ON044580
Based on 1 Customer Validation
ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling.
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。
- 純度: 99.11%
- CAS 番号: 1035199-04-2
- 分子式: C23H15BrFNO5S
- 分子量:516.34
-
保管条件:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
生物活性
|
JAK2-WT 1.23 μM (IC50) |
JAK2-V617F 1.09 μM (IC50) |
WT BCR-ABL |
T315I-BCR-ABL |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | GI50 |
1 μM
Compound: 6c
|
Growth inhibition of human DU145 cells after 96 hrs by trypan blue exclusion assay
Growth inhibition of human DU145 cells after 96 hrs by trypan blue exclusion assay
|
[PMID: 20188579] |
| K562 | GI50 |
<1 μM
Compound: 6c
|
Growth inhibition of human K562 cells expressing p210Bcr/Abl after 96 hrs by trypan blue exclusion assay
Growth inhibition of human K562 cells expressing p210Bcr/Abl after 96 hrs by trypan blue exclusion assay
|
[PMID: 20188579] |
| K562 | IC50 |
0.3 μM
Compound: 6c
|
Growth inhibition of human K562 cells expressing p210Bcr/Abl after 96 hrs by trypan blue exclusion assay
Growth inhibition of human K562 cells expressing p210Bcr/Abl after 96 hrs by trypan blue exclusion assay
|
[PMID: 20188579] |
| K562 | IC50 |
0.5 μM
Compound: 6c
|
Inhibition of BCR/ABL p210 autophosphorylation in human K562 cells after 2 hrs by Western blot analysis
Inhibition of BCR/ABL p210 autophosphorylation in human K562 cells after 2 hrs by Western blot analysis
|
[PMID: 20188579] |
化学情報
-
CAS 番号 1035199-04-2
-
性状 Solid
-
分子量 516.34
-
分子式 C23H15BrFNO5S
-
Color Off-white to light yellow
-
SMILES
O=C(C1=CC=C(C(O)=O)C=C1)/C(SCC2=CC=C(Br)C=C2)=C\C3=CC=C(F)C([N+]([O-])=O)=C3
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
純度とドキュメンテーション
-
データシート (270 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)