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Larotrectinib
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).
Catalog No. T5995Cas No. 1223403-58-4
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Larotrectinib
Catalog No. T5995Alias LOXO-101, ARRY-470Cas No. 1223403-58-4
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).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | 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 |
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CitedProduct Introduction
Bioactivity
Chemical Properties
| 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 |
Storage & Solubility Information
| 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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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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