Larotrectinib sulfate (LOXO-101, ARY-470) is an orally available, selective, and effective inhibitor of ATP-competitive tropomyosin receptor kinase TRK. Larotrectinib inhibits TRKs and induces apoptosis and G1 cell cycle arrest.

 

Brand: BCM

 

Target: Trk receptor; Apoptosis

 

Signaling Pathways: Apoptosis; Tyrosine Kinase/Adaptors

 

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.

 

Stability: Hygroscopic

 

Solubility: Soluble in DMSO. Insoluble in Water; insoluble in Ethanol.

 

GHS: GHS07

 

Isomeric SMILES: C1C[C@@H](N(C1)C2=NC3=C(C=NN3C=C2)NC(=O)N4CC[C@@H](C4)O)C5=C(C=CC(=C5)F)F.OS(=O)(=O)O  

 

InChIKey: PXHANKVTFWSDSG-QLOBERJESA-N  

 

InChI: InChI=1S/C21H22F2N6O2.H2O4S/c22-13-3-4-16(23)15(10-13)18-2-1-7-28(18)19-6-9-29-20(26-19)17(11-24-29)25-21(31)27-8-5-14(30)12-27;1-5(2,3)4/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31);(H2,1,2,3,4)/t14-,18+;/m0./s1

 

Attribute
[Chem Name]	(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxypyrrolidine-1-carboxamide;sulfuric acid
[Synonym]	Larotrectinib sulfate; LOXO-101 (sulfate); ARRY-470
[CAS No.]	1223405-08-0
[EINECS]	232-655-5
[MDL No.]	MFCD29472286
[Formula]	C21H24F2N6O6S
[Molecular]	526.52
[Form]	Solid Powder
[Storage]	Keep in dark place. Inert atmosphere. Room temperature

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