Anticancer agent 43
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Anticancer Agent 43 is a potent anticancer agent. Anticancer Agent 43 induces apoptosis by caspase 3, PARP1, and Bax dependent mechanisms. Anticancer Agent 43 induces DNA damage.
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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: 98.58%
- CAS 番号: 2470015-35-9
- 分子式: C14H9FN2O3S2
- 分子量:336.36
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
|
Caspase 3 |
PARP1 |
Bax |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
9.7 μM
Compound: 3a
|
Cytotoxicity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34634616] |
| BALB/3T3 | GI50 |
>100 μM
Compound: 3a
|
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 24 hrs by coomassie brilliant blue staining based total cellular protein assay
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 24 hrs by coomassie brilliant blue staining based total cellular protein assay
|
[PMID: 34634616] |
| BALB/3T3 | GI50 |
>100 μM
Compound: 3a
|
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 24 hrs by LDH assay
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 24 hrs by LDH assay
|
[PMID: 34634616] |
| BALB/3T3 | GI50 |
>100 μM
Compound: 3a
|
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 24 hrs by neutral red uptake assay
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 24 hrs by neutral red uptake assay
|
[PMID: 34634616] |
| BALB/3T3 | GI50 |
>100 μM
Compound: 3a
|
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 48 hrs by coomassie brilliant blue staining based total cellular protein assay
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 48 hrs by coomassie brilliant blue staining based total cellular protein assay
|
[PMID: 34634616] |
| BALB/3T3 | GI50 |
>100 μM
Compound: 3a
|
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 48 hrs by neutral red uptake assay
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 48 hrs by neutral red uptake assay
|
[PMID: 34634616] |
| BALB/3T3 | GI50 |
25 μM
Compound: 3a
|
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
|
[PMID: 34634616] |
| BALB/3T3 | GI50 |
40.8 μM
Compound: 3a
|
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34634616] |
| BALB/3T3 | GI50 |
48.3 μM
Compound: 3a
|
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 72 hrs by coomassie brilliant blue staining based total cellular protein assay
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 72 hrs by coomassie brilliant blue staining based total cellular protein assay
|
[PMID: 34634616] |
| BALB/3T3 | GI50 |
51.5 μM
Compound: 3a
|
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 72 hrs by neutral red uptake assay
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 72 hrs by neutral red uptake assay
|
[PMID: 34634616] |
| BALB/3T3 | GI50 |
54.3 μM
Compound: 3a
|
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
|
[PMID: 34634616] |
| BALB/3T3 | GI50 |
62.8 μM
Compound: 3a
|
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 72 hrs by LDH assay
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 72 hrs by LDH assay
|
[PMID: 34634616] |
| BALB/3T3 | GI50 |
89.7 μM
Compound: 3a
|
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 48 hrs by LDH assay
Cytotoxicity against mouse BALB/3T3 cells assessed as cell growth inhibition measured after 48 hrs by LDH assay
|
[PMID: 34634616] |
| HaCaT | GI50 |
98.3 μM
Compound: 3a
|
Cytotoxicity against human HaCaT cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human HaCaT cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34634616] |
| HCT-116 | GI50 |
0.8 μM
Compound: 3a
|
Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34634616] |
| HeLa | GI50 |
49.3 μM
Compound: 3a
|
Cytotoxicity against human HeLa cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34634616] |
| HepG2 | GI50 |
>100 μM
Compound: 3a
|
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 24 hrs by coomassie brilliant blue staining based total cellular protein assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 24 hrs by coomassie brilliant blue staining based total cellular protein assay
|
[PMID: 34634616] |
| HepG2 | GI50 |
0.04 μM
Compound: 3a
|
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by LDH assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by LDH assay
|
[PMID: 34634616] |
| HepG2 | GI50 |
0.06 μM
Compound: 3a
|
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by LDH assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by LDH assay
|
[PMID: 34634616] |
| HepG2 | GI50 |
0.31 μM
Compound: 3a
|
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 24 hrs by LDH assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 24 hrs by LDH assay
|
[PMID: 34634616] |
| HepG2 | GI50 |
12.1 μM
Compound: 3a
|
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34634616] |
| HepG2 | GI50 |
16.3 μM
Compound: 3a
|
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
|
[PMID: 34634616] |
| HepG2 | GI50 |
24.5 μM
Compound: 3a
|
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by neutral red uptake assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by neutral red uptake assay
|
[PMID: 34634616] |
| HepG2 | GI50 |
35.6 μM
Compound: 3a
|
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by coomassie brilliant blue staining based total cellular protein assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by coomassie brilliant blue staining based total cellular protein assay
|
[PMID: 34634616] |
| HepG2 | GI50 |
40.1 μM
Compound: 3a
|
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 24 hrs by neutral red uptake assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 24 hrs by neutral red uptake assay
|
[PMID: 34634616] |
| HepG2 | GI50 |
44.7 μM
Compound: 3a
|
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
|
[PMID: 34634616] |
| HepG2 | GI50 |
63.9 μM
Compound: 3a
|
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by coomassie brilliant blue staining based total cellular protein assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by coomassie brilliant blue staining based total cellular protein assay
|
[PMID: 34634616] |
| HepG2 | GI50 |
7.5 μM
Compound: 3a
|
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by neutral red uptake assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by neutral red uptake assay
|
[PMID: 34634616] |
| MCF7 | GI50 |
0.7 μM
Compound: 3a
|
Cytotoxicity against human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34634616] |
| THP-1 | GI50 |
62.4 μM
Compound: 3a
|
Cytotoxicity against human THP-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human THP-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34634616] |
| WM793 | GI50 |
80.4 μM
Compound: 3a
|
Cytotoxicity against human WM793 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human WM793 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34634616] |
Anticancer agent 43 (compound 3a) shows selectivity toward human tumor cells (SI50=28.94)[1].
