LOXO-101

Alternative_name

3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide; ARRY 470; Larotrectinib
Description

LOXO-101 is a potent, ATP-competitive TRK inhibitor with IC₅₀s in low nanomolar range for inhibition of all TRK family members in binding and cellular assays, with 100-fold selectivity over other kinases, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.
CAS Number

1223403-58-4
Structure Available

Yes
Salt Form

No
Molecular Formula

C₂₁H₂₂F₂N₆O₂
Molecular Weight

428.44
Cell Permeable

Yes
Purity

≥98% by HPLC
Solubilities

DMSO (~5 mg/ml)
Handling

Protect from air and light
Tag Line

A potent, ATP-competitive TRK inhibitor
Storage Condition

-20°C
Shipping Condition

gel pack
Shelf Life

36 months
PubChem CID

46188928
PubChem CID Link
SMILES

C1CC(N(C1)C2=NC3=C(C=NN3C=C2)NC(=O)N4CCC(C4)O)C5=C(C=CC(=C5)F)F
InChi

InChI=1S/C21H22F2N6O2/c22-13-3-4-16(23)15(10-13)18-2-1-7-28(18)19-6-9-29-20(26-19)17(11-24-29)25-21(31)27-8-5-14(30)12-27/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31)/t14-,18+/m0/s1
InChi Key

NYNZQNWKBKUAII-KBXCAEBGSA-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