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LOXO-101 sulfate

Cat. No. M6211
LOXO-101 sulfate Structure
Synonym:

Larotrectinib sulfate

Size Price Availability Quantity
5mg USD 90 In stock
10mg USD 155 In stock
50mg USD 500 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: ARRY-470(LOXO-101) is a selective kinase inhibitor with nanomolar activity against TRKA, TRKB and TRKC but no other notable kinase inhibition below 1,000 nM. ARRY-470 does not inhibit proliferation of Ba/F3 cells expressing other oncogene targets (epidermal growth factor receptor (EGFR), ALK or ROS1) or of lung and colorectal cell lines that do not harbor an NTRK1 fusion. It induces cell-cycle arrest in G1 and apoptosis of KM12 cells.

In vivo: Early/sustained but not late/acute administration of ARRY-470(LOXO-101) markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone, but does not have a significant effect on tumor growth or bone remodeling. It has very limited ability crossing of the blood brain barrier

Protocol
Cell Experiment
Cell lines Ba/F3 cells
Preparation method Ba/F3 cells expressing MPRIP-NTRK1 (RIP-TRKA) or EV were lysed after 5 h of treatment with the indicated doses of drugs (ARRY-470; G, gefitinib 1,000 nM) or DMSO control. The cell lysate are used for western bolt analysis.
Concentrations 10, 100, 1000 nM
Incubation time 5 h
Animal Experiment
Animal models Adult male C3H/HeJ mice
Formulation Labrafac;polygly-colyzed glyceride
Dosages 10-100 mg/kg
Administration p.o.
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 526.51
Formula C21H22F2N6O2.H2O4S
CAS Number 1223405-08-0
Purity >99%
Solubility 100 mg/mL in DMSO
Storage at -20°C
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 sulfate, Larotrectinib sulfate supplier, Trk, inhibitors

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