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234772-64-6

中文名称 CGP 77675; CGP-77675
英文名称 CGP77675
CAS 234772-64-6
分子式 C26H29N5O2
分子量 443.54
MOL 文件 234772-64-6.mol
更新日期 2023/03/20 15:41:19
234772-64-6 结构式 234772-64-6 结构式

基本信息

中文别名
化合物 T30855
化合物CGP77675
英文别名
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]-

物理化学性质

储存条件2-8°C
溶解度二甲基亚砜:>10mg/mL
形态粉末
颜色白色至米色

安全数据

WGK Germany3
CGP 77675; CGP-77675价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/05/22HY-W062835CGP77675234772-64-61 mg636元
2025/05/22HY-W062835CGP 77675; CGP-77675
CGP77675
234772-64-610 mM * 1 mLin DMSO1366元
2025/05/22HY-W062835CGP 77675; CGP-77675
CGP77675
234772-64-65mg1400元

常见问题列表

生物活性
CGP77675 是一种有效的 Src 家族激酶抑制剂。CGP77675 抑制 Src,EGFR,KDR,v-Abl 和 Lck,IC50 分别为 0.02、0.15、1.0、0.31 和 0.29 μM。具有抗肿瘤活性。
靶点

IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)

体外研究

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.
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.
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