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- T30855L
- 2026年07月07日
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25mg/50mg/100mg
| 规格： | 25mg | 产品价格： | ￥8480.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥11040.0 |
| 规格： | 100mg | 产品价格： | ￥14000.0 |
Product Introduction
Bioactivity
| 名称 | CGP77675 hydrate |
| 描述 | CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src ( IC 50 s of 5-20 and 40 nM, respectively),and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC 50 s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. CGP77675 hydrate can be useful for the treatment of diseases associated with elevated bone loss and has anticancer activity[1]. |
| 体外活性 | CGP77675 hydrate inhibits phosphorylation of poly-Glu-Tyr in a dose-dependent manner 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) [1]. CGP77675 hydrate inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC 50 of 0.8 μM [1]. CGP77675 hydrate (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 [1]. 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. |
| 体内活性 | CGP77675 hydrate (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits hypercalcemia induced by IL-1β in Mice [1]. CGP77675 hydrate (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]. 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. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 关键字 | CGP-77675 hydrate | CGP77675 hydrate | CGP 77675 Hydrate |
| 相关产品 | Pelitinib | MCB-613 | Dasatinib monohydrate | SI-2 hydrochloride | Vemurafenib | TAK-901 | Tofacitinib | Staurosporine | Dasatinib | Nintedanib | Ibrutinib | iHCK-37 |
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文献和实验，使其与抗体、酶等生物大分子结合后，不受位阻效应的影响，更易发挥生物索的活性作用。BCNHS的制备是先用6－氨基己糖与生物素连接制得长臂生物素，然后再将其活化。 标记蛋白质醛基的活化生物素 用于此类标记的活化生物素有两种：生物衰酰肼（biotin hydrazine，BHZ）和肼化生物胞素（biocyin hydrazine，BCHZ）。BHZ是水合肼（hydraine hydrate）与生物素的合成物，主要用于偏酸性糖蛋白的生物素标记。也可在BHZ侧链上添加一个赖氨酸基团作为连结臂，减少标记
度使非特异性的杂交体减少。由于RNA杂交的稳定性，应用cRNA探针进行细胞或组织的原位杂交时的杂交温度比其它核酸探针要高10～15℃。实验证明，cRNA产生的信号比双链cDNA要强。单链的RNA探针其杂交信号大于双链的cDNA的约8倍。 5．硫酸葡聚糖（Dextran sulphate）和甲酰胺（formamide） 硫酸葡聚糖是核酸杂交液中仅次于甲酰胺的一种组成成份。在杂交液中，甲酰胺占50%左右，而硫酸葡聚糖占10%左右。它是一种大分子的多聚胺化合物，具有极强的水合（hydrate
使非特异性的杂交体减少。由于RNA杂交的稳定性，应用cRNA探针进行细胞或组织的原位杂交时的杂交温度比其它核酸探针要高10～15℃。实验证明，cRNA产生的信号比双链cDNA要强。单链的RNA探针其杂交信号大于双链的cDNA的约8倍。 5．硫酸葡聚糖（Dextran sulphate）和甲酰胺（formamide）硫酸葡聚糖是核酸杂交液中仅次于甲酰胺的一种组成成份。在杂交液中，甲酰胺占50%左右，而硫酸葡聚糖占10%左右。它是一种大分子的多聚胺化合物，具有极强的水合（hydrate）作用
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