9.44 nM
Compound: 4
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Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method
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[PMID: 37676745] |
| KARPAS-299 | IC50 |
40 nM
Compound: TPX-0005
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Antiproliferative activity against human KARPAS-299 cells assessed as cell growth inhibition by CCK-8 assay
Antiproliferative activity against human KARPAS-299 cells assessed as cell growth inhibition by CCK-8 assay
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[PMID: 37127101] |
| NCI-H1373 | IC50 |
5 μM
Compound: 1
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Cytotoxicity against human NCI-H1373 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
Cytotoxicity against human NCI-H1373 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
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[PMID: 34676026] |
| NCI-H1792 | IC50 |
1901 nM
Compound: 1
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Cytotoxicity against human NCI-H1792 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
Cytotoxicity against human NCI-H1792 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
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[PMID: 34676026] |
| NCI-H2122 | IC50 |
1936 nM
Compound: 1
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Cytotoxicity against human NCI-H2122 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
Cytotoxicity against human NCI-H2122 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
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[PMID: 34676026] |
| NCI-H23 | IC50 |
4059 nM
Compound: 1
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Cytotoxicity against human NCI-H23 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
Cytotoxicity against human NCI-H23 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
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[PMID: 34676026] |
| NCI-H358 | IC50 |
2500 nM
Compound: 1
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Cytotoxicity against human NCI-H358 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
Cytotoxicity against human NCI-H358 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
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[PMID: 34676026] |
Repotrectinib (TPX-0005) inhibits mutant ALKs including ALK G1202R (IC50=1.26 nM) and ALK L1196M (IC50=1.08 nM). Repotrectinib also inhibits a variety of other kinases, including JAK2, LYN, Src, and FAK (IC50=1.04, 1.66, 5.3, and 6.96 nM, respectively)[1].
Repotrectinib 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1802220-02-5
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Appearance Solid
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Molecular Weight 355.37
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Formula C18H18FN5O2
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Color White to off-white
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SMILES
O=C1NC[C@H](C)OC2=CC=C(F)C=C2[C@@H](C)NC3=NC4=C1C=NN4C=C3
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Synonyms
TPX-0005
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Cancer Discov
NVL-520 is a selective, TRK-sparing, and brain-penetrant inhibitor of ROS1 fusions and secondary resistance mutations. [Abstract]2023 Mar 1;13(3):598-615. PMID: 36511802
Repotrectinib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2023 Mar 1;13(3):598-615. [Abstract]
Repotrectinib (15-75 mg/kg; i.g.; twice daily for 14 d) induced regression in the Ba/F3 CD74-ROS1 G2032R xenograft mice.
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Nat Commun
Somatic gene delivery faithfully recapitulates a molecular spectrum of high-risk sarcomas. [Abstract]2025 Jun 16;16(1):5283. PMID: 40523919
Repotrectinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jun 16;16(1):5283. [Abstract]
Repotrectinib (1-1000 nM; 72 h) showed specific and significant activity in NTRK-Mono and NTRK-Pleo cell lines in vitro.
Repotrectinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jun 16;16(1):5283. [Abstract]
Repotrectinib (2 mg/mL; i.g.; twice daily for 3 weeks) resulted in profound antitumor activity and complete tumor regression in mice bearing an NTRK-Mono allograft model.
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J Med Chem
Discovery of Oral Degraders of the ROS1 Fusion Protein with Potent Activity against Secondary Resistance Mutations. [Abstract]2024 Oct 24;67(20):18098-18123. PMID: 39361251 -
Mol Cancer Ther
2025 Jul 2;24(7):1005-1019. PMID: 40299789
Repotrectinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2025 Jul 2;24(7):1005-1019. [Abstract]
Repotrectinib (15-75 mg/kg; twice daily for 24 d). Weight changes and survival analysis of Ba/F3 CD74-ROS1 G2032R luciferase mice.
Repotrectinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2025 Jul 2;24(7):1005-1019. [Abstract]
Graph showed the number of resistant wells out of 480 and the distribution of kinase domain mutations among sequenced wells for Repotrectinib (5.6-28 nM; 28 d) in Ba/F3 CD74-ROS1 cells.
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Sci Rep
Novel insight into mechanisms of ROS1 catalytic activation via loss of the extracellular domain. [Abstract]2024 Sep 27;14(1):22191. PMID: 39333184 -
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Solvent & Solubility
DMSO : 25 mg/mL (70.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8140 mL | 14.0698 mL | 28.1397 mL | 70.3492 mL |
| 5 mM | 0.5628 mL | 2.8140 mL | 5.6279 mL | 14.0698 mL | |
| 10 mM | 0.2814 mL | 1.4070 mL | 2.8140 mL | 7.0349 mL | |
| 15 mM | 0.1876 mL | 0.9380 mL | 1.8760 mL | 4.6899 mL | |
| 20 mM | 0.1407 mL | 0.7035 mL | 1.4070 mL | 3.5175 mL | |
| 25 mM | 0.1126 mL | 0.5628 mL | 1.1256 mL | 2.8140 mL | |
| 30 mM | 0.0938 mL | 0.4690 mL | 0.9380 mL | 2.3450 mL | |
| 40 mM | 0.0703 mL | 0.3517 mL | 0.7035 mL | 1.7587 mL | |
| 50 mM | 0.0563 mL | 0.2814 mL | 0.5628 mL | 1.4070 mL | |
| 60 mM | 0.0469 mL | 0.2345 mL | 0.4690 mL | 1.1725 mL |