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- Solarbio
- 北京
- IM2170
- 2025年12月22日
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- 详细信息
- 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：
Motesanib
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
453562-69-1
- 规格：
100mg/50mg/10mg/5mg
| 规格： | 100mg | 产品价格： | ￥2090.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥1490.0 |
| 规格： | 10mg | 产品价格： | ￥640.0 |
| 规格： | 5mg | 产品价格： | ￥530.0 |
| 基本信息 | |
| CAS | No.453562-69-1 |
| 英文名称 | Motesanib |
| 别名 | 莫替沙尼;AMG 706 |
| 分子式 | C22H23N5O |
| 分子量 | 373.45 |
| 溶解性 | Soluble in DMSO ≥10mg/mL |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD10567689 |
| SMILES | CC1(CNC2=C1C=CC(=C2)NC(=O)C3=C(N=CC=C3)NCC4=CC=NC=C4)C |
| InChIKey | RAHBGWKEPAQNFF-UHFFFAOYSA-N |
| InChI | InChI=1S/C22H23N5O/c1-22(2)14-26-19-12-16(5-6-18(19)22)27-21(28)17-4-3-9-24-20(17)25-13-15-7-10-23-11-8-15/h3-12，26H，13-14H2，1-2H3，(H，24，25)(H，27，28) |
| PubChem CID | 11667893 |
| 靶点 | VEGFR1/2/3 |
| 通路 | Angiogenesis;Protein Tyrosine Kinase/RTK |
| 背景说明 | Motesanib 是一种有效的 VEGFR1/2/3 的 ATP 竞争性抑制剂。 |
| 生物活性 | Motesanib (AMG 706) is a potent ATP-competitive inhibitor of?VEGFR1/2/3?with?IC50s?of 2 nM/3 nM/6 nM， respectively， and has similar activity against Kit， and is appr 10-fold more selective for VEGFR than PDGFR and Ret.[1-3] |
| In Vitro | Motesanib has broad activity against the human VEGFR family， and displays > 1000 selectivity against EGFR， Src， and p38 kinase. Motesanib significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC50 of 10 nM， while displaying little effect at bFGF-induced proliferation with an IC50 of >3，000 nM. Motesanib also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC50 of 207 nM and 37 nM， respectively， but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells[1].?Althouth displaying little antiproliferative activity on cell growth of HUVECs alone， Motesanib treatment significantly sensitizes the cells to fractionated radiation[2]. |
| 细胞实验 | Motesanib (100 mg/kg) significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib twice daily or once daily potently inhibits， in a dose-dependent manner， VEGF-induced angiogenesis using the rat corneal model with ED50 of 2.1 mg/kg and 4.9 mg/kg， respectively. Motesanib induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells[1]. Motesanib in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models[2].?Motesanib treatment also induces significant dose-dependent reductions in tumor growth and blood vessel density of MCF-7， MDA-MB-231， or Cal-51 xenografts， which can be markedly enhanced when combined with docetaxel or tamoxifen[3]. |
| 细胞实验 | Cells are preincubated for 2 hours with different concentrations of Motesanib， and exposed with 50 ng/mL VEGF or 20 ng/mL bFGF for an additional 72 hours. Cells are washed twice with DPBS， and plates are frozen at -70°C for 24 hours. Proliferation is assessed by the addition of CyQuant dye， and plates are read on a Victor 1420 workstation. IC50 data are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equatio.[1-3] |
| 动物实验 | A431 cells are cultured in DMEM (low glucose) with 10% FBS and penicillin/streptomycin/glutamine. Cells are harvested by trypsinization， washed， and adjusted to a concentration of 5×107/mL in serum-free medium. Animals are challenged s.c. with 1×107 cells in 0.2 mL over the left flank. Approximately 10 days thereafter， mice are randomized based on initial tumor volume measurements and treated with either vehicle (Ora-Plus) or Motesanib. Tumor volumes and body weights are recorded twice weekly and/or on the day of sacrifice. Tumor volume is measured with a Pro-Max electronic digital caliper and calculated using the formula length (mm)×width (mm)×height (mm) and expressed in mm3. Data are expressed as mean±SE. Repeated measures ANOVA followed by Scheffe post hoc testing for multiple comparisons is used to evaluate the statistical significance of observed differences.[1-3] |
| 激酶实验 | Optimal enzyme， ATP， and substrate (gastrin peptide) concentrations are established for each enzyme using homogeneous time-resolved fluorescence (HTRF) assays. Motesanib is tested in a 10-point dose-response curve for each enzyme using an ATP concentration of two-thirds Km for each. Most assays consist of enzyme mixed with kinase reaction buffer [20 mM Tris-HCl (pH 7.5)， 10 mM MgCl2， 5 mM MnCl2， 100 mM NaCl， 1.5 mM EGTA]. A final concentration of 1 mM DTT， 0.2 mM NaVO4， and 20 μg/mL BSA is added before each assay. For all assays， 5.75 mg/mL streptavidin-allophycocyanin and 0.1125 nM Eu-PT66 are added immediately before the HTRF reaction. Plates are incubated for 30 minutes at room temperature and read on a Discovery instrument. IC50 values are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equation.[1-3] |
| 数据来源文献 | [1]. Polverino A， et al. AMG 706， an oral， multikinase inhibitor that selectively targets vascular endothelial growth factor， platelet-derived growth factor， and kit receptors， potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer R [2]. Kruser TJ， et al. Augmentation of radiation response by motesanib， a multikinase inhibitor that targets vascular endothelial growth factor receptors. Clin Cancer Res， 2010， 16(14)， 3639-3647. [3]. Coxon A， et al. Broad antitumor activity in breast cancer xenografts by motesanib， a highly selective， oral inhibitor of vascular endothelial growth factor， platelet-derived growth factor， and Kit receptors. Clin Cancer Res， 2009， 15(1)， 110-118. |
| 单位 | 瓶 |
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IM2170 Motesanib 血管生成 索莱宝
￥530 - 2090
