Motesanib Diphosphate
作者：齐岳
发布时间：2023-08-23
09:38:00
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产品名称：Motesanib Diphosphate
产品描述：
| 产品描述 | Motesanib Diphosphate is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity. |
| 靶点活性 | Kit:8 nM, VEGFR2/Flk1:6 nM, VEGFR1:2 nM, VEGFR3:6 nM, VEGFR2:3 nM |
| 体外活性 | 在大鼠角膜模型中,每天口服两次（ED50=2.1 mg/kg ）或一次（ED50=4.9 mg/kg ）Motesanib Diphosphate能够抑制血管内皮生长因子诱导的血管生成.在头部和颈部鳞状细胞*移植瘤模型中,Motesanib Diphosphate和辐射**联用,显示出显著地抗*活性. |
| 体内活性 | 在VEGF诱导的HUVECs细胞中（IC50 =10 nM）,Motesanib Diphosphate 明显抑制细胞增殖。对于血小板衍生因子诱导的增殖（IC50=207 nM）和SCF诱导的c-kit磷酸化（IC50=37 nM）,Motesanib Diphosphate能够显著抑制。人脐静脉内皮细胞,Motesanib Diphosphate增强细胞对于放射性的敏感程度。对人VEGFR家族,Motesanib Diphosphate具有广谱活性。 |
| 激酶实验 | In vitro kinase assays: Optimal enzyme, ATP, and substrate (gastrin peptide) concentrations are established for each enzyme using homogeneous time-resolved fluorescence (HTRF) assays. Motesanib Diphosphate 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. |
| 细胞实验 | Cells are preincubated for 2 hours with different concentrations of Motesanib Diphosphate, 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(Only for Reference) |
| 别名 | Motesanib, 二磷酸莫替沙尼, AMG 706 |
| 分子量 | 569.448 |
| 分子式 | C22H29N5O9P2 |
| CAS No. | 857876-30-3 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: 16 mg/mL (28.1 mM)
Ethanol: <1 mg/mL
DMSO: 93 mg/mL (163.3 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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