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Larotrectinib (LOXO-101)

Cat. No. M6151
Larotrectinib (LOXO-101) Structure
Synonym:

ARRY-470, larotrectinib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 40  USD40 In stock
5mg USD 70  USD70 In stock
10mg USD 90  USD90 In stock
50mg USD 250  USD250 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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.
Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Nagasubramanian R, et al. Pediatr Blood Cancer. Infantile Fibrosarcoma With NTRK3-ETV6 Fusion Successfully Treated With the Tropomyosin-Related Kinase Inhibitor LOXO-101.

[2] Doebele RC, et al. Cancer Discov. An Oncogenic NTRK Fusion in a Patient with Soft-Tissue Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101.

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Keywords: Larotrectinib (LOXO-101), ARRY-470, larotrectinib supplier, Trk, inhibitors, activators


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