lapatinib

Lapatinib (GW572016) is an inhibitor of ErbB2 and EGFR (IC50=9.2/10.8 nM) with oral activity. Lapatinib has antitumor activity and can be used to treat advanced or metastatic breast cancer with HER2 overexpression.

Lapatinib Ditosylate (Tykerb ditosylate) is an effective EGFR and ErbB2 inhibitor (IC50: 10.8/9.2 nM for EGFR/ErbB2).

Lapatinib ditosylate (Lapatinib tosilate) monohydrate is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib ditosylate monohydrate therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury.

Lapatinib tosylate (GW572016), a robust and orally administered inhibitor specifically targeting the tyrosine kinase domains of ErbB-2 and EGFR, exhibits inhibitory concentration 50 (IC50) values of 10.2 nM and 9.8 nM against purified EGFR and ErbB-2, respectively.

Lapatinib-d4 is a deuterated compound of Lapatinib. Lapatinib has a CAS number of 231277-92-2. Lapatinib is a dual inhibitor of Lapatinib is a dual ErbB2 EGFR (IC50: 9.2 10.8 nM) inhibitor

Sapitinib (AZD-8931) , a reversible, ATP competitive inhibitor of EGFR(IC50=4 nM), ErbB2(IC50=3 nM) and ErbB3(IC50=4 nM), is more effective over Gefitinib or Lapatinib against NSCLC cell, 100-fold more specific for the ErbB family over MNK1 and Flt.

SARS-CoV-2-IN-110 (compound Bb1) is an inhibitor of SARS-CoV-2, demonstrating antiviral efficacy with an EC50 of 1.10 μM, and significantly reduced toxicity compared to Lapatinib. The compound exhibits a CC50 of greater than 100 μM against SARS-CoV-2, with a selectivity index (SI) exceeding 91.

HQY1428 is an orally active CDK12 inhibitor. It impedes DNA replication, causing cell cycle arrest at the G2/M phase in SKOV3 cells, and induces DNA double-strand breaks as well as apoptosis. In the SKOV3 xenograft mouse model, HQY1428 demonstrates antitumor activity. Additionally, when combined with the HER2 inhibitor Lapatinib in the NCI-N87 xenograft mouse model, HQY1428 produces a synergistic therapeutic effect.

Potent EGFR Degrader (DC50 values are 39.2 nM for wild-type EGFR in OVCAR8 cells and 736 nM for Exon20Ins mutated EGFR in HeLa cells). Also degrades HER2. Comprises the EGFR inhibitor lapatinib (Cat. No. 6811) joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. Inhibits proliferation of HER2-driven breast cancer cell lines (IC50 = 102 nM for SKBr3 cells).