234772-64-6
234772-64-6 結(jié)構(gòu)式
基本信息
化合物CGP77675
CGP 77675
CGP-77675
CGP77675 >=98% (HPLC)
1-(4-(4-Amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol
1-(2-{4-[4-Amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]phenyl}ethyl)piperidin-4-ol
4-Piperidinol, 1-[2-[4-[4-aMino-5-(3-Methoxyphenyl)-7H-pyrrolo[2,3-d]pyriMidin-7-yl]phenyl]ethyl]-
常見問題列表
IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)
CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC
50
s of 5-20 and 40 nM, respectively) .
CGP77675 dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC
50
value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC
50
value of 16.7 nM. These IC
50
values are similar to the value obtained with chicken Src (20 nM).
CGP77675 inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC
50
of 0.8 μM.
CGP77675 (0.04-10 μM; 2 hours) potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin, but has much less effect on Src (IC
50
values 0.2, 0.5, and 5.7μM) in IC8.1 cells.
Cell Viability Assay
| Cell Line: | MC3T3-E1 cells |
| Concentration: | 0.2, 1, and 5 μM |
| Incubation Time: | 3 days |
| Result: | Did not influence cell viability for up to 3 days of treatment. |
Western Blot Analysis
| Cell Line: | Src-overexpressing IC8.1 cells |
| Concentration: | 0.04, 0.2, 1, 5, and 10 μM |
| Incubation Time: | 2 hours |
| Result: | Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src. |
CGP77675 (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice.
CGP77675 (10 and 50 mg/kg; administered orally; twice a day for 6 weeks) partially prevents bone loss and rescues bone microarchitectural features in young ovx rats.
| Animal Model: | Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body |
| Dosage: | 1, 5, and 25 mg/kg |
| Administration: | Injected s.c.; twice a day |
| Result: | Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels. |
| Animal Model: | Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf |
| Dosage: | 10 and 50 mg/kg |
| Administration: | Administered orally; twice a day for 6 weeks |
| Result: | Partly prevented bone loss. |