Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ODM-203 是 FGFR 和 VEGFR 家族的抑制剂,具有显著的抗肿瘤活性,能够诱导抗肿瘤免疫。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 245 | 现货 | ||
2 mg | ¥ 359 | 现货 | ||
5 mg | ¥ 618 | 现货 | ||
10 mg | ¥ 997 | 现货 | ||
25 mg | ¥ 2,150 | 现货 | ||
50 mg | ¥ 3,720 | 现货 | ||
100 mg | ¥ 5,350 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 483 | 现货 |
产品描述 | ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity |
靶点活性 | VEGFR2:9nM , VEGFR3:5 nM, VEGFR1:26nM, FGFR2:16nM, FGFR1:1nM, FGFR3:6nM, FGFR4:35 nM |
体外活性 | ODM-203 inhibits FGFR and VEGFR family kinases selectively and with equal potency in the low nanomolar range (IC50 6-35 nmol/L) in biochemical assays.?In cellular assays, ODM-203 inhibits VEGFR-induced tube formation (IC50 33 nmol/L) with similar potency as it inhibits proliferation in FGFR-dependent cell lines (IC50 50-150 nmol/L). |
体内活性 | In vivo, ODM-203 shows strong antitumor activity in both FGFR-dependent xenograft models and in an angiogenic xenograft model at similar well-tolerated doses. |
细胞实验 | Inhibition of FRS2 Tyrosine 196 phosphorylation by ODM-203 in FGFR-dependent cell lines was measured using an MSD 96-well multiarray Phospho-FRS2 Tyr196 assay (MesoScale Diagnostics) .?Briefly, the cell lines were seeded at a density of 75,000 cells/well on poly-d-lysine-coated 96-well plates?in the cell culture media .?The cells were allowed to attach overnight and subsequently treated with the vehicle (0.5% DMSO) or increasing concentrations of ODM-203 for 20 minutes.?The cell culture media were aspirated and the cells lysed in MSD Tris Lysis Buffer?supplemented with 10 mmol/L NaF, 1× phosphatase inhibitor cocktail 2 and 3 and Complete Protease Inhibitor Cocktail .?The electrochemiluminescence signal was detected with a SECTOR Imager 2400 plate reader coupled to a CCD camera.?Data were expressed as percentages of vehicle control values and analyzed with GrapPadPrism 7.03 .?Each test concentration was studied at least in triplicate and inhibition percentages were calculated for the parallel samples.?Average IC50 values were calculated from two independent experiments. |
动物实验 | Athymic Nude-Foxn1nu female mice (9 weeks old;?Harlan, the Netherlands) were subcutaneously injected with 1 million H1581, KMS11, RT4, or SNU16 cells in 100 μL of McCoy's 5a modified medium and Matrigel (BD) (1:1).?Tumor growth was monitored twice weekly by caliper measurements.?Oral treatment with ODM-203 and AZD-4547 was started when the average tumor volume reached 100 mm^3 and continued for 21 days for the RT4 xenograft model (n = 12/group) and 12 days for the SNU16 xenograft model (n = 6/group).?Necropsy, and plasma and tumor sampling were carried out 4 hours after the last dosing.Doses for 12.5 mg/kg AZD4547 and 40 mg/kg sorafenib were chosen based on published data.?Oral treatment (ODM-203 or AZD4547) was initiated when the average tumor volume reached ≈125 mm^3.?Mean tumor volumes were calculated for each treatment group. |
分子量 | 505.54 |
分子式 | C26H21F2N5O2S |
CAS No. | 1430723-35-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 13 mg/mL (25.72 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9781 mL | 9.8904 mL | 19.7808 mL | 49.4521 mL |
5 mM | 0.3956 mL | 1.9781 mL | 3.9562 mL | 9.8904 mL | |
10 mM | 0.1978 mL | 0.989 mL | 1.9781 mL | 4.9452 mL | |
20 mM | 0.0989 mL | 0.4945 mL | 0.989 mL | 2.4726 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
ODM-203 1430723-35-5 Angiogenesis Tyrosine Kinase/Adaptors VEGFR FGFR anti-tumor immunity ODM203 ODM 203 HUVEC H1581 Inhibitor cancer Vascular endothelial growth factor receptor SNU16 RT4 Fibroblast growth factor receptor inhibit inhibitor