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LOXO-101

Cat. No. M6151
LOXO-101 Structure
Synonym:

ARRY-470, larotrectinib

Size Price Availability Quantity
5mg USD 110 In stock
10mg USD 200 In stock
50mg USD 720 In stock
100mg USD 1055 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: 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.

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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 428.44
Formula C21H22F2N6O2
CAS Number 1223403-58-4
Purity >98%
Solubility 4.6 mg/mL in DMSO
Storage at -20°C
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.
Rating
References

Infantile Fibrosarcoma With NTRK3-ETV6 Fusion Successfully Treated With the Tropomyosin-Related Kinase Inhibitor LOXO-101.
Nagasubramanian R, et al. Pediatr Blood Cancer. 2016 Aug;63(8):1468-70. PMID: 27093299.

An Oncogenic NTRK Fusion in a Patient with Soft-Tissue Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101.
Doebele RC, et al. Cancer Discov. 2015 Oct;5(10):1049-57. PMID: 26216294.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LOXO-101, ARRY-470, larotrectinib supplier, Trk, inhibitors

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