2. Protein Tyrosine Kinase/RTK MAPK/ERK Pathway
  3. Src VEGFR Raf p38 MAPK
  4. SKLB646

SKLB646 是一种具有口服活性的多靶点激酶抑制剂。SKLB646 对 SRC 和 VEGFR2 的抑制作用显著，IC50 值分别为 0.002 μmol/L 和 0.012 μmol/L。同时，SKLB646 对 B-Raf 和 C-Raf 的抑制作用也相当显著，IC50 值分别为 0.022 μmol/L 和 0.019 μmol/L。SKLB646 抑制了 SRC 信号通路的激活，并通过抑制 Raf 激酶阻断了 MAPK 信号通路。此外，SKLB646 还可以抑制人脐静脉内皮细胞 (HUVEC) 的增殖、迁移和侵袭，来抑制肿瘤诱导的心血管的生成。SKLB646 对三阴性乳腺癌 (TNBC) 细胞系表现出显著的抗增殖和抗生存活性。

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SKLB646 Chemical Structure

SKLB646 Chemical Structure

CAS No. : 1970149-05-3

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SKLB646 相关抗体

Top Publications Citing Use of Products

查看 Src 亚型特异性产品:

查看所有亚型
Lck Fyn Blk

查看 VEGFR 亚型特异性产品:

查看所有亚型
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

查看 Raf 亚型特异性产品:

查看所有亚型
BRaf c-Raf Raf

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC50 values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC50 values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines[1].

IC50 & Target[1]

VEGFR2

0.012 μM (IC50)

B-Raf

0.022 μM (IC50)

c-Raf

0.019 μM (IC50)

分子量

533.55

Formula

C28H26F3N7O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SKLB646 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SKLB6461970149-05-3SKLB 646SKLB-646SrcVEGFRRafp38 MAPKVascular endothelial growth factor receptorRaf kinasesHUVECanti-proliferationanti-angiogenesistriple-negative breast cancerinhibitorInhibitorinhibit

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