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ChemicalBook--->CAS DataBase List--->1350884-56-8

1350884-56-8

1350884-56-8 Structure

1350884-56-8 Structure
IdentificationBack Directory
[Name]

LOXO-195
[CAS]

1350884-56-8
[Synonyms]

LOXO-195
(6RS)-LOXO-195
Selitrectinib Racemate
Selitrectinib(LOXO-195) Racemate
(18bR)-17-Fluoro-1,2,3,11,12,13,14,18b-octahydro-12-methyl-10H-5,7-ethenopyrazolo[3,4-d]pyrido[2,3-k]pyrrolo[2,1-m][1,3,7]triazacyclotridecin-10-one
12H-15,17-Ethenopyrazolo[3,4-d]pyrido[2,3-k]pyrrolo[2,1-m][1,3,7]triazacyclotridecin-12-one, 5-fluoro-1,2,3,3a,8,9,10,11-octahydro-10-methyl-, (3aR)-
[Molecular Formula]

C20H21FN6O
[MDL Number]

MFCD31620755
[MOL File]

1350884-56-8.mol
[Molecular Weight]

380.42
Chemical PropertiesBack Directory
[density ]

1.51±0.1 g/cm3(Predicted)
[pka]

11.44±0.40(Predicted)
Hazard InformationBack Directory
[Description]

LOXO-195 is an orally available, highly potent, and selective TRK kinase inhibitor designed to overcome drug resistance mediated by acquired mutations. Although responses to TRK inhibition can be dramatic and durable; however, eventually emergence of acquired resistance is found to be inevitable.
[Uses]

(3aR)-Selitrectinib ((3aR)-LOXO-195) is an isform of Selitrectinib (HY-101977), which is a next-generation TRK kinase inhibitor, with IC50s of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively[1].
[References]

[1] Drilon A, et al. A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors. Cancer Discov. 2017 Sep;7(9):963-972. DOI:10.1158/2159-8290.CD-17-0507
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