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Larotrectinib sulfate

Catalog No. T6880   CAS 1223405-08-0
Synonyms: LOXO-101 sulfate, Larotrectinib (LOXO-101) sulfate, Larotrectinib, LOXO-101 (sulfate), ARRY-470, ARRY-470 (sulfate)

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Larotrectinib sulfate Chemical Structure
Larotrectinib sulfate, CAS 1223405-08-0
Pack Size Availability Price/USD Quantity
2 mg In stock $ 33.00
5 mg In stock $ 52.00
10 mg In stock $ 85.00
25 mg In stock $ 133.00
50 mg In stock $ 166.00
100 mg In stock $ 288.00
500 mg In stock $ 693.00
1 mL * 10 mM (in DMSO) In stock $ 60.00
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Purity: 99.69%
Purity: 99.49%
Purity: 98.62%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Larotrectinib sulfate (LOXO-101 sulfate) is an oral active and specific ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).
In vitro LOXO-101(ARRY-470) is a specific kinase inhibitor with nanomolar activity against TRKA/TRKB/TRKC but no other notable kinase inhibition (1 μM). ARRY-470 hasn't the inhibitory of the proliferation of Ba/F3 cells expressing other oncogene targets (EGFR, ROS1 or ALK) 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) obviously attenuates bone cancer pain and blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor-bearing bone, but no significant inhibition for tumor growth or bone remodeling. It has very limited ability crossing of the blood-brain barrier.
Cell Research Concentrations: 10,100,1000 nM. 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 is used for western blot analysis.
Animal Research Animal Models: Adult male C3H/HeJ mice. Formulation: Labrafac; polygly-colyzed glyceride. Dosages: 10-100 mg/kg. Administration: p.o.
Synonyms LOXO-101 sulfate, Larotrectinib (LOXO-101) sulfate, Larotrectinib, LOXO-101 (sulfate), ARRY-470, ARRY-470 (sulfate)
Molecular Weight 526.51
Formula C21H22F2N6O2·H2O4S
CAS No. 1223405-08-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 93 mg/mL (176.6 mM)

Ethanol: 10 mg/mL(19 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Ghilardi JR, et al. Mol Pain. 2010, 6:87. 2. Vaishnavi A, et al. Nat Med. 2013, 19(11):1469-72.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Fluorochemical Library Approved Drug Library Anti-Cancer Compound Library Targeted Therapy Drug Library

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Keywords

Larotrectinib sulfate 1223405-08-0 Apoptosis Tyrosine Kinase/Adaptors Trk receptor inhibit Inhibitor LOXO 101 Sulfate Tropomyosin related kinase receptor LOXO-101 sulfate ARRY470 LOXO101 Sulfate Larotrectinib (LOXO-101) sulfate Trk Receptor Larotrectinib LOXO-101 (sulfate) LOXO101 LOXO 101 Larotrectinib (LOXO-101) Sulfate LOXO-101 ARRY-470 ARRY 470 ARRY-470 (sulfate) LOXO-101 Sulfate Larotrectinib Sulfate inhibitor

 

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