An inhibitor of TrkA and TrkC (IC50s = 0.6 and G595R

LOXO-195 – 10 mg

Brand:
Cayman
CAS:
2097002-61-2
Storage:
-20
UN-No:
Non-Hazardous - /

LOXO-195 is an inhibitor of the receptor tyrosine kinases TrkA and TrkC (IC50s = 0.6 and G595R, TrkAG667C, TrkCG623R, and TrkCG696A (IC50s = 2, 9.8, 2.3, and 50 value of 1.9 nM. It selectively inhibits proliferation of Trk fusion-positive K12, CUTO-3, and MO-91 cell lines (IC50s = ≤5 nM) over Trk fusion-negative cell lines when used at concentrations up to 10 μM. LOXO-195 (≥30 mg/kg) reduces tumor growth in TrkA-dependent KM12, as well as NIH 3T3 ΔTrkA, ΔTrkA + TrkAG595R, and ΔTrkA + TrkAG667C mouse xenograft models.  

 

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SKU: 27062 - 10 mg Category:

Description

An inhibitor of TrkA and TrkC (IC50s = 0.6 and G595R, TrkAG667C, TrkCG623R, and TrkCG696A (IC50s = 2, 9.8, 2.3, and 50 = 1.9 nM); selectively inhibits proliferation of Trk fusion-positive K12, CUTO-3, and MO-91 cell lines (IC50s = ≤5 nM) over Trk fusion-negative cell lines; reduces tumor growth in TrkA-dependent KM12, as well as NIH 3T3 ΔTrkA, ΔTrkA + TrkAG595R, and ΔTrkA + TrkAG667C mouse xenograft models at ≥30 mg/kg

Formal name: (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

Synonyms:  Selitrectinib

Molecular weight: 380.4

CAS: 2097002-61-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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