Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CGP77675 (ZINC1488120) 是一种有效的选择性 Src 家族激酶抑制剂,IC50 为 5-20 和 40 nM,用于肽底物的磷酸化和纯化的 Src 的自磷酸化。 CGP77675 具有抗癌活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 498 | 现货 | ||
2 mg | ¥ 719 | 现货 | ||
5 mg | ¥ 1,160 | 现货 | ||
10 mg | ¥ 1,870 | 现货 | ||
25 mg | ¥ 3,730 | 现货 | ||
50 mg | ¥ 5,450 | 现货 |
产品描述 | CGP77675 (ZINC1488120) is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylation of purified Src. CGP77675 exhibits anticancer activity. |
靶点活性 | EGFR:0.15 μM (IC50), KDR:1.0 μM (IC50), v-ABL:0.31 μM (IC50), Lck:0.29 μM (IC50), Src:0.02 μM (IC50) |
体外活性 | CGP77675 inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 20, 150, 1000, 310, and 290 nM, respectively. CGP77675 dose-dependently inhibits phosphorylation of poly-Glu-Tyr (IC50 = 5.5 nM), and of the optimal Src substrate (OSS) peptide (IC50 = 16.7 nM). In rat fetal long bone cultures, CGP77675 inhibits the parathyroid hormone-induced bone resorption (IC50 = 0.8 μM). In Src-overexpressing IC8.1 cells, CGP77675 (0.04-10 μM) dose-dependently inhibits phosphorylation of Fak (IC50 = 0.2 μM) and paxillin(IC50 = 0.5 μM), but not of Src(IC50 = 5.7μM)[3]. |
体内活性 | In female rats of the Sprague-Dawley-derived strain Tif:RAlf, CGP77675 (10 and 50 mg/kg;orally) partially prevents bone loss and rescues bone microarchitectural features. In male mice, CGP77675 (1, 5, and 25 mg/kg; s.c.) inhibits IL-1β-induced hypercalcemia without affecting serum amyloid protein levels[3]. |
别名 | CGP-77675, 1-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol, ZINC1488120, CGP 77675 |
分子量 | 443.54 |
分子式 | C26H29N5O2 |
CAS No. | 234772-64-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (56.4 mM), Sonication and heating are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2546 mL | 11.2729 mL | 22.5459 mL | 56.3647 mL |
5 mM | 0.4509 mL | 2.2546 mL | 4.5092 mL | 11.2729 mL | |
10 mM | 0.2255 mL | 1.1273 mL | 2.2546 mL | 5.6365 mL | |
20 mM | 0.1127 mL | 0.5636 mL | 1.1273 mL | 2.8182 mL | |
50 mM | 0.0451 mL | 0.2255 mL | 0.4509 mL | 1.1273 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。
CGP77675 234772-64-6 Angiogenesis Cytoskeletal Signaling JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR VEGFR Bcr-Abl Src CGP-77675 1-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol ZINC1488120 ZINC 1488120 CGP 77675 ZINC-1488120 Inhibitor inhibitor inhibit