2803679-07-2
2803679-07-2
Chemical Structure
LPM4870108
- CAS. Nr.: 2803679-07-2
- Formula:C20H19FN6O3
- Molecular Weight:410.40
IUPAC Name: (S,3'E,4'E)-5'-fluorospiro[cyclopropane-1,6'-4-oxa-7-aza-2(4,3)-morpholina-1(5,3)-pyrazolo[1,5-a]pyrimidina-3(3,2)-pyridinacyclooctaphan]-8'-one
InChIKey: UMZFBMAHLWQSBF-OAHLLOKOSA-N
SMILES: O=C1C2=C3N(C=CC(N4[C@@H](C5=CC(F)=CN=C5OCC6(N1)CC6)COCC4)=N3)N=C2
Biological Activity: 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].
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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. | |||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
