nci-n87

CH5138303 是一种可口服的 Hsp90 抑制剂，Kd 为 0.48 nM。

Dxd (OQM5SD32BQ) 是一种有效的DNA 拓扑异构酶 I 抑制剂（IC50= 0.31 μM）。Dxd用作HER2靶向ADC 的偶联药物。

HQY1428 是一种可口服的 CDK12 抑制剂。它通过抑制 DNA 复制使 SKOV3 细胞在 G2/M 期停滞，并诱导 DNA 双链断裂和细胞凋亡 (Apoptosis)。HQY1428 在 SKOV3 异种移植小鼠模型中显示出抗肿瘤活性。在 NCI-N87 异种移植小鼠模型中，HQY1428 与 HER2 抑制剂 Lapatinib 联合使用，能够产生协同的治疗效果。

Selatinib 是一种具有口服活性和有效性的 EGFR 和 ErbB2 双重抑制剂，具有抗癌活性，抑制 NCI-N87 肿瘤细胞生长。

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为一种Hsp90抑制剂，具有41 nM 的IC50值，能有效抑制癌细胞增殖，并在裸鼠模型中显著抑制NCI-N87和HT-29肿瘤生长。

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).