Larotrectinib (LOXO-101) sulfate

Catalog No.S7960 Synonyms: ARRY-470, Larotrectinib

Larotrectinib (LOXO-101) sulfate Chemical Structure

Molecular Weight(MW): 526.51

Larotrectinib (LOXO-101) sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).

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Cited by 3 Publications

3 Customer Reviews

  • Quantification of colony formation in (A), shown as a percentage of the control for NCIH2077 and RT112. Mean (3 biological replicates) +/- standard deviation (SD) shown (* p-value < 0.05, ** < 0.005, *** < 0.0005, two-sided t-test, comparing combination treatment to BGJ398 treatment). ns = not significant. (BGJ, BGJ398; Tram, Trametinib; BKM, BKM120; AZD, 8931; LDC, LDC1267; LOXO, LOXO-101; Imat, Imatinib; MGCD, MGCG-265).

    molecular cancer therapeutics. Larotrectinib (LOXO-101) sulfate purchased from Selleck.

    Immunoblot analysis for FRS2, AKT, and ERK activity for NCI-H2077 cells treated for 48 hours with DMSO, BGJ398, or additional kinase inhibitors as indicated, or combination treatment as indicated (Tram, trametinib; LDC, LDC1267; LOXO, LOXO-101; Imat, imatinib; MGCD, MGCG-265).

    Mol Cancer Ther, 2018, 17(7):1526-1539. Larotrectinib (LOXO-101) sulfate purchased from Selleck.

  • Inhibition of TRKA phosphorylation by Larotrectinib in NGF stimulated HEK293 cells. X-axis denotes concentrations of larotrectinib in nM. Y-Axis denotes percent inhibition of TRKA phosphorylation. Average IC50 of larotrectinib was found to be 10.9 nM. NGF: Neurite growth factor.

    Analytical Biochemistry, 2018, 545(15):78-83. Larotrectinib (LOXO-101) sulfate purchased from Selleck.

Purity & Quality Control

Choose Selective Trk receptor Inhibitors

Biological Activity

Description Larotrectinib (LOXO-101) sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).
Targets
TRK [1]
()
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[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KM12 cells MmHWSpVv[3Srb36gZZN{[Xl? Mlr1NEwhOTBuIEGwNEwhOTByMDDuUS=> M1zJdlMhcG:3coO= MWnMU3hQNTFyMTDpcohq[mm2ZXSgUnRTUzFicHjvd5Bpd3K7bHH0bY9vKGG2IEGwNEBvdW:uL1y= NVL6RYo3Ojh5NUG1N|k>
Ba/F3 NF22dVJHfW6ldHnvckBie3OjeR?= NUD3[IRTOCxiMUCsJFExOCxiMUCwNEBvVQ>? M16zcVMhcG:3coO= NHrXSVlNV1iRLUGwNUBqdmirYnn0[YQhVlSUS{GgdIhwe3Cqb4L5cIF1cW:wIHH0JFExOCCwbX;sM2wt M1:1VVI5PzVzNUO5
CR20 MVLGeY5kfGmxbjDhd5NigQ>? MoLpNEwhOTBuIEGwNEwhOTByMDDuUS=> NYDyUVdtOyCqb4Xydy=> MVLOWHJMOSCyaH;zdIhwenmuYYTpc44hf2G|IHnubIljcXSnZB?= NYHlR4lGOjh5NUG1N|k>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-NTRK(Y490) / p-ERK (T202/Y204) / p-Eif4e; 

PubMed: 29568395     


Western blots of KM-12 cells treated with merestinib, crizotinib, entrectinib and larotrectinib in vitro. Cells were treated with compound ranging from 3.9 - 1000 nM for 2 hours. Western blots were re-probed for total NTRK, ERK, eIF4E and β-actin for loading control purposes.

pTRKA / TRKA / pTRKC / TRKC / p-AKT / AKT; 

PubMed: 26216294     


(E) LOXO-101 inhibits phosphorylation of Y496 of TPM3-TRKA kinase and downstream phosphorylation of ERK1/2 and S473 AKT in KM12 cells. (F) LOXO-101 inhibits phosphorylation of TEL-TRKC kinase and ERK1/2 and AKT phosphorylation in MO-91 cells. Cells were treated for 2 hours with the indicated doses of LOXO-101 or DMSO alone and cell lysates were analyzed using the indicated antibodies except for MO-91 cells were treated for 2 hours with 100 nM of LOXO-101 or DMSO alone and cell lysates were immunoprecipitated with an anti-TRK antibody followed by immunoblot analysis with the indicated antibodies. 

29568395 26216294
Growth inhibition assay
Cell proliferation; 

PubMed: 26216294     


(A)–(C) Dose-dependent inhibition with LOXO-101 is demonstrated in three cancer cell line models of oncogenic TRK. CUTO-3.29 lung adenocarcinoma with MPRIP-NTRK1 (A), KM12 colorectal cancer with TPM3-NTRK1(B), and MO-91 acute myeloid leukemia with ETV6-NTRK3 (C) cell lines were treated with a dose range of LOXO-101 and cellular proliferation was assayed by MTS assay. The cellular was IC50 was ~59.4 ± 2.2 nM for CUTO-3.29, 3.5 ± 0.7 nM for KM12 and 1.0 ± 0.05 nM for MO-91.

26216294
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[1].

Protocol

Cell Research:[2]
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  • Cell lines: Ba/F3 cells
  • Concentrations: 10, 100, 1000 nM
  • Incubation Time: 5 h
  • 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.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: Adult male C3H/HeJ mice
  • Formulation: Labrafac;polygly-colyzed glyceride
  • Dosages: 10-100 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (189.92 mM)
Ethanol 100 mg/mL (189.92 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 526.51
Formula

C21H22F2N6O2.H2SO4

CAS No. 1223405-08-0
Storage powder
in solvent
Synonyms ARRY-470, Larotrectinib

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Trk receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID