Motesanib Diphosphate
作者：齊岳
發布時間：2023-08-23
09:38:00
點擊數：
產品名稱：Motesanib Diphosphate
產品描述：
| 產品描述 | Motesanib Diphosphate is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity. |
| 靶點活性 | Kit:8 nM, VEGFR2/Flk1:6 nM, VEGFR1:2 nM, VEGFR3:6 nM, VEGFR2:3 nM |
| 體外活性 | 在大鼠角膜模型中,每天口服兩次（ED50=2.1 mg/kg ）或一次（ED50=4.9 mg/kg ）Motesanib Diphosphate能夠抑制血管內皮生長因子誘導的血管生成.在頭部和頸部鱗狀細胞癌移植瘤模型中,Motesanib Diphosphate和輻射治療聯用,顯示出顯著地抗癌活性. |
| 體內活性 | 在VEGF誘導的HUVECs細胞中（IC50 =10 nM）,Motesanib Diphosphate 明顯抑制細胞增殖。對于血小板衍生因子誘導的增殖（IC50=207 nM）和SCF誘導的c-kit磷酸化（IC50=37 nM）,Motesanib Diphosphate能夠顯著抑制。人臍靜脈內皮細胞,Motesanib Diphosphate增強細胞對于放射性的敏感程度。對人VEGFR家族,Motesanib Diphosphate具有廣譜活性。 |
| 激酶實驗 | 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. |
| 細胞實驗 | 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) |
| 別名 | Motesanib, 二磷酸莫替沙尼, AMG 706 |
| 分子量 | 569.448 |
| 分子式 | C22H29N5O9P2 |
| CAS No. | 857876-30-3 |
存儲
| 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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