Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Larotrectinib sulfate (LOXO-101 sulfate) is an oral active and specific ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (176.6 mM)
Ethanol: 10 mg/mL(19 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. More
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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