BAY 1135626 is used to synthesize BAY 1129980, and use to anti-tumor research. BAY 1129980 is a Auristatin-based anti-C4.4A (LYPD3) antibody–agent conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research.
C4.4A (LYPD3) is a protein expressed in non-small cell lung cancer (NSCLC), with scarcely expressing in normal tissues[1].BAY 1135626 can be synthesized into BAY 1129980 (C4.4A-ADC), shows a strong anti-proliferative effect on C4.4A expressing cell lines[1]. BAY 1129980 (0.001-100 nM; 72 h) inhibits the proliferation of A549 lung cancer cell lines transfected with C4.4A[1].BAY 1129980 (0.001-100 nM; 72 h) exhibits high and selective efficacy on hC4.4A:A549 cells in vitro[1].
BAY 1129980 (1.9-7.5 mg/kg; i.v.; 20 d) inhibits tumor growth in vivo in mouse[1].BAY 1129980 with a repeated dosing (15 mg/kg; i.v.; 21 d for 1st cycle and 57 d for 2nd cycle) is well tolerated without changing the sensitivity to the treatment[1].
References:
[1]. Willuda J, et al. Preclinical Antitumor Efficacy of BAY 1129980-a Novel Auristatin-Based Anti-C4.4A (LYPD3) Antibody-Drug Conjugate for the Treatment of Non-Small Cell Lung Cancer. Mol Cancer Ther. 2017 May. 16(5):893-904.