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

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.

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SKLB646 Chemical Structure

SKLB646 Chemical Structure

CAS No. : 1970149-05-3

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SKLB646 Related Antibodies

Top Publications Citing Use of Products

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Lck Fyn Blk

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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BRaf c-Raf Raf

View All p38 MAPK Isoform Specific Products:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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Description

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)

Molecular Weight

533.55

Formula

C28H26F3N7O
CAS No.
SMILES

CC1=CC=C(NC(C2=CC(C(F)(F)F)=CC=C2)=O)C=C1C#CC3=NN(C4CCN(C)CC4)C5=C3C(N)=NC=N5
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SKLB646 Related Classifications

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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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