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
Cell Experiment | |
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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 | |
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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 |
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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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Products are for research use only. Not for human use. We do not sell to patients.
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