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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 |
|---|
| GNF-5837
GNF-5837 is a potent pan-Trk inhibitor which display antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively. |
| GW441756
GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. |
| ANA-12
ANA-12 is a potent and selective TrkB antagonist with IC50s of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively. |
| 7,8-Dihydroxyflavone
7,8-Dihydroxyflavone acts as a potent and selective small-molecule agonist of the TrkB receptor (Kd ≈ 320 nM), the main signaling receptor of brain-derived neurotrophic factor (BDNF). |
| LOXO-101 sulfate
LOXO-101 sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). |
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Products are for research use only. Not for human use. We do not sell to patients.
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