| Name | Larotrectinib |
| 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). |
| 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]. |
| In vivo | In vivo, Larotrectinib?(60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 83.33 mg/mL (194.5 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.33 mM), Sonication is recommended.
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| Keywords | Tropomyosin related kinase receptor | Trkreceptor | Trk receptor | Trk | LOXO101 | LOXO 101 | Larotrectinib | Inhibitor | inhibit | ARRY470 | ARRY 470 | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |