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Larotrectinib (LOXO-101) is an orally administered inhibitor of the TRK kinase, demonstrating high selectivity exclusively for the TRK family of receptors (IC50s = 2-20 nM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $33 | In Stock | In Stock | |
| 5 mg | $72 | In Stock | In Stock | |
| 10 mg | $97 | In Stock | In Stock | |
| 25 mg | $168 | In Stock | In Stock | |
| 50 mg | $263 | In Stock | In Stock | |
| 100 mg | $396 | In Stock | In Stock | |
| 500 mg | $912 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $78 | In Stock | In Stock |
| Description | Larotrectinib (LOXO-101) is an orally administered inhibitor of the TRK kinase, demonstrating high selectivity exclusively for the TRK family of receptors (IC50s = 2-20 nM). |
| Targets&IC50 | Trk:2-20 nM |
| In vivo | In vivo, Larotrectinib?(60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model[1]. |
| Animal Research | Mice were maintained under aseptic conditions.?The care and treatment of experimental animals was in accordance with institutional guidelines.?5 × 10^5 KM12 cells were injected subcutaneously into the dorsal flank area of the mice.?Tumor volume was monitored by direct measurement with calipers and calculated by the formula: length × (width^2)/2.?Following the establishment of tumor and when the tumor size was between 150–200 mm^2, mice were randomly selected to receive diluent, 60 mg/kg/dose or 200 mg/kg/dose of Larotrectinib(LOXO-101).?LOXO-101 was administered by oral gavage once daily for 14 days.?After the last dose, tissue and blood were collected at 3, 6 and 24 hours post-treatment[1]. |
| Synonyms | LOXO-101, ARRY-470 |
| Molecular Weight | 428.44 |
| Formula | C21H22F2N6O2 |
| Cas No. | 1223403-58-4 |
| Smiles | O[C@H]1CCN(C1)C(=O)Nc1cnn2ccc(nc12)N1CCC[C@@H]1c1cc(F)ccc1F |
| Relative Density. | 1.55 g/cm3 (Predicted) |
| Color | Yellow |
| Appearance | Solid |
| Storage | keep away from direct sunlight,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 4.6 mg/mL (10.74 mM), Sonication is recommended. | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.33 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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