CGP 77675是一种高效的酪氨酸激酶Src抑制剂，其抑制纯化Src的自磷酸化反应的IC50为40nM。
Cas No.:234772-64-6
Sample solution is provided at 25 µL, 10mM.
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CGP 77675 is a kind of potent inhibitor of the tyrosine kinase Src which inhibits autophosphorylation of purified Src with an IC50 value of 40nM [1]. CGP 77675 potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin [1]. CGP 77675 has the potential to treat primary prostate cancers and diseases associated with elevated bone loss [1, 2].
CGP 77675 (0.1~10μM; 5d) inhibited the parathyroid hormone (PTH)-stimulated release of 45Ca in a concentration-dependent manner in the fetal rat long bone organ culture system [1]. CGP 77675 (2μM; 30min) reduced adhesion of PC3 cells; CGP 77675 (0.1~10μM; 30min) decreased [3H]-thymidine incorporation in serum-starved PC3 cells [2].
CGP 77675 (1, 5 and 25mg/kg; 4d; bid; s.c.) inhibited IL-1β-induced hypercalcemia, lowered the serum calcium concentration in the male mice; CGP 77675 (5 and 20mg/kg; 6 weeks; bid; p.o.) reduced bone loss induced by ovariectomy in the female Sprague-Dawley rats [1].
References:
[1] Missbach M, Jeschke M, Feyen J, et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellular substrates and reduces bone resorption in vitro and in rodent models in vivo [J]. Bone, 1999, 24(5): 437-449.
[2] Recchia I, Rucci N, Festuccia C, et al. Pyrrolopyrimidine c-Src inhibitors reduce growth, adhesion, motility and invasion of prostate cancer cells in vitro [J]. European journal of cancer, 2003, 39(13): 1927-1935.
CGP 77675是一种高效的酪氨酸激酶Src抑制剂，其抑制纯化Src的自磷酸化反应的IC50为 40nM[1]。CGP 77675能有效抑制Src底物Fak和paxillin的酪氨酸磷酸化[1]。CGP 77675具有治疗原发性前列腺癌以及与骨丢失相关的疾病的潜力[1, 2]。
CGP 77675（0.1~10μM；5d）在胎鼠长骨组织培养体系中，以浓度依赖的方式抑制了甲状旁腺激素（PTH）刺激的45Ca的释放[1]。CGP 77675（2μM；30min）降低了PC3细胞的黏附能力；CGP 77675（0.1~10μM；30min）减少了饥饿血清培养的PC3细胞中[3H]-胸腺嘧啶核苷的掺入[2]。
CGP 77675（1，5和25mg/kg；4d；bid；s.c.）抑制了IL-1β引起的高钙血症，降低了雄性小鼠的血钙浓度；CGP 77675（5和20mg/kg；6 weeks；bid；p.o.）减少雌性Sprague-Dawley大鼠因卵巢切除而产生的骨丢失[1]。
| Cell experiment [1]: | |
Cell lines | PC3 cells |
Preparation Method | PC3 cells were trypsinised, treated with 2μM of CGP 77675 (DMSO as a control) for 30min and re-plated in wells. Two hours later, morphological observation was performed. |
Reaction Conditions | 2μM; 30min |
Applications | CGP 77675 reduced adhesion of PC3 cells. |
| Animal experiment [2]: | |
Animal models | Male mice (Tif:MAGf) |
Preparation Method | The mice were received continuous injection of IL-1β (2mg/day) for 72h. CGP 77675 were administered subcutaneously twice daily. The last administration (seventh injection) was given in the morning of day 4 and 2h thereafter the mice were killed and blood samples were collected to determine the total serum calcium concentration. |
Dosage form | 1, 5 and 25mg/kg; 4d; bid; s.c. |
Applications | CGP 77675 inhibited IL-1β-induced hypercalcemia, lowered the serum calcium concentration in a dose dependent manner. |
References: | |
| Cas No. | 234772-64-6 | SDF | |
| 化学名 | 1-[2-[4-[4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]phenyl]ethyl]-4-piperidinol | ||
| Canonical SMILES | OC1CCN(CCC2=CC=C(N3C4=NC=NC(N)=C4C(C5=CC=CC(OC)=C5)=C3)C=C2)CC1 | ||
| 分子式 | C26H29N5O2 | 分子量 | 443.5 |
| 溶解度 | DMSO: 10 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2548 mL | 11.274 mL | 22.5479 mL |
| 5 mM | 451 μL | 2.2548 mL | 4.5096 mL |
| 10 mM | 225.5 μL | 1.1274 mL | 2.2548 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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