Capmatinib (dihydrochloride hydrate)

• UNSPSC Description:

  Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase[1][2][3].

• Target Antigen:

  Apoptosis; c-Met/HGFR

• Type:

  Reference compound

• Related Pathways:

  Apoptosis;Protein Tyrosine Kinase/RTK

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/capmatinib-dihydrochloride-hydrate.html

• Smiles:

  O=C(NC)C1=CC=C(C2=NN3C(N=C2)=NC=C3CC4=CC=C5N=CC=CC5=C4)C=C1F.O.Cl.Cl

• Molecular Weight:

  503.36

• References & Citations:

  [1]Liu X, et al. A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3. Clin Cancer Res. 2011 Nov 15;17(22):7127-38.|[2]Baltschukat S, et al. Capmatinib (INC280) Is Active Against Models of Non-Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation. Clin Cancer Res. 2019 May 15;25(10):3164-3175.|[3]Dhillon S. Capmatinib: First Approval. Drugs. 2020 Jul;80(11):1125-1131.

• Shipping Conditions:

  Room Temperature

• CAS Number:

  1865733-40-9