CGP77675

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CGP77675  纯度: 98.85%

CGP77675 是一种口服有效的 Src 家族激酶抑制剂。CGP77675 抑制肽底物的磷酸化和纯化 Src 的自磷酸化 (IC50 分别为 5-20 和 40 nM)，并且还抑制 Src，EGFR，KDR，v-Abl 和 Lck，IC50 分别为 20、150、1000、310 和 290 nM。具有抗肿瘤活性。

CGP77675

CGP77675 Chemical Structure

CAS No. : 234772-64-6

规格 价格 是否有货 数量
5 mg ￥5500 In-stock
10 mg ￥8250 In-stock
50 mg   询价  
100 mg   询价  

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CGP77675 相关产品

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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[1].

IC50 & Target

IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)[1]
体外研究
(In Vitro)

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)[1].
CGP77675 inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC50 of 0.8 μM[1].
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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

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
(In Vivo)

CGP77675 (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice[1].
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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body[1]
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[1]
Dosage: 10 and 50 mg/kg
Administration: Administered orally; twice a day for 6 weeks
Result: Partly prevented bone loss.

分子量

443.54

Formula

C26H29N5O2
CAS 号

234772-64-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献

  • [1]. Missbach M, et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellularsubstrates and reduces bone resorption in vitro and in rodent models in vivo. Bone. 1999 May;24(5):437-49.

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