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
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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
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生物活性
|
VEGFR2 0.012 μM (IC50) |
B-Raf 0.022 μM (IC50) |
C-Raf 0.019 μM (IC50) |
|
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
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CAS 番号 1970149-05-3
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分子量 533.55
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分子式 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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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.
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)