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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 | Availability | Quantity |
---|---|---|---|
1 mg | $33 | In Stock | |
5 mg | $72 | In Stock | |
10 mg | $97 | In Stock | |
25 mg | $168 | In Stock | |
50 mg | $263 | In Stock | |
100 mg | $396 | In Stock | |
500 mg | $912 | In Stock | |
1 mL x 10 mM (in DMSO) | $78 | 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]. |
Alias | 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) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 4.6 mg/mL (10.74 mM) | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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