产品
编 号：F286115
分子式：C26H29N5O2
分子量：443.54
分子式：C26H29N5O2
分子量：443.54
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 234772-64-6
产品详情
生物活性：
CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity.
体内研究：
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.
体外研究：
CGP77675 dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC50 value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC50 value of 16.7 nM. These IC50 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 IC50 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 (IC50 values 0.2, 0.5, and 5.7μM) in IC8.1 cells.
CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity.
体内研究：
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.
体外研究：
CGP77675 dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC50 value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC50 value of 16.7 nM. These IC50 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 IC50 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 (IC50 values 0.2, 0.5, and 5.7μM) in IC8.1 cells.
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