TNO155

SHP-2抑制剂(IC50=0.011µM)；在52种激酶和磷酸酶中对SHP-2具有选择性（所有IC50s=>10µM）；降低KYSE-520人食管癌细胞中的ERK磷酸化并抑制其增殖（IC50s分别为0.011和0.1µM）；与达拉非尼和曲美替尼协同作用，抑制表达B-RAFV600E的HT-29、RKO和MDST8结直肠癌细胞的增殖；以每天两次2.5、10和20mg/kg的剂量降低KYSE-520小鼠异种移植模型中的肿瘤生长。A SHP-2 inhibitor (IC50 = 0.011 µM); selective for SHP-2 over a panel of 52 kinases and phosphatases (IC50s = >10 µM for all); decreases phosphorylation of ERK in, and inhibits proliferation of, KYSE-520 human esophageal cancer cells (IC50s = 0.011 and 0.1 µM, respectively); acts synergistically with dabrafenib and trametinib to inhibit proliferation of B-RAFV600E-expressing HT-29, RKO, and MDST8 colorectal cancer cells; reduces tumor growth in a KYSE-520 mouse xenograft model at 2.5, 10, and 20 mg/kg twice per day.分子式C18H24ClN7OS分子量421.9ClC1=C(N)N=CC=C1SC2=C(N)N=C(N3CCC4([C@H](N)[C@H](C)OC4)CC3)C=N2