Antitumor agent-83
Antitumor agent-83 is an activator of pro-apoptotic protein BAX and has significant anti-proliferation effect on tumor cells. Antiumor agent-83 mediates cell Apoptosis by inducing the conformational activation of BAX and has inhibitory effect on A549 cell cycle. Antiumor agent-83 has good metabolic stability and CYPs spectrum in vitro.
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: 3038789-74-8
- 分子式: C29H30N6O2
- 分子量:494.59
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
2.15 μM
Compound: 6d
|
Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
|
[PMID: 36680883] |
| HCT-116 | GI50 |
3.31 μM
Compound: 6d
|
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
|
[PMID: 36680883] |
| K562 | GI50 |
1.41 μM
Compound: 6d
|
Antiproliferative activity against human K562 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis
Antiproliferative activity against human K562 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis
|
[PMID: 36680883] |
| MDA-MB-231 | GI50 |
3.98 μM
Compound: 6d
|
Antiproliferative activity against human MDA-MB-231 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by MTT assay
|
[PMID: 36680883] |
| MV4-11 | GI50 |
2.84 μM
Compound: 6d
|
Antiproliferative activity against human MV4-11 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis
Antiproliferative activity against human MV4-11 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis
|
[PMID: 36680883] |
| NCI-H1581 | GI50 |
2.15 μM
Compound: 6d
|
Antiproliferative activity against human NCI-H1581 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1581 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by MTT assay
|
[PMID: 36680883] |
| PC-3 | GI50 |
2.5 μM
Compound: 6d
|
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
|
[PMID: 36680883] |
| THP-1 | GI50 |
2.18 μM
Compound: 6d
|
Antiproliferative activity against human THP-1 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis
Antiproliferative activity against human THP-1 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis
|
[PMID: 36680883] |
Antitumor agent-83 (compound 6d) (5-40 µM; 24 h) activates BAX and mediates cell apoptosis, promotes the release cytochrome c in a dose-dependent manner[1].
Antitumor agent-83 has significant anti-proliferation effect on A549, HCT-116, PC-3, H1581, MDA-MB-231, K562, MV4-11 and THP-1 tumor cells with GI50 values of 2.15 µM, 3.31 µM, 2.50 µM, 2.15 µM, 3.98 µM, 1.41 µM, 2.84 µM, 2.18 µM, respectively[1].
Antitumor agent-83 (1-5 µM; 24, 48 and 72h) significantly reduces the viability of A549 cells in a dose-and time-dependent manner[1].
Antitumor agent-83 (5 µM and 10 µM; 48 h) promotes A549 cells apoptosis in a dose-dependent manner[1].
Antitumor agent-83 (2.5 µM and 5 µM; 48 h) induces cell cycle arrest in G0/G1 phase with dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:A549 cells.
-
Concentration:5, 10, 20 and 40 µM.
-
Incubation Time:24 h.
-
Result:Significantly up-regulated the expression level of BAX, activated the conformation of BAX and caused the release of cytochrome c.
-
Cell Line:A549 cells.
-
Concentration:1, 2, 3, 4 and 5 µM.
-
Incubation Time:24, 48 and 72h.
-
Result:Showed inhibitory effect on the growth of A549 cells and exhibited greatest impact on the viability of A549 cells (5 µM; 72 h).
-
Cell Line:A549 cells.
-
Concentration:5 and 10 µM.
-
Incubation Time:48 h.
-
Result:Showed active effect on the apoptosis of A549 cells with cell apoptosis were 15.43 % and 73.40 % at the concentration of 5 µM and 10 µM, respectively.
-
Cell Line:A549 cells.
-
Concentration:2.5 and 5 µM.
-
Incubation Time:48 h.
-
Result:Exhibited inhibitory effect on A549 cell cycle.
化学情報
-
CAS 番号 3038789-74-8
-
分子量 494.59
-
分子式 C29H30N6O2
-
SMILES
CN(C1CCN(CC1)C(C2=CC=C(C=C2)N3N=C(/C(C3=O)=N/NC4=CC=CC=C4)C5=CC=CC=C5)=O)C
-
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)
Antitumor agent-83 関連分類
HY-152468 関連分類
Powered by Bioz