For research use only. Not for therapeutic Use.
LOXO-101 (Cat No.: I000858), also known as larotrectinib, is a selective inhibitor of tropomyosin receptor kinases (TRK) including TRKA, TRKB, and TRKC. It is used for the treatment of solid tumors harboring NTRK gene fusions, which lead to constitutive activation of TRK signaling. LOXO-101 has demonstrated remarkable efficacy in patients with NTRK fusion-positive cancers, showing high response rates and durable responses. It is an oral medication that has shown promise in various tumor types, including pediatric and adult cancers, making it a targeted therapy option for patients with NTRK fusion-positive tumors.
| Catalog Number | I000858 |
| CAS Number | 1223403-58-4 |
| Synonyms | Larotrectinib |
| Molecular Formula | C21H22F2N6O2 |
| Purity | 98% |
| Target | Protein Tyrosine Kinase/RTK |
| Target Protein | |
| Solubility | DMSO: ≥ 4.6 mg/mL |
| Appearance | Solid |
| Storage | Dry, dark and at 2 - 8 °C for six months or -20°C for two years. |
| IC50 | CUTO-3.29:＜100 nM(IC50) KM12 and MO-91：＜10 nM(IC50) |
| IUPAC Name | (3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxypyrrolidine-1-carboxamide |
| InChI | InChI=1S/C21H22F2N6O2/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/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31)/t14-,18+/m0/s1 |
| InChIKey | NYNZQNWKBKUAII-KBXCAEBGSA-N |
| 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 |
| Reference | 1:Infantile Fibrosarcoma With NTRK3-ETV6 Fusion Successfully Treated With the Tropomyosin-Related Kinase Inhibitor LOXO-101. Nagasubramanian R, Wei J, Gordon P, Rastatter JC, Cox MC, Pappo A.Pediatr Blood Cancer. 2016 Aug;63(8):1468-70. doi: 10.1002/pbc.26026. Epub 2016 Apr 19. PMID: 27093299 Free PMC Article<br /> |
