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| 10mg |
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| Targets |
Fequesetide targets the G2 checkpoint in the cell cycle. The compound inhibits the G2 checkpoint, preventing cancer cells from repairing DNA damage before entering mitosis. By abrogating the G2 checkpoint, fequesetide sensitizes cancer cells to DNA-damaging agents, leading to mitotic catastrophe and apoptosis. The specific molecular target of fequesetide is being elucidated.
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|---|---|
| ln Vitro |
Fequesetide demonstrates in vitro chemosensitizing activity by abrogating the G2 checkpoint in cancer cells. It enhances the cytotoxicity of DNA-damaging agents such as cisplatin and radiation. The compound's activity is assessed in cell-based assays measuring cell viability, cell cycle distribution, and DNA damage responses.
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| ln Vivo |
In vivo activity of fequesetide has been demonstrated in animal models of cancer, where it enhances the antitumor efficacy of DNA-damaging chemotherapeutic agents. The compound is being investigated in clinical trials as a chemosensitizer in combination with chemotherapy for the treatment of various cancers.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for fequesetide are not extensively documented, as its mechanism involves cell cycle checkpoint abrogation. The compound's ability to inhibit the G2 checkpoint can be assessed by measuring cell cycle distribution using flow cytometry and by evaluating mitotic entry following DNA damage.
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| Cell Assay |
In vitro cellular assays for fequesetide involve treating cancer cell lines with the compound in combination with DNA-damaging agents (e.g., cisplatin). Cell viability is assessed using MTT or other assays. Cell cycle distribution is analyzed by flow cytometry. DNA damage and mitotic catastrophe are evaluated by measuring γ-H2AX and other markers.
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| Animal Protocol |
In vivo animal experiments for fequesetide involve administering the compound to tumor-bearing mouse models in combination with DNA-damaging chemotherapeutic agents. Efficacy is evaluated by measuring tumor growth inhibition, survival rates, and biomarker changes such as DNA damage and apoptosis markers.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for fequesetide are derived from preclinical and clinical studies. The compound is administered intravenously. Its distribution, metabolism, and elimination are being characterized. The compound's pharmacokinetic profile supports its use as a chemosensitizer in combination with chemotherapy.
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| Toxicity/Toxicokinetics |
Toxicological data for fequesetide are derived from preclinical and clinical studies. The compound is generally well-tolerated when used in combination with chemotherapy. Common adverse effects may include those associated with the chemotherapeutic agents used in combination. Comprehensive toxicological studies are being conducted.
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| References | |
| Additional Infomation |
Fequesetide (CAS#: 476014-70-7) is a synthetic peptide that acts as a G2 checkpoint abrogator. It enhances the antitumor activity of DNA-damaging agents by abrogating the G2 checkpoint, leading to mitotic catastrophe and cell death. The compound is being investigated as a chemosensitizer in combination with chemotherapy for the treatment of cancer.
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| Molecular Formula |
C36H66N10O13
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|---|---|
| Molecular Weight |
846.97
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| Exact Mass |
846.481
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| CAS # |
476014-70-7
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| PubChem CID |
10169788
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| Appearance |
White to off-white solid powder
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| LogP |
0.649
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
31
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| Heavy Atom Count |
59
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| Complexity |
1420
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C[C@H]([C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(=O)N)C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)N)O
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| InChi Key |
LVLWJWXFRFTMLK-JMWNXRNDSA-N
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| InChi Code |
InChI=1S/C36H66N10O13/c1-18(2)17-21(39)30(52)41-22(9-5-7-15-37)31(53)42-23(10-6-8-16-38)32(54)45-28(19(3)47)34(56)43-24(12-14-27(50)51)33(55)46-29(20(4)48)35(57)44-25(36(58)59)11-13-26(40)49/h18-25,28-29,47-48H,5-17,37-39H2,1-4H3,(H2,40,49)(H,41,52)(H,42,53)(H,43,56)(H,44,57)(H,45,54)(H,46,55)(H,50,51)(H,58,59)/t19-,20-,21+,22+,23+,24+,25+,28+,29+/m1/s1
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| Chemical Name |
(2S)-5-amino-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-amino-4-methylpentanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-hydroxybutanoyl]amino]-4-carboxybutanoyl]amino]-3-hydroxybutanoyl]amino]-5-oxopentanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ≥ 100 mg/mL (118.07 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1807 mL | 5.9034 mL | 11.8068 mL | |
| 5 mM | 0.2361 mL | 1.1807 mL | 2.3614 mL | |
| 10 mM | 0.1181 mL | 0.5903 mL | 1.1807 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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