Anticancer agent 43 (45 µM, 24 h) induces apoptosis via caspase 3, PARP1 and Bax dependent pathways in HepG2 cells[1].
Anticancer agent 43 (45 µM, 24 h) shows no effect on the transition of G1/S phases in HepG2 cells[1].
Anticancer agent 43 (0.7, 45, 55 µM) induces DNA damage in HCT116 cells (Tail DNA=16.1%, OTM=3.7), MCF-7 cells, HepG2 cells (Tail DNA=26.2%, OTM=13.2), Balb/c 3T3 cells (Tail DNA = 8.4%, OTM = 3.5)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2, MCF-7, HCT116, HeLa, A549, WM793, THP-1, HaCaT, Balb/c3T3 cells
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Concentration:0, 1, 10, 100 µM
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Incubation Time:72 h
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Result:Showed cytotoxic action with GI50s of 12.1, 0.7, 0.8, 49.3, 9.7 µM for for HepG2, MCF-7, HCT116, HeLa, A549 cells, low toxicity towards WM793, THP-1, HaCaT, Balb/c 3T3 cells with GI50s of 80.4, 62.4,98.3,40.8 µM , respectively.
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Cell Line:HepG2 cells
-
Concentration:45 µM
-
Incubation Time:24 h
-
Result:Induced apoptosis in HepG2 cells via caspase 3, PARP1 and Bax dependent pathways.
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Cell Line:HCT116, MCF-7 cells
-
Concentration:0.7 µM
-
Incubation Time:24 h
-
Result:Decreased the expression of Cdk2 protein in HCT116 and MCF-7 cells.
-
Cell Line:HepG2 cells
-
Concentration:45 µM
-
Incubation Time:24 h
-
Result:Showed no effect on the transition of G1/S phases in HepG2 cells.
化学情報
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CAS 番号 2470015-35-9
-
性状 Solid
-
分子量 336.36
-
分子式 C14H9FN2O3S2
-
Color Light yellow to yellow
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SMILES
COC(C1=C(C2=C(N1)C=CC(F)=C2)/C=C3SC(NC\3=O)=S)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 125 mg/mL (371.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (282 KB)
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SDS (251 KB)
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- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9730 mL | 14.8650 mL | 29.7301 mL | 74.3251 mL |
| 5 mM | 0.5946 mL | 2.9730 mL | 5.9460 mL | 14.8650 mL | |
| 10 mM | 0.2973 mL | 1.4865 mL | 2.9730 mL | 7.4325 mL | |
| 15 mM | 0.1982 mL | 0.9910 mL | 1.9820 mL | 4.9550 mL | |
| 20 mM | 0.1487 mL | 0.7433 mL | 1.4865 mL | 3.7163 mL | |
| 25 mM | 0.1189 mL | 0.5946 mL | 1.1892 mL | 2.9730 mL | |
| 30 mM | 0.0991 mL | 0.4955 mL | 0.9910 mL | 2.4775 mL | |
| 40 mM | 0.0743 mL | 0.3716 mL | 0.7433 mL | 1.8581 mL | |
| 50 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL | 1.4865 mL | |
| 60 mM | 0.0496 mL | 0.2478 mL | 0.4955 mL | 1.2388 mL | |
| 80 mM | 0.0372 mL | 0.1858 mL | 0.3716 mL | 0.9291 mL | |
| 100 mM | 0.0297 mL | 0.1487 mL | 0.2973 mL | 0.7433 mL |