LOXO-195

Alternative_name

(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
Description

LOXO-195 is a potent and selective TRK (tropomyosin-related-kinase) inhibitor, with potential anticancer activity. LOXO-195 specifically targets and binds to TRK, including the fusion proteins containing sequences from neurotrophic tyrosine receptor kinase (NTRK) types 1 (NTRK1), 2 (NTRK2), and 3 (NTRK3). This prevents neurotrophin-TRK interaction and TRK activation, which results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress TRK and/or express NTRK fusion proteins.
CAS Number

2097002-61-2
Structure Available

Yes
Salt Form

No
Molecular Formula

C₂₀H₂₁FN₆O
Molecular Weight

380.43
Cell Permeable

Yes
Purity

≥98% by HPLC
Solubilities

DMSO (>10 mg/ml)
Handling

Protect from air and light
Tag Line

A potent and selective TRK (tropomyosin-related-kinase) inhibitor
Storage Condition

-20°C
Shipping Condition

gel pack
Shelf Life

36 months
PubChem CID

129103609
PubChem CID Link
SMILES

CC1CCC2=NC=C(C=C2C3CCCN3C4=NC5=C(C=NN5C=C4)C(=O)N1)F
InChi

InChI=1S/C20H21FN6O/c1-12-4-5-16-14(9-13(21)10-22-16)17-3-2-7-26(17)18-6-8-27-19(25-18)15(11-23-27)20(28)24-12/h6,8-12,17H,2-5,7H2,1H3,(H,24,28)/t12-,17-/m1/s1
InChi Key

OEBIHOVSAMBXIB-SJKOYZFVSA-N
Data Sheet Link
MSDS Available

Yes

Name

Cloning, Molecular
Concept

Scope note: The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.
Tree numbers
- E05.393.220
Qualifiers

drug effects, methods, radiation effects