(E)-3-AP
Based on 1 Customer Validation
(E)-3-AP is the E configuration of 3-AP. 3-AP is a potent ribonucleotide reductase inhibitor. 3-AP shows anti-proliferative activity. 3-AP shows anticancer activity in L1210 leukemia model. 3-AP inhibits RR activity and DNA synthesis.
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: 99.24%
- CAS 番号: 200933-27-3
- 分子式: C7H9N5S
- 分子量:195.24
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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
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.7 μM
Compound: Triapine
|
Cytotoxicity against human A2780 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human A2780 cells incubated for 72 hrs by MTT assay
|
[PMID: 27336684] |
| A549 | IC50 |
2.288 μM
Compound: 3-AP
|
Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| BGC-823 | IC50 |
3.07 μM
Compound: 3-AP
|
Antiproliferative activity against human BGC-823 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human BGC-823 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| EC9706 | IC50 |
3.084 μM
Compound: 3-AP
|
Antiproliferative activity against human EC9706 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human EC9706 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| GES1 | IC50 |
5.4 μM
Compound: 3-AP
|
Cytotoxicity against human GES-1 cells after 72 hrs by MTT assay
Cytotoxicity against human GES-1 cells after 72 hrs by MTT assay
|
[PMID: 30108734] |
| GES1 | IC50 |
5.6 μM
Compound: 3-AP
|
Antiproliferative activity against human GES-1 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human GES-1 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay
|
[PMID: 31614257] |
| GES1 | IC50 |
6.103 μM
Compound: 3-AP
|
Cytotoxicity against human GES1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human GES1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| HCT-116 | IC50 |
1.226 μM
Compound: II
|
Dark cytotoxicity against human HCT116 cells expressing wild type p53 after 96 hrs by MTT assay
Dark cytotoxicity against human HCT116 cells expressing wild type p53 after 96 hrs by MTT assay
|
[PMID: 24900837] |
| HGC-27 | IC50 |
11.495 μM
Compound: 3-AP
|
Antiproliferative activity against human HGC-27 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HGC-27 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| HUVEC | IC50 |
3448 nM
Compound: 3-AP
|
Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay
Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay
|
[PMID: 30835473] |
| KB 3-1 | IC50 |
>800 μM
Compound: 3-AP
|
Antiproliferative activity against human KB3-1 cells after 24 hrs by MTT assay
Antiproliferative activity against human KB3-1 cells after 24 hrs by MTT assay
|
[PMID: 27524608] |
| KB 3-1 | IC50 |
>800 μM
Compound: 3-AP
|
Antiproliferative activity against human KB3-1 cells after 24 hrs in presence of P-gp inhibitor elacridar by MTT assay
Antiproliferative activity against human KB3-1 cells after 24 hrs in presence of P-gp inhibitor elacridar by MTT assay
|
[PMID: 27524608] |
| KB 3-1 | IC50 |
1.4 μM
Compound: 9
|
Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay
Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay
|
[PMID: 19397322] |
| KB 3-1 | IC50 |
3.1 μM
Compound: Triapine
|
Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay
|
[PMID: 27336684] |
| KB-V1 | IC50 |
>800 μM
Compound: 3-AP
|
Antiproliferative activity against human KBV1 cells over expressing P-gp after 24 hrs by MTT assay
Antiproliferative activity against human KBV1 cells over expressing P-gp after 24 hrs by MTT assay
|
[PMID: 27524608] |
| KB-V1 | IC50 |
>800 μM
Compound: 3-AP
|
Antiproliferative activity against human KBV1 cells over expressing P-gp after 24 hrs in presence of P-gp inhibitor elacridar by MTT assay
Antiproliferative activity against human KBV1 cells over expressing P-gp after 24 hrs in presence of P-gp inhibitor elacridar by MTT assay
|
[PMID: 27524608] |
| KB-V1 | IC50 |
5.9 μM
Compound: 9
|
Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay
Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay
|
[PMID: 19397322] |
| L1210 | IC50 |
1.3 μM
Compound: 1; 3-AP
|
Growth inhibition of mouse L1210 cells by MTS assay
Growth inhibition of mouse L1210 cells by MTS assay
|
[PMID: 30904782] |
| MCF7 | IC50 |
>32 μM
Compound: 3-AP
|
Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| MCF7 | IC50 |
18.85 μM
Compound: 3-AP
|
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
|
[PMID: 30108734] |
