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In vitro: Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is a selective kinase inhibitor with nanomolar activity against TRKA, TRKB and TRKC but no other notable kinase inhibition below 1,000 nM. ARRY-470 does not inhibit proliferation of Ba/F3 cells expressing other oncogene targets (epidermal growth factor receptor (EGFR), ALK or ROS1) or of lung and colorectal cell lines that do not harbor an NTRK1 fusion. It induces cell-cycle arrest in G1 and apoptosis of KM12 cells.
In vivo: Early/sustained but not late/acute administration of ARRY-470(LOXO-101) markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone, but does not have a significant effect on tumor growth or bone remodeling. It has very limited ability crossing of the blood brain barrier
| Cell Experiment | |
|---|---|
| Cell lines | Ba/F3 cells |
| Preparation method | Ba/F3 cells expressing MPRIP-NTRK1 (RIP-TRKA) or EV were lysed after 5 h of treatment with the indicated doses of drugs (ARRY-470; G, gefitinib 1,000 nM) or DMSO control. The cell lysate are used for western bolt analysis. |
| Concentrations | 10, 100, 1000 nM |
| Incubation time | 5 h |
| Animal Experiment | |
|---|---|
| Animal models | Adult male C3H/HeJ mice |
| Formulation | Labrafac;polygly-colyzed glyceride |
| Dosages | 10-100 mg/kg |
| Administration | p.o. |
| Molecular Weight | 526.51 |
| Formula | C21H22F2N6O2.H2O4S |
| CAS Number | 1223405-08-0 |
| Solubility (25°C) | DMSO 50 mg/mL (Need ultrasonic) |
| Storage | 4°C, dry, sealed |
| Related Trk Products |
|---|
| Cyclotraxin B
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. |
| Gambogic amide
Gambogic amide is a potent and selective agonist of TrkA and also induces its tyrosine phosphorylation and activation of downstream signaling, including Akt and MAPK. |
| Protein kinase inhibitor 4
Protein kinase inhibitor 4 is a protein kinase inhibitor that inhibits TRK-A and ROS1 (IC50=3.0 nM and 104 nM respectively). |
| TRK-IN-22
TRK-IN-22 is a TRK inhibitor. |
| TrkB-IN-1
TrkB-IN-1 is a potent and orally active TrkB agonist and has favorable PK properties. |
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