1223405-08-0

Product Details:

CasNo： 1223405-08-0

Molecular Formula： C21H24F2N6O6S

Purity： 99%

Synonyms: LOXO-101(sulfate); (3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide sulfate; (3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide sulfate; ARRY 470 sulfate; Larotrectinib(LOXO101); Larotrectinib (LOXO-101) sulfate
Solubility: ≥18.47 mg/mL in DMSO; ≥2.14 mg/mL in EtOH; ≥29.65 mg/mL in H2O
Color: Light yellow to brown
Form: Solid

Description:
LOXO-101 (sulfate) (or Larotrectinib Sulfate) is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC. LOXO-101 has IC50 values in the low nanomolar range for inhibition of all three TRK family members in binding and cellular assays, with 100x selectivity over other kinases, and has shown acceptable pharmaceutical properties and safety in nonclinical models. The TRK family of neurotrophin receptors, TRKA, TRKB, and TRKC (encoded by NTRK1, NTRK2, and NTRK3 genes, respectively) and their neurotrophin ligands regulate growth, differentiation and survival of neurons.

Uses:
Larotrectinib Sulfate is a potent and selective oral ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).

Clinical Use:
Larotrectinib sulfate is approved to treat solid tumors with NTRKgene fusion without drug resistance mutation in specific TRK proteins. It is used in adults and children whose cancer has metastasized (spread to other parts of the body) or cannot be removed by surgery and has gotten worse after other treatments or cannot be treated with other therapies. This use is approved under FDA’s Accelerated Approval Program. As a condition of approval, a confirmatory trial(s) must show that larotrectinib sulfate provides a clinical benefit in these patients. Larotrectinib sulfate is also being studied in treating other types of cancer.