LOXO-101 sulfate

  • CAT Number: I000859
  • CAS Number: 1223405-08-0
  • Molecular Formula: C21H24F2N6O6S
  • Molecular Weight: 526.51
  • Purity: ≥95%
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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
Molecular Formula

C21H24F2N6O6S

Purity 95%
Target Trk
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
A, Varella-Garcia M, Aisner DL, Li Y, Stephens PJ, Morosini D, Tuch BB, Fernandes
M, Nanda N, Low JA. An Oncogenic NTRK Fusion in a Patient with Soft-Tissue
Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101.
Cancer Discov. 2015 Oct;5(10):1049-57. doi: 10.1158/2159-8290.CD-15-0443. Epub
2015 Jul 27. PubMed PMID: 26216294; PubMed Central PMCID: PMC4635026.<br />
2: Nagasubramanian R, Wei J, Gordon P, Rastatter JC, Cox MC, Pappo A. Infantile
Fibrosarcoma With NTRK3-ETV6 Fusion Successfully Treated With the
Tropomyosin-Related Kinase Inhibitor LOXO-101. Pediatr Blood Cancer. 2016
Aug;63(8):1468-70. doi: 10.1002/pbc.26026. Epub 2016 Apr 19. PubMed PMID:
27093299; PubMed Central PMCID: PMC5074243.

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