nci-n87

CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.

Dxd (OQM5SD32BQ) is a potent DNA topoisomerase I inhibitor (IC50= 0.31 μM). Dxd was used as a conjugate drug for HER2-targeted ADCs.

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.

HER2-IN-19 (Compound 10e) is a potent inhibitor of HER2 and EGFR, with IC50 values of 0.87 and 3.5 nM, respectively. It shows significant inhibitory activity against tumor cells, with IC50 values for NCI-N87, BT474, and BaF3-HER2YVMA being 1.63 nM, 15.17 nM, and 1.49 nM, respectively.

Selatinib is an orally active and potent dual inhibitor of EGFR and ErbB2 with anticancer activity that inhibits the growth of NCI-N87 tumor cells.

Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1]. Ipivivint (SW480 cells; 0.01~10 μM; 1 hour) potently inhibits SRSF5/6 phosphorylation[1].Ipivivint (SW480 cells; 0.03 μM~3 μM; 48 hour) induced apoptosis[1]..Ipivivint (HEK-293T cells; 0.03 μM~3 μM; 1 hour) inhibits Wnt/β-catenin signaling induced by Wnt3a[1].Ipivivint (SW480 cells; 0.3~10 μM; 6 hour) increases nuclear speckle enlargement[1].Ipivivint (SW480 cells; 0.3~3μM; 24hours) significantly decreases expression of Wnt target genes (AXIN2, LEF1, MYC, and TCF7) and TCF7L2. SM08502 (SW480 cells; 0.03~3μM; 24hours) inhibits cytoplasmic or nuclear fractions protein expression. Ipivivint (NCI-N87 cells) inhibits proliferation[1].Ipivivint strongly inhibits Wnt pathway signaling activity (EC50 = 0.046 μM) in SW480 colon cancer cells[1]. Ipivivint (25 mg/kg; p.o.) potently inhibits tumor SRSF6 phosphorylation[1]. [1]. Tam BY, et al. The CLK inhibitor SM08502 induces anti-tumor activity and reduces Wnt pathway gene expression in gastrointestinal cancer models. Cancer Lett. 2020;473:186-197.

BX-2819 is an Hsp90 inhibitor that exhibits potent antiproliferative activity with an IC50 of 41 nM . It effectively suppresses the growth of NCI-N87 and HT-29 tumor cells in nude mice[1].

Benzyl ferulate has antimicrobial activity. It also shows good anti-proliferative against three gastro-intestinal cancer cell lines(HCT-116 colon carcinoma, KYSE-30 oesophageal squamous cancer, and NCI-N87 gastric carcinoma).