For research use only. Not for therapeutic Use.
LOXO-101 (CAST: I000859), also known as larotrectinib, is a small molecule inhibitor that specifically targets the tropomyosin receptor kinase (TRK) family of receptors. It is designed to bind to the ATP binding site of TRKA, TRKB, and TRKC kinases, inhibiting their activity. LOXO-101 demonstrates potent cellular potency, with a range of 2 to 20 nM, against these TRK kinases. By blocking TRK signaling, LOXO-101 aims to disrupt the aberrant growth and survival signals that can contribute to the development and progression of TRK fusion-positive cancers. It has shown promising results in clinical trials, particularly in patients with solid tumors harboring TRK gene fusions.
| Catalog Number | I000859 |
| CAS Number | 1223405-08-0 |
| Synonyms | Larotrectinib sulfate; ARRY-470 sulfate; LOXO-101 sulfate; UNII-RDF76R62ID; RDF76R62ID |
| Molecular Formula | C21H24F2N6O6S |
| Purity | ≥95% |
| Target | Protein Tyrosine Kinase/RTK |
| Solubility | Soluble in DMSO |
| Storage | Store at -20°C |
| IC50 | 2 - 20 nM |
| SMILES | O=S(O)(O)=O.O=C(N1C[C@@H](O)CC1)NC2=C3N=C(N4[C@@H](C5=CC(F)=CC=C5F)CCC4)C=CN3N=C2 |
| Reference | 1: Doebele RC, Davis LE, Vaishnavi A, Le AT, Estrada-Bernal A, Keysar S, Jimeno |
