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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Bosutinib
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
380843-75-4
- 规格：
200mg/50mg/5mg/1mg/100mg/10mg
| 规格： | 200mg | 产品价格： | ￥1790.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥840.0 |
| 规格： | 5mg | 产品价格： | ￥272.0 |
| 规格： | 1mg | 产品价格： | ￥130.0 |
| 规格： | 100mg | 产品价格： | ￥1090.0 |
| 规格： | 10mg | 产品价格： | ￥440.0 |
Bosutinib是 Src/Abl 的双抑制剂。
| 基本信息 | |
| CAS | No.380843-75-4 |
| 中文名称 | 伯舒替尼 |
| 英文名称 | Bosutinib |
| 别名 | SKI-606 |
| 分子式 | C26H29Cl2N5O3 |
| 分子量 | 530.45 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥99% |
| 外观(性状) | White to yellow Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC | EINECS 700-455-1 |
| MDL | MFCD07367846 |
| SMILES | CN1CCN(CC1)CCCOC2=C(C=C3C(NC4=CC(OC)=C(C=C4Cl)Cl)=C(C=NC3=C2)C#N)OC |
| 靶点 | Src;Abl |
| 通路 | Protein Tyrosine Kinase/RTK |
| 背景说明 | Bosutinib是 Src/Abl 的双抑制剂。 |
| 生物活性 | Bosutinib（SKI-606） is a dual Src/Abl inhibitor with IC50s of 1.2 nM and 1 nM, respectively.[1] |
| IC50 | Src: 1.2nM;Abl: 1nM[1] |
| In Vitro | SKI-606(bosutinib)，a selective Src family kinase inhibitor，on human cancer cells derived from breast cancer patients to assess its potential for breast cancer treatment. The results show that SKI-606 caused a decrease in cell motility and invasion of breast cancer cell lines with an IC50 of f250 nmol/L，which was also the IC50 for inhibition of cellular Src kinase activity in intact tumor cells. These changes were accompanied by an increase in cell-to-cell adhesion and membrane localization of B-catenin. Analysis of downstream effectors of Src revealed that SKI-606 inhibits the phosphorylation of focal adhesion kinase(FAK)，proline-rich tyrosine kinase 2(Pyk2)，and Crk-associated substrate(p130Cas)，with an IC50 similar to inhibition of cellular Src kinase. SKI-606 inhibits signaling pathways involved in controlling tumor cell motility and invasion，suggesting that SKI-606 is a promising therapeutic for breast cancer.[2] SKI-606，a potent inhibitor of Src and Abl kinases. SKI-606 inhibited Src autophosphorylation with an IC(50)of approximately 0.25 micromol/L in HT29 cells. Phosphorylation of Tyr(925)of focal adhesion kinase，a Src substrate，was reduced by similar concentrations of inhibitor. [3] |
| 细胞实验 | On oral administration to nude mice at the lowest efficacious dose，peak plasma concentrations of approximately 3 micromol/L，an oral bioavailability of 18%，and a t(1/2)of 8.6 hours were observed. SKI-606 was orally active in s.c. colon tumor xenograft models and caused substantial reductions in Src autophosphorylation on Tyr(418)in HT29 and Colo205 tumors. SKI-606 inhibited HT29 tumor growth on once daily administration，whereas twice daily administration was necessary to inhibit Colo205，HCT116，and DLD1 tumor growth. [3] |
| 细胞实验 | Briefly，f5，000 cells were seeded in each well of a 96-well plate and allowed to adhere before the addition of 0.01% DMSO or 0.1，0.3，and 1 umol/L of SKI-606. After 2to 6 d of incubation at 37℃ in 5% CO2，MTS reagent was added to each well for 30 min and absorbance measured at 490 nm.[2] |
| 动物实验 | In HT29 xenograft studies，SKI-606 was given by oral gavage once daily to mice with tumors ranging from 200 to 300mg. A dose-dependent antitumor response was observed in those mice given doses of 25 to 150 mg/kg over a 21-day period(P < 0.003 in Student’s two-tailed t test in the group that received the 25 mg/kg/d). Although the once daily 25 mg/kg dose was not consistently active，the higher doses were reproducibly effective. No deaths occurred and no weight loss was observed in animals given SKI-606 at 150 mg/kg. [3] |
| 数据来源文献 | [1]. Boschelli DH， et al. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J Med Chem， 2001， 44(23)， 3965-3977. [2]. Vultur A， et al. SKI-606 (bosutinib)， a novel Src kinase inhibitor， suppresses migration and invasion of human breast cancer cells. Mol Cancer Ther， 2008， 7(5)， 1185-1194. [3]. Golas JM， et al. SKI-606， a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Res， 2005， 65(12)， 5358-5364. |
| 单位 | 瓶 |
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