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SKLB1002 是一种有效的 ATP 竞争性 VEGFR2 抑制剂,IC50 为 32 nM。
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SKLB1002 是一种有效的 ATP 竞争性 VEGFR2 抑制剂,IC50 为 32 nM。
规格 | 价格 | 库存 | 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 |
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 |
Smiles | COc1cc2ncnc(Sc3nnc(C)s3)c2cc1OC |
密度 | 1.45 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | DMSO: 1 mg/ml, Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) |
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