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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1970149-05-3
- 分子式: C28H26F3N7O
- 分子量:533.55
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
VEGFR アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
[1]|
VEGFR2 0.012 μM (IC50) |
B-Raf 0.022 μM (IC50) |
C-Raf 0.019 μM (IC50) |
Cellular Effect
|
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] |
化学情報
-
CAS 番号 1970149-05-3
-
分子量 533.55
-
分子式 C28H26F3N7O
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
-
Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
-
Endothelial Tube Formation Assay
Endothelial tube formation assay evaluates the ability of endothelial cells to attach, migrate, align, and organize into capillary-like networks when cultured on gelled basement membrane extract or Matrigel; the readout is the morphology and quantity of tube-like networks, which reflects an in vitro endothelial morphogenesis step related to angiogenesis. Basement membrane extract/Matrigel provides laminin-rich extracellular matrix cues that support endothelial differentiation into capillary-like structures, but it can contain biologically active growth factors, so growth-factor-reduced matrix is preferred when testing defined angiogenic stimulators or inhibitors.
-
Cell invasion
Cell invasion is the ability of cells to migrate from one area to another via the extracellular matrix. Cell invasion is the response of normal and cancer cells to chemical and mechanical stimuli. Before migrating to a new region, the extracellular matrix is degraded by proteases within the cell. Cell invasion often occurs during wound repair, vascularization and inflammation, abnormal tissue invasion, and tumor cell metastasis.
-
Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
-
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)