Sacibertinib

Names

[ CAS No. ]:
1351941-69-9

[ Name ]:
Sacibertinib

Biological Activity

[Description]:

Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC50 value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[Target]

EGFR-TK phosphorylation:110 nM (EC50)

HER2:244 nM (EC50)

[In Vitro]

Sacibertinib has inhibitory activity against Sk-Br-3, SW620 cells with GI50s of 3.8 nM and 1.78 μM, and against CCRF-CEM/T, Fadu, BxPc-3 and AsPC-1 with IC50s of 5.6 μM, 101 nM, 337 nM and 1 μM, respectively[1].

[References]

[1]. Hesheng Zhang, et al. Cyanoquinoline derivatives. CA2802130A1 (Example 138)

[2]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 36, No. 2, 2022.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₂H₃₁ClN₆O₄

[ Molecular Weight ]:
599.08

Sacibertinib

Names

Biological Activity

Chemical & Physical Properties

Related Compounds