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Selitrectinib

Chemical Structure : Selitrectinib

CAS No.: 2097002-61-2

Selitrectinib (LOXO-195, LOXO195)

Catalog No.: PC-60901Not For Human Use, Lab Use Only.

LOXO-195 (Selitrectinib, LOXO195) is a potent, selective, next-generation Trk tyrosine kinase inhibitor with IC50 of 0.6 nM and <2.5 nM for WT TrkA and WT TrKC, respectively.

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Purity & Documentation Purity: 98.79% (HPLC) Select Batch:

Biological Activity

LOXO-195 (Selitrectinib, LOXO195) is a potent, selective, next-generation Trk tyrosine kinase inhibitor with IC50 of 0.6 nM and <2.5 nM for WT TrkA and WT TrKC, respectively.
LOXO-195 also diplays high potentcy against mutant TrkA G595R, TrkA G667C, TrkC G623R and TrkC G696A with IC50 of 2.0, 9.8, 2.3 and <2.5 nM, respectively.
LOXO-195 overcomes acquired resistance mediated by recurrent kinase domain (solvent front and xDFG) mutations identified in multiple patients.

Physicochemical Properties

M.Wt 380.427
Formula C20H21FN6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(13E,14E,22R,6R)-35-fluoro-6-methyl-7-aza-1(5,3)-pyrazolo[1,5-a]pyrimidina-3(3,2)-pyridina-2(1,2)-pyrrolidinacyclooctaphan-8-one

References

1. Drilon A, et al. Cancer Discov. 2017 Sep;7(9):963-972.

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