All AbMole products are for research use only, cannot be used for human consumption.
In vitro: Larotrectinib (LOXO-101) was evaluated for off-target kinase enzyme inhibition against a panel of 226 non-TRK kinases at a compound concentration of 1,000 nM and ATP concentrations near the Km for each enzyme. LOXO-101 demonstrated greater than 50% inhibition for only one non-TRK kinase (TNK2 IC50 = 576 nM).
In vivo: A single dose (30 mg/kg) of LOXO-101 reduced tyrosine phosphorylation of TRKA and downstream signal transduction (pERK) in the tumor >80%. LOXO-101 was well tolerated up to 200 mg/kg/day for 14 d in this model.
Br J Cancer. 2023 Mar 23.
Functional genomics of human clear cell sarcoma: genomic, transcriptomic and chemical biology landscape for clear cell sarcoma
Larotrectinib (LOXO-101) purchased from AbMole
Clin Transl Med. 2022 Jul;12(7):e961.
Functional genomic analysis of epithelioid sarcoma reveals distinct proximal and distal subtype biology
Larotrectinib (LOXO-101) purchased from AbMole
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Source | Cancer Discov (2015). Figure 1. LOXO-101 |
| Method | MTS assay | |
| Cell Lines | CUTO-3.29 cells | |
| Concentrations | 100 nM | |
| Incubation Time | 2 h | |
| Results | pAKT was not inhibited in the CUTO-3.29 cells by LOXO-101 suggesting that TRK signaling is not AKT-dependent in this tumor. |
| Cell Experiment | |
|---|---|
| Cell lines | KM12 cells |
| Preparation method | Dose-dependent inhibition with LOXO-101 is demonstrated in three cancer cell line models of oncogenic TRK. |
| Concentrations | 100 nM |
| Incubation time | 24h |
| Animal Experiment | |
|---|---|
| Animal models | Athymic nude mice |
| Formulation | |
| Dosages | 60 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 428.44 |
| Formula | C21H22F2N6O2 |
| CAS Number | 1223403-58-4 |
| Solubility (25°C) | DMSO 4.3 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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