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SKLB646 是一种口服多靶点激酶抑制剂,其抑制效果针对多种激酶。在对SRC和VEGFR2的抑制上,SKLB646表现出强效性,其IC50分别为0.002 μmol/L和0.012 μmol/L。此外,该化合物对B-Raf 和 C-Raf的抑制IC50分别为0.022 μmol/L和0.019 μmol/L。SKLB646能有效抑制SRC信号通路的激活,并阻断MAPK信号通路,通过抑制Raf激酶达到这种效果。SKLB646亦可阻止人脐静脉内皮细胞(HUVEC)的增殖、迁移和侵袭,并抑制肿瘤诱导的心血管生成。对于三阴性乳腺癌(TNBC)细胞系,SKLB646显示了显著的抗增殖和抗生存活性。
SKLB646 是一种口服多靶点激酶抑制剂,其抑制效果针对多种激酶。在对SRC和VEGFR2的抑制上,SKLB646表现出强效性,其IC50分别为0.002 μmol/L和0.012 μmol/L。此外,该化合物对B-Raf 和 C-Raf的抑制IC50分别为0.022 μmol/L和0.019 μmol/L。SKLB646能有效抑制SRC信号通路的激活,并阻断MAPK信号通路,通过抑制Raf激酶达到这种效果。SKLB646亦可阻止人脐静脉内皮细胞(HUVEC)的增殖、迁移和侵袭,并抑制肿瘤诱导的心血管生成。对于三阴性乳腺癌(TNBC)细胞系,SKLB646显示了显著的抗增殖和抗生存活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 10-14周 | |
50 mg | 询价 | 10-14周 |
产品描述 | SKLB646 is an orally active multitarget kinase inhibitor that exhibits potent suppression of several kinases. It demonstrates significant inhibitory effects on SRC and VEGFR2, with IC50 values of 0.002 μmol/L and 0.012 μmol/L, respectively. Additionally, SKLB646 shows notable inhibition of B-Raf and C-Raf, with IC50 values of 0.022 μmol/L and 0.019 μmol/L, respectively. The compound inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinases. Furthermore, SKLB646 inhibits the proliferation, migration, and invasion of human umbilical vein endothelial cells (HUVEC), thereby suppressing tumor-induced angiogenesis. SKLB646 also displays significant anti-proliferative and anti-survival effects on triple-negative breast cancer (TNBC) cell lines. |
靶点活性 | VEGFR2:0.012 μM, B-Raf:0.022 μM, c-Raf:0.019 μM |
分子量 | 533.55 |
分子式 | C28H26F3N7O |
CAS No. | 1970149-05-3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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