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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- No. CAS: 1970149-05-3
- Fòrmula: C28H26F3N7O
- Peso molecular:533.55
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
VEGFR2 0.012 μM (IC50) |
B-Raf 0.022 μM (IC50) |
C-Raf 0.019 μM (IC50) |
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
>10 μM
Compound: 13b
|
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 27739679] |
| MDA-MB-231 | IC50 |
0.013 μM
Compound: 13b
|
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 27739679] |
| MDA-MB-231 | IC50 |
0.013 μM
Compound: 92; SKLB646
|
Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
|
[PMID: 33650861] |
| MDA-MB-435 | IC50 |
0.08 μM
Compound: 13b
|
Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 27739679] |
| MDA-MB-435 | IC50 |
0.08 μM
Compound: 92; SKLB646
|
Anticancer activity against human MDA-MB-435 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Anticancer activity against human MDA-MB-435 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
|
[PMID: 33650861] |
Chemical Information
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No. CAS 1970149-05-3
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Peso molecular 533.55
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Fòrmula C28H26F3N7O
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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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)