| 名称 | CP-724714 |
| 描述 | CP-724714 (CP724714) is an effective and selective HER2/ErbB2 inhibitor (IC50: 10 nM), >640-fold selectivity against EGFR, Abl, InsR, PDGFR, IRG-1R, Src, VEGFR2, c-Met etc. |
| 体外活性 | CP-724714 is obvious selectively against EGFR (IC50: 6.4 μM). CP-724714 is >1,000-fold less potent for IGF-1R, IR, VGFR2, PDGFRβ, Src, ZAP-70, JNK-2/3, and CDK-2/5. CP-724714 markedly reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain (IC50: 32 nM). CP-724714 inhibits the proliferation of erbB2-amplified cells including BT-474 (IC50: 0.25 μM) and SKBR3 (IC50: 0.95 μM). CP-724714 (1 μM) induces the accumulation of cells in G1 phase and a marked reduction in S-phase in BT-474 cells. CP-724714 inhibits TC transport in membrane vesicles expressing human bile salt export pump (IC50: 16 μM) and inhibits the major efflux transporter in bile canaliculi, MDR1 (IC50: 28 μM). |
| 体内活性 | CP-724714 (25 mg/kg) is rapidly absorbed after p.o. administration and causes reduction of tumor erbB2 receptor phosphorylation after dosing in FRE-erbB2 or BT-474 xenografts. CP-724,714 induces apoptosis in FRE-erbB2 xenograft-bearing (s.c.) mice and shows 50% tumor growth inhibition at 50 mg/kg, without mortality or weight loss. In MDA-MB-453, MDA-MB-231, LoVo (colon), and Colo-205 (colon) xenografts, CP-724714 also has great antitumor activity. In BT-474 xenografts, CP-724714 (30/100 mg/kg) reduces the extracellular signal-regulated kinase and Akt phosphorylation. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 55 mg/mL (117.14 mM)
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| 关键字 | mice | Epidermal growth factor receptor | autophosphorylation | Apoptosis | athymic | CP-724714 | inhibit | cycle | HER1 | ErbB-1 | Inhibitor | oral | EGFR | cell | selective |
| 相关产品 | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Gefitinib |
| 相关库 | 细胞凋亡化合物库 | 经典已知活性库 | 膜蛋白靶向化合物库 | ReFRAME 相关化合物库 | 酪氨酸激酶分子库 | 激酶抑制剂库 | 抑制剂库 | 肿瘤免疫治疗小分子化合物库 | 已知活性化合物库 | 抗癌活性化合物库 |
United States
