- Imatinib Mesylate (STI571)
- Amuvatinib (MP-470, HPK 56)
| MotesanibInhibitor of Flk-1/Flt-4/PDGFR-/c-Kit |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | Motesanib is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 values of 2 nM, 3 nM and 6 nM, respectively. | |||||
| Targets | VEGFR1 | VEGFR2 | VEGFR3 | |||
| IC50 | 2 nM | 3 nM | 6 nM | |||
| Kinase experiment [1]: | |
In vitro kinase assays | Optimal enzyme, ATP and substrate (gastrin peptide) concentrations were established for each enzyme using homogeneous time-resolved fluorescence (HTRF) assays. Motesanib was tested in a 10-point dose-response curve for each enzyme using an ATP concentration of two-thirds Km for each. Most assays consisted 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 was added before each assay. For all assays, 5.75 mg/mL streptavidin-allophycocyanin and 0.1125 nM Eu-PT66 were added immediately before the HTRF reaction. Plates were incubated for 30 mins at room temperature and read on a Discovery instrument. IC50 values were calculated. |
| Cell experiment [1]: | |
Cell lines | HUVECs |
Preparation method | This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
Reacting condition | 2 hrs |
Applications | In HUVECs, Motesanib significantly inhibited vascular endothelial growth factor (VEGF)-induced cell proliferation, with an IC50 value of 10 nM. However, it showed little effect on basic fibroblast growth factor (bFGF)-induced cell proliferation, with an IC50 value of > 3,000 nM. Similarly, Motesanib potently inhibited platelet-derived growth factor (PDGF)-induced cell proliferation as well as stem cell factor (SCF)-induced c-kit phosphorylation, with IC50 values of 207 nM and 37 nM, respectively. |
| Animal experiment [1]: | |
Animal models | A rat model of corneal angiogenesis, and nude mice bearing A431 cells |
Dosage form | 100 mg/kg; p.o.; q.d. or b.i.d. |
Applications | At the dose of 100 mg/kg, Motesanib significantly inhibited VEGF-induced vascular permeability in a time-dependent manner. In a rat model of corneal angiogenesis, Motesanib (q.d. or b.i.d.) substantially inhibited VEGF-induced angiogenesis in a dose-dependent manner. In nude mice bearing A431 cells, Motesanib also dose-dependently induced tumor regression by selectively targeting neovascularization in tumor cells. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Polverino A, Coxon A, Starnes C, 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 Res. 2006;66(17):8715-21. | |
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| Cas No. | 453562-69-1 | SDF | Download SDF |
| Synonyms | AMG706; AMG 706;AMG-706 | ||
| Chemical Name | N-(3,3-dimethyl-1,2-dihydroindol-6-yl)-2-(pyridin-4-ylmethylamino)pyridine-3-carboxamide | ||
| Canonical SMILES | CC1(CNC2=C1C=CC(=C2)NC(=O)C3=C(N=CC=C3)NCC4=CC=NC=C4)C | ||
| Formula | C22H23N5O | M.Wt | 373.46 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
AMG 706 (Motesanib)Description:IC50: Motesanib diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively [1].Vascular endothelial growth factor (VEGF) is an important signaling protein involved in both vasculogenesis (the formation of the circulatory system) and angiogenesis (the growth of blood vessels from pre-existing vasculature). Motesanib (AMG 706) is an orally administered small molecule belonging to angiokinase inhibitor class which acts as an antagonist of VEGF receptors, platelet-derived growth factor receptors, and stem cell factor receptors.In vitro: Motesanib diphosphate has broad