Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CP-724714 (CP724714) 是一种高效、选择性口服活性的 ErbB2 (HER2)酪氨酸激酶抑制剂,IC50为 10 nM。它能抑制完整细胞中 ErbB2 受体的自磷酸化,具有抗肿瘤活性。它对 EGFR 激酶有明显的选择性,IC50值为6400 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 275 | 现货 | ||
2 mg | ¥ 392 | 现货 | ||
5 mg | ¥ 693 | 现货 | ||
10 mg | ¥ 1,250 | 现货 | ||
25 mg | ¥ 2,290 | 现货 | ||
50 mg | ¥ 3,990 | 现货 | ||
100 mg | ¥ 5,530 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 763 | 现货 |
产品描述 | 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. |
靶点活性 | HER2:10 nM, ErbB2:10 nM |
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. |
别名 | CP724714, CP 724714 |
分子量 | 469.54 |
分子式 | C27H27N5O3 |
CAS No. | 383432-38-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (117.14 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1297 mL | 10.6487 mL | 21.2974 mL | 53.2436 mL |
5 mM | 0.4259 mL | 2.1297 mL | 4.2595 mL | 10.6487 mL | |
10 mM | 0.213 mL | 1.0649 mL | 2.1297 mL | 5.3244 mL | |
20 mM | 0.1065 mL | 0.5324 mL | 1.0649 mL | 2.6622 mL | |
50 mM | 0.0426 mL | 0.213 mL | 0.4259 mL | 1.0649 mL | |
100 mM | 0.0213 mL | 0.1065 mL | 0.213 mL | 0.5324 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CP-724714 383432-38-0 Angiogenesis Apoptosis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR mice CP724714 Epidermal growth factor receptor autophosphorylation athymic inhibit cycle HER1 ErbB-1 Inhibitor oral cell CP 724714 selective inhibitor