5F-203
Based on 1 Customer Validation
5F-203 (NSC-703786) is a cytotoxic molecule that forms DNA adducts and cell cycle arrest. 5F-203 induces aryl hydrocarbon receptor (AhR) signaling and elevates expression of CYP1A1. 5F-203 also increases the levels of reactive oxygen species as well as activates JNK, ERK, and p38.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.04%
- CAS No.: 260443-89-8
- 화학식: C14H11FN2S
- 분자량:258.31
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Cancer cell lines | GI50 |
<0.01 μM
Compound: 10h
|
Growth inhibition against cancer cell line TH-10
Growth inhibition against cancer cell line TH-10
|
[PMID: 11311068] |
| HCC 2998 | GI50 |
>100 μM
Compound: 2
|
Antiproliferative activity against human colon cancer cell line HCC2998
Antiproliferative activity against human colon cancer cell line HCC2998
|
[PMID: 16392802] |
| HCC 2998 | GI50 |
<0.01 μM
Compound: 130
|
Cytotoxicity against human HCC 2998 cells
Cytotoxicity against human HCC 2998 cells
|
[PMID: 31926469] |
| HCT-116 | GI50 |
16 μM
Compound: 4a
|
Antiproliferative activity against human HCT116 cell line
Antiproliferative activity against human HCT116 cell line
|
[PMID: 16789754] |
| HT-29 | GI50 |
63 μM
Compound: 4a
|
Antiproliferative activity against human HT29 cell line
Antiproliferative activity against human HT29 cell line
|
[PMID: 16789754] |
| IGROV-1 | GI50 |
<0.01 μM
Compound: 10h
|
Growth inhibition against ovarian cancer cell line IGROV1
Growth inhibition against ovarian cancer cell line IGROV1
|
[PMID: 11311068] |
| IGROV-1 | GI50 |
<0.01 μM
Compound: 130
|
Cytotoxicity against human IGROV-1 cells
Cytotoxicity against human IGROV-1 cells
|
[PMID: 31926469] |
| KM12 | GI50 |
>100 μM
Compound: 2
|
Antiproliferative activity against human colon cancer cell line KM12
Antiproliferative activity against human colon cancer cell line KM12
|
[PMID: 16392802] |
| MCF7 | GI50 |
<0.01 μM
Compound: 10h
|
Growth inhibition against breast cancer line MCF-7
Growth inhibition against breast cancer line MCF-7
|
[PMID: 11311068] |
| MCF7 | GI50 |
<0.0001 μM
Compound: 2
|
Antiproliferative activity against human breast cancer cell line MCF7
Antiproliferative activity against human breast cancer cell line MCF7
|
[PMID: 16392802] |
| MCF7 | GI50 |
<0.1 nM
Compound: 2
|
Antiproliferative activity against human breast cancer cell line MCF7
Antiproliferative activity against human breast cancer cell line MCF7
|
[PMID: 16392802] |
| MCF7 | GI50 |
<0.0001 μM
Compound: 4a
|
Antiproliferative activity against human MCF7 cell line
Antiproliferative activity against human MCF7 cell line
|
[PMID: 16789754] |
| MCF7 | GI50 |
<0.1 nM
Compound: 4a
|
Antiproliferative activity against human MCF7 cell line
Antiproliferative activity against human MCF7 cell line
|
[PMID: 16789754] |
| MCF7 | IC50 |
0.1 nM
Compound: 5F-203
|
Anticancer activity against human MCF7 cells assessed as inhibition of cell growth
Anticancer activity against human MCF7 cells assessed as inhibition of cell growth
|
[PMID: 26994845] |
| MCF7 | GI50 |
<0.1 μM
Compound: 130
|
Cytotoxicity against human MCF7 cells
Cytotoxicity against human MCF7 cells
|
[PMID: 31926469] |
| MDA-MB-468 | GI50 |
<0.0001 μM
Compound: 2
|
Antiproliferative activity against human breast cancer cell line MDA468
Antiproliferative activity against human breast cancer cell line MDA468
|
[PMID: 16392802] |
| MDA-MB-468 | GI50 |
<0.1 nM
Compound: 2
|
Antiproliferative activity against human breast cancer cell line MDA468
Antiproliferative activity against human breast cancer cell line MDA468
|
[PMID: 16392802] |
| MDA-MB-468 | GI50 |
<0.0001 μM
Compound: 4a
|
Antiproliferative activity against human MDA-MB-468 cell line
Antiproliferative activity against human MDA-MB-468 cell line
|
[PMID: 16789754] |
