Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SKLB1002 是一种有效的 ATP 竞争性 VEGFR2 抑制剂,IC50 为 32 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 212 | 现货 | ||
2 mg | ¥ 293 | 现货 | ||
5 mg | ¥ 669 | 现货 | ||
10 mg | ¥ 920 | 现货 | ||
25 mg | ¥ 1,930 | 现货 | ||
50 mg | ¥ 2,880 | 现货 | ||
100 mg | ¥ 4,270 | 现货 | ||
500 mg | ¥ 9,230 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 693 | 现货 |
产品描述 | SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM. |
靶点活性 | VEGFR2:32 nM |
体外活性 | 在4T1和CT26肿瘤模型中,SKLB1002和局部热疗产生协同抗血管生成,抗癌和促进细胞凋亡功效.在携带SW620或HepG2异种移植物的无胸腺小鼠中,SKLB1002(100 mg/kg每天,i.p.)引起显著的肿瘤生长抑制,抑制肿瘤血管生成并诱导肿瘤细胞凋亡.SKLB1002在斑马鱼胚胎中,明显阻断胚胎形成和肿瘤诱导的血管生成,对正常细胞增殖没有影响或影响很小. |
体内活性 | SKLB1002通过抑制VEGF诱导的VEGFR2激酶磷酸化和下游蛋白激酶,包括ERK,FAK和Src,明显抑制人脐静脉内皮细胞增殖,迁移,侵袭和管腔形成。SKLB1002对正常人细胞L-02细胞毒性显著降低。 |
激酶实验 | Kinase inhibition assays : Kinase inhibition is measured by the use of radiometric assays conducted by Kinase Profiler service. Briefly, in the presence or absence of SKLB1002, VGFR2 (5–10 mU) is incubated in 25-μL reaction solution containing 8 mmol/L 3-(N-morpholino)propanesulfonic acid (MOPS), pH 7.0, 0.2 mmol/L EDTA, 0.33 mg/mL myelin basic protein, 10 mmol/L Mg acetate, and γ-[33P]ATP. After incubation for 40 minutes at room temperature, the reaction is stopped and 10 μL of the reaction solution is then spotted onto a P30 filtermat and washed 3 times for 5 minutes in 75 mmol/L phosphoric acid and once in methanol prior to scintillation counting. |
细胞实验 | Cell proliferation is measured using MTT assay. Various cells including HUVECs, L-02, B16-F10, HepG2, and SW620 are treated with indicated concentrations of SKLB1002 for 24 hours. Vandetanib and sunitinib serve as positive controls. Each assay is replicated 3 times.(Only for Reference) |
分子量 | 320.39 |
分子式 | C13H12N4O2S2 |
CAS No. | 1225451-84-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 7 mg/mL (21.84 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.1212 mL | 15.606 mL | 31.212 mL | 78.0299 mL |
5 mM | 0.6242 mL | 3.1212 mL | 6.2424 mL | 15.606 mL | |
10 mM | 0.3121 mL | 1.5606 mL | 3.1212 mL | 7.803 mL | |
20 mM | 0.1561 mL | 0.7803 mL | 1.5606 mL | 3.9015 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。
SKLB1002 1225451-84-2 Angiogenesis Tyrosine Kinase/Adaptors VEGFR SKLB-1002 SKLB 1002 Inhibitor inhibitor inhibit