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Motesanib Diphosphate (AMG 706) 是一种有效的VEGFR1/2/3的 ATP 竞争性抑制剂,IC50值为 2 nM/3 nM/6 nM,与对 Kit 的选择性相似,是 PDGFR 和 Ret 的 10 倍多。
Motesanib Diphosphate (AMG 706) 是一种有效的VEGFR1/2/3的 ATP 竞争性抑制剂,IC50值为 2 nM/3 nM/6 nM,与对 Kit 的选择性相似,是 PDGFR 和 Ret 的 10 倍多。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 377 | 现货 | |
5 mg | ¥ 913 | 现货 | |
10 mg | ¥ 1,580 | 现货 | |
25 mg | ¥ 2,680 | 现货 | |
50 mg | ¥ 3,920 | 现货 | |
100 mg | ¥ 5,680 | 现货 | |
500 mg | ¥ 11,800 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,130 | 现货 |
产品描述 | Motesanib Diphosphate (AMG 706) is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity. |
靶点活性 | c-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癌移植瘤模型中,Motesanib Diphosphate和辐射治疗联用,显示出显著地抗癌活性. |
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, AMG 706, 二磷酸莫替沙尼 |
分子量 | 569.44 |
分子式 | C22H23N5O·2H3PO4 |
CAS No. | 857876-30-3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 16 mg/mL (28.1 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 93 mg/mL (163.3 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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