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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
5mg USD 70  USD70 In stock
10mg USD 130  USD130 In stock
50mg USD 420  USD420 In stock
100mg USD 700  USD700 In stock
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Quality Control
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.

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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 428.44
Formula C21H22F2N6O2
CAS Number 1223403-58-4
Purity 99.56%
Solubility 4 mg/mL in DMSO
Storage at -20°C
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

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