LPM4870108
LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC50s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkAG595R and TrkAG667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC50=182 nM) . LPM4870108 exhibits anti-tumor activity[1][2].
Product Specifications
CAS Number
2803679-07-2
UNSPSC
12352005
Target
Trk Receptor
Type
Reference compound
Related Pathways
Neuronal Signaling; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/lpm4870108.html
Solubility
10 mM in DMSO
Smiles
O=C1C2=C3N(C=CC(N4[C@@H](C5=CC(F)=CN=C5OCC6(N1)CC6)COCC4)=N3)N=C2
Molecular Formula
C20H19FN6O3
Molecular Weight
410.40
References & Citations
[1]Liu Z, et, al. Discovery of the Next-Generation Pan-TRK Kinase Inhibitors for the Treatment of Cancer. J Med Chem. 2021 Jul 22;64 (14) :10286-10296.|[2]Duan S, et, al. Assessment of the toxicity and toxicokinetics of the novel potent tropomyosin receptor kinase (Trk) inhibitor LPM4870108 in rhesus monkeys. Regul Toxicol Pharmacol. 2021 Jun;122:104886.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
TrkA; TrkC
Frequently Asked Questions
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