| MES-SA | IC50 |
1.305 μM
Compound: Triapine
|
Cytotoxicity against human MES-SA cells transfected with mCherry fluorescent protein assessed as inhibition of cell proliferation incubated for 72 hrs by fluorescent assay
Cytotoxicity against human MES-SA cells transfected with mCherry fluorescent protein assessed as inhibition of cell proliferation incubated for 72 hrs by fluorescent assay
|
[PMID: 27161177] |
| MES-SA/Dx5 | IC50 |
2.523 μM
Compound: Triapine
|
Cytotoxicity against human MES-SA/DX5 cells transfected with mCherry fluorescent protein assessed as inhibition of cell proliferation incubated for 72 hrs by fluorescent assay
Cytotoxicity against human MES-SA/DX5 cells transfected with mCherry fluorescent protein assessed as inhibition of cell proliferation incubated for 72 hrs by fluorescent assay
|
[PMID: 27161177] |
| MGC-803 | IC50 |
5.411 μM
Compound: 3-AP
|
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| MGC-803 | IC50 |
9.68 μM
Compound: 3-AP
|
Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay
Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay
|
[PMID: 30108734] |
| MV4-11 | IC50 |
967.6 nM
Compound: 3-AP
|
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay
|
[PMID: 30835473] |
| PC-3 | IC50 |
0.56 μM
Compound: 3-AP
|
Antiproliferative activity against human PC3 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay
|
[PMID: 31614257] |
| PC-3 | IC50 |
0.56 μM
Compound: 3-AP
|
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 33153765] |
| SGC-7901 | IC50 |
18.349 μM
Compound: 3-AP
|
Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| SK-N-MC | IC50 |
0.26 μM
Compound: 3-AP
|
Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay
Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay
|
[PMID: 17602603] |
| SK-N-MC | IC50 |
0.26 μM
Compound: 3-AP
|
Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay
Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay
|
[PMID: 19601577] |
| SK-N-MC | IC50 |
0.31 μM
Compound: triapine
|
Antiproliferative activity against human SK-N-MC cells by MTT assay
Antiproliferative activity against human SK-N-MC cells by MTT assay
|
[PMID: 17142046] |
| SK-N-MC | IC50 |
0.54 μM
Compound: 3-AP
|
Antiproliferative activity against human SK-N-MC cells by MTT assay
Antiproliferative activity against human SK-N-MC cells by MTT assay
|
[PMID: 17963372] |
| SMMC-7721 | IC50 |
42.81 μM
Compound: 3-AP
|
Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay
Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay
|
[PMID: 30108734] |
| SW480 | IC50 |
>50 μM
Compound: Triapine
|
Cytotoxicity against triapine-resistant human SW480 cells incubated for 72 hrs by MTT assay
Cytotoxicity against triapine-resistant human SW480 cells incubated for 72 hrs by MTT assay
|
[PMID: 27336684] |
| SW480 | IC50 |
0.84 μM
Compound: Triapine
|
Cytotoxicity against human SW480 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human SW480 cells incubated for 72 hrs by MTT assay
|
[PMID: 27336684] |
| WI-38 | IC50 |
>25 μM
Compound: Triapine
|
Cytotoxicity against human WI38 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human WI38 cells incubated for 72 hrs by MTT assay
|
[PMID: 27336684] |
3-AP shows anti-proliferative activity with IC50 values of 1.3, 1.6 µM for L1210, L1210/HUr cells, respectively[1].
3-AP (5, 10, 15, 20, 30 mg/kg; i.p.; twice daily for six consecutive days) significantly increases in life span were observed with each dosage employed and long term survivors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 200933-27-3
-
性状 Solid
-
分子量 195.24
-
分子式 C7H9N5S
-
Color Light yellow to yellow
-
SMILES
NC1=CC=CN=C1/C=N/NC(N)=S.[(E)]
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別名
(E)-PAN-811; (E)-NSC# 663249; (E)-OCX191
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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
純度とドキュメンテーション
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データシート (268 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Finch RA, et al. Triapine (3-aminopyridine-2-carboxaldehyde thiosemicarbazone; 3-AP): an inhibitor of ribonucleotide reductase with antineoplastic activity. Adv Enzyme Regul. 1999;39:3-12. [Content Brief]
[2]. Enyedy ÉA ,et al. Complex formation and cytotoxicity of Triapine derivatives: a comparative solution study on the effect of the chalcogen atom and NH-methylation. Dalton Trans. 2020 Dec 8;49(46):16887-16902. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)