Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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1 mg | 在庫あり | ¥ 10,000 | |||
2 mg | 在庫あり | ¥ 15,000 | |||
5 mg | 在庫あり | ¥ 26,000 | |||
10 mg | 在庫あり | ¥ 42,000 | |||
25 mg | 在庫あり | ¥ 85,500 | |||
50 mg | 在庫あり | ¥ 137,000 |
説明 | 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. |
ターゲット&IC50 | 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) |
In vitro | 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]. |
In vivo | 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 | 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.
You can also refer to dose conversion for different animals. 詳細
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CGP77675 234772-64-6 Angiogenesis Cytoskeletal Signaling JAK/STAT signaling Tyrosine Kinase/Adaptors Src Bcr-Abl VEGFR EGFR 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