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LOXO-195 is a second-generation TRK inhibitor shown to be active against NTRK resistant mutations, including solvent-front substitutions. In preclinical species, LOXO-195 showed high oral exposure and exhibited favorable absorption, distribution, metabolism, and excretion properties.
| Cas No. | 2097002-61-2 |
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| Purity | ≥99% |
| Formula | C20H21FN6O |
| Formula Wt. | 380.43 |
| Chemical Name | 9-Fluoro-15-methyl-2,11,16,20,21,24-hexaazapentacyclo(16.5.2.02,6.07,12.021,25)pentacosa-1(24),7,9,11,18(25),19,22-heptaen-17-one |
| IUPAC Name | (6R,15R)-9-fluoro-15-methyl-2,11,16,20,21,24-hexazapentacyclo[16.5.2.02,6.07,12.021,25]pentacosa-1(24),7(12),8,10,18(25),19,22-heptaen-17-one |
| Synonym | LOXO195; 0J45910S3X; Selitrectinib |
| Solubility | Ethanol (3 mg/mL), DMSO (5 mg/mL), DMF (12 mg/mL). |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Parikh AR, Corcoran RB. Fast-tracking drug development for rare molecular targets. Cancer Discov. 2017 Sep;7(9):934-936. PMID: 28864638.
Drilon A, Nagasubramanian R, Blake JF, 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. PMID: 28578312.