selitrectinib(LOXO-195)

Name	LOXO-195
Synonyms	CS-2800 LOXO195 LOXO-195 Selitrectinib LOXO 195(Selitrectinib) selitrectinib(LOXO-195) (3aR,10R)-5-Fluoro-1,2,3,3a,8,9,10,11-octahydro-10-methyl-12H-15,17-ethenopyrazolo[3,4-d]pyrido[2,3-k]pyrrolo[2,1-m][1,3,7]triazacyclotridecin-12-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,10R)-
CAS	2097002-61-2

Molecular Formula	C20H21FN6O
Molar Mass	380.42
Density	1.51±0.1 g/cm3(Predicted)
pKa	11.44±0.40(Predicted)
Storage Condition	-20℃
Physical and Chemical Properties	Bioactive Selitrectinib (LOXO-195, BAY 2731954) is an orally active, highly effective, selective TRK kinase inhibitor with IC50 values of 2-9.8 nM for TRKA G595R, TRKC G623R and TRKA G667C. Its selectivity to targets is more than 1000 times that of non-TRK kinases detected by other 98%.
Use	Introduction LOXO-195 is the next generation TRK kinase inhibitor. The IC50 of TRKA and TRKC is 0.6 nM and <2.5 nM respectively.
In vitro study	LOXO-195 can effectively inhibit different activated TRK kinases in vitro. At a concentration of 1 μm, LOXO-195 was more than 98%-fold more selective for the target target than 228 of the other kinases tested (the pool contained 1000 kinases). In km2, CUTO-3 and O-91 cell lines containing TRK fusion, LOXO-195 can effectively inhibit the cell proliferation (IC50 <5 nmol/L). In the 84 cell lines that did not contain TRK fusions, LOXO-195 at concentrations up to 10 μm did not inhibit cell growth.
In vivo study	In tumors driven by Δtrka, LOXO-195 effectively reduced phosphorylated TRKA levels. In four TRKA-dependent tumor models (a tumor model constructed by inoculating KM12 cells containing a fusion of NIH 3T3 Δtrka, Δtrka G595R, Δtrka G667C, and TPM3-NTRK1),LOXO-195 can cause tumor growth inhibition.

Last Update：2024-01-02 23:10:35

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Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052

Wechat: 15671228036

Spot supply

Product Name: Selitrectinib(LOXO-195) Visit Supplier Webpage Request for quotation
CAS: 2097002-61-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

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