FR901464
Based on 1 Customer Validation
FR901464 is a potent spliceosome inhibitor with prominent anti-tumor and anti-cancer effects.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.08%
- No. CAS: 146478-72-0
- Fòrmula: C27H41NO8
- Peso molecular:507.62
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
1 nM
Compound: FR901464
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Antiproliferative activity against human A549 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay
Antiproliferative activity against human A549 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay
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10.1039/C0MD00179A |
| A549 | IC50 |
0.0013 μM
Compound: FR-901464
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Cytotoxicity against human A549 cells after 72 hrs by XTT colorimetric assay
Cytotoxicity against human A549 cells after 72 hrs by XTT colorimetric assay
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[PMID: 18788726] |
| DU-145 | GI50 |
1.05 nM
Compound: 4, FR901464
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Antiproliferative activity against human DU145 cells assessed as growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human DU145 cells assessed as growth inhibition measured after 48 hrs by MTT assay
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[PMID: 23517093] |
| HCT-116 | GI50 |
1 nM
Compound: FR901464
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Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay
Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay
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10.1039/C0MD00179A |
| HEK293 | IC50 |
0.58 μM
Compound: 4, FR901464
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Inhibition of Pre-mRNA splicing in human HEK293 cells using p32-labeled CDC14-15 pre-mRNA by exonjunction complex (EJC) immunoprecipitation assay
Inhibition of Pre-mRNA splicing in human HEK293 cells using p32-labeled CDC14-15 pre-mRNA by exonjunction complex (EJC) immunoprecipitation assay
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[PMID: 23517093] |
| MCF7 | GI50 |
1 nM
Compound: FR901464
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Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay
Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay
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10.1039/C0MD00179A |
| MCF7 | GI50 |
1.1 nM
Compound: 1; FR901464
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Cytotoxicity against human MCF7 cells incubated for 7 to 10 days by MTS assay
Cytotoxicity against human MCF7 cells incubated for 7 to 10 days by MTS assay
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[PMID: 33974423] |
| MCF7 | IC50 |
0.0018 μM
Compound: FR-901464
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Cytotoxicity against human MCF7 cells after 72 hrs by XTT colorimetric assay
Cytotoxicity against human MCF7 cells after 72 hrs by XTT colorimetric assay
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[PMID: 18788726] |
| MDA-MB-231 | GI50 |
2.1 nM
Compound: 4, FR901464
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Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 48 hrs by MTT assay
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[PMID: 23517093] |
| P388 | GI50 |
1 nM
Compound: FR901464
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Antiproliferative activity against mouse P388 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay
Antiproliferative activity against mouse P388 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay
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10.1039/C0MD00179A |
| SK-OV-3 | GI50 |
1.06 nM
Compound: 4, FR901464
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Antiproliferative activity against human SKOV3 cells assessed as growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human SKOV3 cells assessed as growth inhibition measured after 48 hrs by MTT assay
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[PMID: 23517093] |
FR901464 (10-20 ng/ml; 6-24 hours) inhibits the growth of murine solid tumors, Colon 38 carcinoma and Meth A fibrosarcoma. FR901464 induces characteristic G1 and G2/M phase arrest in the cell cycle and internucleosomal degradation of genomic DNA with the same kinetics as activation of SV40 promoter-dependent cellular transcription in M-8 tumor cells[1].FR901464 (1-10 ng/ml; 16 hours) suppresses the transcription of some inducible endogenous genes but not house keeping genes in M-8 cells[1].FR901464 exhibits potent anticancer activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 146478-72-0
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Appearance Solid
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Peso molecular 507.62
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Fòrmula C27H41NO8
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Color White to off-white
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SMILES
O[C@H]([C@H](O1)/C=C/C(C)=C/C[C@H](O[C@@H]2C)[C@H](C[C@H]2NC(/C=C\[C@H](C)OC(C)=O)=O)C)[C@@]3(C[C@]1(O)C)CO3
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Structure Classification
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Initial Source
Pseudomonas sp
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (197.00 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 (4.92 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:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. H Nakajima, et al. New antitumor substances, FR901463, FR901464 and FR901465. II. Activities against experimental tumors in mice and mechanism of action. J Antibiot (Tokyo). 1996 Dec;49(12):1204-11. [Content Brief]
[2]. Arun K Ghosh, et al. Enantioselective total syntheses of FR901464 and spliceostatin A and evaluation of splicing activity of key derivatives. J Org Chem. 2014 Jun 20;79(12):5697-709. [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 | 1.9700 mL | 9.8499 mL | 19.6998 mL | 49.2494 mL |
| 5 mM | 0.3940 mL | 1.9700 mL | 3.9400 mL | 9.8499 mL | |
| 10 mM | 0.1970 mL | 0.9850 mL | 1.9700 mL | 4.9249 mL | |
| 15 mM | 0.1313 mL | 0.6567 mL | 1.3133 mL | 3.2833 mL | |
| 20 mM | 0.0985 mL | 0.4925 mL | 0.9850 mL | 2.4625 mL | |
| 25 mM | 0.0788 mL | 0.3940 mL | 0.7880 mL | 1.9700 mL | |
| 30 mM | 0.0657 mL | 0.3283 mL | 0.6567 mL | 1.6416 mL | |
| 40 mM | 0.0492 mL | 0.2462 mL | 0.4925 mL | 1.2312 mL | |
| 50 mM | 0.0394 mL | 0.1970 mL | 0.3940 mL | 0.9850 mL | |
| 60 mM | 0.0328 mL | 0.1642 mL | 0.3283 mL | 0.8208 mL | |
| 80 mM | 0.0246 mL | 0.1231 mL | 0.2462 mL | 0.6156 mL | |
| 100 mM | 0.0197 mL | 0.0985 mL | 0.1970 mL | 0.4925 mL |
FR901464 Related Classifications
HY-16212 Related Classifications
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