| MDA-MB-468 | GI50 |
<0.1 nM
Compound: 4a
|
Antiproliferative activity against human MDA-MB-468 cell line
Antiproliferative activity against human MDA-MB-468 cell line
|
[PMID: 16789754] |
| NCI-H226 | GI50 |
1.3 μM
Compound: 10h
|
Growth inhibition against non-small cell lung cancer cell line NCI-H266
Growth inhibition against non-small cell lung cancer cell line NCI-H266
|
[PMID: 11311068] |
| NCI-H226 | GI50 |
<0.01 μM
Compound: 130
|
Cytotoxicity against human NCI-H226 cells
Cytotoxicity against human NCI-H226 cells
|
[PMID: 31926469] |
| NCI-H460 | GI50 |
0.05 μM
Compound: 10h
|
Growth inhibition against non-small cell lung cancer cell line NCI-H460
Growth inhibition against non-small cell lung cancer cell line NCI-H460
|
[PMID: 11311068] |
| NCI-H460 | GI50 |
<0.01 μM
Compound: 130
|
Cytotoxicity against human NCI-H460 cells
Cytotoxicity against human NCI-H460 cells
|
[PMID: 31926469] |
| OVCAR-4 | GI50 |
<0.01 μM
Compound: 10h
|
Growth inhibition against ovarian cancer cell line OVCAR-4
Growth inhibition against ovarian cancer cell line OVCAR-4
|
[PMID: 11311068] |
| OVCAR-4 | GI50 |
<0.1 μM
Compound: 130
|
Cytotoxicity against human OVCAR-4 cells
Cytotoxicity against human OVCAR-4 cells
|
[PMID: 31926469] |
| OVCAR-5 | GI50 |
<0.01 μM
Compound: 10h
|
Growth inhibition against ovarian cancer cell line OVCAR-5
Growth inhibition against ovarian cancer cell line OVCAR-5
|
[PMID: 11311068] |
| OVCAR-5 | GI50 |
<0.1 μM
Compound: 130
|
Cytotoxicity against human OVCAR-5 cells
Cytotoxicity against human OVCAR-5 cells
|
[PMID: 31926469] |
| T47D | GI50 |
<0.01 μM
Compound: 10h
|
Growth inhibition against breast cancer line T-47-D
Growth inhibition against breast cancer line T-47-D
|
[PMID: 11311068] |
Chemical Information
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CAS No. 260443-89-8
-
Appearance Solid
-
분자량 258.31
-
화학식 C14H11FN2S
-
Color Off-white to light yellow
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SMILES
NC1=CC=C(C2=NC3=CC(F)=CC=C3S2)C=C1C
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Synonyms
NSC-703786
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선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (387.13 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (270 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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hutchinson I, et al. Antitumor benzothiazoles. 16. Synthesis and pharmaceutical properties of antitumor 2-(4-aminophenyl)benzothiazole amino acid prodrugs. J Med Chem. 2002 Jan 31;45(3):744-7. [Content Brief]
[2]. Hose CD, et al. Induction of CYP1A1 in tumor cells by the antitumor agent 2-[4-amino-3-methylphenyl]-5-fluoro-benzothiazole: a potential surrogate marker for patient sensitivity. Mol Cancer Ther. 2003 Dec;2(12):1265-72. [Content Brief]
[3]. Callero MA, et al. Biomarkers of sensitivity to potent and selective antitumor 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F203) in ovarian cancer. J Cell Biochem. 2013 Oct;114(10):2392-404. [Content Brief]
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 | 3.8713 mL | 19.3566 mL | 38.7132 mL | 96.7829 mL |
| 5 mM | 0.7743 mL | 3.8713 mL | 7.7426 mL | 19.3566 mL | |
| 10 mM | 0.3871 mL | 1.9357 mL | 3.8713 mL | 9.6783 mL | |
| 15 mM | 0.2581 mL | 1.2904 mL | 2.5809 mL | 6.4522 mL | |
| 20 mM | 0.1936 mL | 0.9678 mL | 1.9357 mL | 4.8391 mL | |
| 25 mM | 0.1549 mL | 0.7743 mL | 1.5485 mL | 3.8713 mL | |
| 30 mM | 0.1290 mL | 0.6452 mL | 1.2904 mL | 3.2261 mL | |
| 40 mM | 0.0968 mL | 0.4839 mL | 0.9678 mL | 2.4196 mL | |
| 50 mM | 0.0774 mL | 0.3871 mL | 0.7743 mL | 1.9357 mL | |
| 60 mM | 0.0645 mL | 0.3226 mL | 0.6452 mL | 1.6130 mL | |
| 80 mM | 0.0484 mL | 0.2420 mL | 0.4839 mL | 1.2098 mL | |
| 100 mM | 0.0387 mL | 0.1936 mL | 0.3871 mL | 0.9678 mL |