[CAS NO. 1223405-08-0] Larotrectinib (LOXO-101) sulfate
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PRODUCTS SPECIFICATIONS [1223405-08-0]
Store
Catalog
SLK-S7960
Brand
Selleck
CAS
1223405-08-0
DESCRIPTION [1223405-08-0]
Overview
| MDL | MFCD29472286 |
|---|---|
| Molecular Weight | 526.51 |
| Molecular Formula | C21H22F2N6O2.H2SO4 |
| SMILES | O=S(O)(O)=O.O=C(N1CC[C@H](O)C1)NC2=C3N=C(N4[C@@H](C5=CC(F)=CC=C5F)CCC4)C=CN3N=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8993 mL | 9.4965 mL | 18.9930 mL |
| 5 mM | 0.3799 mL | 1.8993 mL | 3.7986 mL |
| 10 mM | 0.1899 mL | 0.9496 mL | 1.8993 mL |
| 50 mM | 0.0380 mL | 0.1899 mL | 0.3799 mL |
Description
Larotrectinib sulfate (LOXO-101, ARRY-470) is an oral potent and selective ATP-competitive inhibitor of . Larotrectinib inhibition of TRKs induces cellular and G1 cell-cycle arrest.
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.
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.
References
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