CGP77675
作者：齊岳
發布時間：2023-08-25
09:00:17
點擊數：
產品名稱：CGP77675
產品描述：
| 產品描述 | CGP77675 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. |
| 靶點活性 | 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) |
| 體外活性 | 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]. |
| 體內活性 | 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]. |
| 別名 | 1-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol, ZINC1488120 |
| 分子量 | 443.54 |
| 分子式 | C26H29N5O2 |
| CAS No. | 234772-64-6 |
存儲
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 25 mg/mL (56.4 mM),Need ultrasonic and warming
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
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