activity against the human VEGFR family, and displays >1000 selectivity against EGFR, Src, and p38 kinase. Motesanib Diphosphate 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 Diphosphate 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 diphosphate treatment significantly sensitizes the cells to fractionated radiation [2]. In vivo: Oral administration of AMG 706 potently inhibited VEGF-induced angiogenesis in the rat corneal model and induced regression of established A431 xenografts. AMG 706 was well tolerated and had no significant effects o AMG 706n body weight or on the general health of the animals. Histologic analysis of tumor xenografts from AMG 706–treated animals revealed an increase in endothelial apoptosis and a reduction in blood vessel area that preceded an increase in tumor cell apoptosis. In summary, AMG 706 is an orally bioavailable, well-tolerated multikinase inhibitor that is presently under clinical investigation for the treatment of human malignancies [1]. Clinical trial: Motesanib was originally investigated for effectiveness against advanced nonsquamous non-small-cell lung cancer (NSCLC), with Phase II trials indicating an effectiveness comparable to bevacizumab when they were both used in combination with paclitaxel/carboplatin. However a later and more detailed Phase III trial failed to show any benefit for the treatment of NSCLC. A second Phase III trial was started in 2012, which focused on patients from Asian backgrounds (performed on the bases of subgroup analysis) however this also failed to meet its primary endpoint. The drug has undergone a Phase II evaluation as first-line therapy for breast cancer however this study found no evidence to support further investigation. Phase II testing against persistent or recurrent ovarian, fallopian tube and primary peritoneal carcinomas was also unsuccessful. There have also been 2 separate Phase II clinical trials for thyroid cancer which have both shown promising results (http://en.wikipedia.org/wiki/Motesanib). Reference:[1] Polverino A, Coxon A, Starnes C, 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 Res. 2006;66(17):8715-21.[2] Kruser TJ1 Wheeler DL, Armstrong EA, Iida M, Kozak KR, van der Kogel AJ, Bussink J, Coxon A, Polverino A, Harari PM. Augmentation of radiation response by motesanib, a multikinase inhibitor that targets vascular endothelial growth factor receptors. Clin Cancer Res. 2010;16(14):3639-47.
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20种蛋白质氨基酸都是α氨基酸。
其中除了甘氨酸外，其他氨基酸都具有旋光性，旋光性是由分子的空间构象引起的，你可以理解成像你的手掌一样，左右手的指头位置不同导致左右手的区别。根据旋光性分为L型（左型）和D型（右型）两种。
组成生命的氨基酸基本上都是L型。
在一些解热镇痛药注射剂中，为避免药物发黄变色，又加入了氨基酸抗氧化剂（除了亚硫酸氢钠外）。氨基酸抗氧化剂有哪些呢，常用的。查了一下，含S的抗氧化剂有甲硫氨酸(Met)和半胱氨酸(Cys)，是这些吗？还是有其他常用的呢？
氨基酸的结构通式：氨基酸是指一类含有羧基并在与羧基相连的碳原子下连有氨基的有机化合物。
人体所需的氨基酸约有22种，分非必需氨基酸和必需氨基酸（须从食物中供给）。另有酸性、碱性、中性、杂环分类，是根据其化学性质分类的。
1、必需氨基酸（essential amino acid）： 指人体（或其它脊椎动物）不能合成或合成速度远不适应机体的需要，必需由食物蛋白供给，这些氨基酸称为必需氨基酸。共有10种其作用分别是：
（一） 赖氨酸（Lysine ）：促进大脑发育，是肝及胆的组成成分，能促进脂肪代谢，调节松果腺、乳腺、黄体及卵巢，防止细胞退化；
（二） 色氨酸（Tryptophane）：促进胃液及胰液的产生；
（三） 苯丙氨酸（Phenylalanine）：参与消除肾及膀胱功能的损耗；
（四） 蛋氨酸（又叫甲硫氨酸）（Methionine）；参与组成血红蛋白、组织与血清，有促进脾脏、胰脏及淋巴的功能；
（五） 苏氨酸（Threonine）：有转变某些氨基酸达到平衡的功能；
（六） 异亮氨酸（Isoleucine ）：参与胸腺、脾脏及脑下腺的调节以及代谢；脑下腺属总司令部作用于甲状腺、性腺；
（七） 亮氨酸（Leucine ）：作用平衡异亮氨酸；
（八） 缬氨酸（Viline）：作用于黄体、乳腺及卵巢。
（九） 组氨酸（Hlstidine）：作用于代谢的调节；
（十） 精氨酸（Argnine）：促进伤口愈合，精子蛋白成分。
2、非必需氨基酸（nonessential amino acid）：指人（或其它脊椎动物）自己能由简单的前体合成，不需要从食物中获得的氨基酸。例如甘氨酸、丙氨酸等氨基酸。
各位，有没有做过附件中的比对分析，用什么软件来完成的
只有9个氨基酸，分子量1KD左右，想免疫小鼠制备单抗，有没有前辈做过这方面的东西？想了一些方法，但价值不大，请前辈们指教，不甚感激。
