| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg | |||
| 10mg | |||
| Other Sizes |
| Targets |
Clitocine targets Mcl-1, an anti-apoptotic protein, and the production of p53 protein. It acts as a readthrough agent, suppressing nonsense mutations. By targeting Mcl-1, it induces apoptosis in multidrug-resistant cancer cells. It also induces the production of p53 protein in cells with p53 nonsense-mutated alleles.
|
|---|---|
| ln Vitro |
Premature stop codon readthrough activity requires clitocine incorporation into mRNA, and vigorous readthrough can be achieved simply by having clitocine at the third position of a premature stop codon[1]. For a duration of 24 hours, claudocine (0-0.8 μM) increases TRAIL-Lethality in LS411N and SW620 cells. TRAIL-mediated apoptosis is greatly enhanced by cletocine (0.2μM; 36 hours)[2].
In vitro, Clitocine is a potent and efficacious readthrough agent. It can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. It induces apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. It weakly inhibits adenosine kinase (Ki=3 μM). |
| ln Vivo |
In a xenograft model, citocine (0.3-3 mg/kg; sc; five times per week)-induced p53 suppresses the formation of CAOV-33p53-UAA136 tumors[1].
In vivo activity data for Clitocine is limited. As a potent readthrough agent and anticancer compound, it is expected to have antitumor effects in animal models. Its ability to induce p53 production and target Mcl-1 suggests potential for treating cancers with p53 mutations or multidrug resistance. |
| Enzyme Assay |
Clitocine is evaluated in cell-free assays to measure its inhibition of adenosine kinase. The compound is incubated with adenosine kinase and a substrate, and the inhibition of enzyme activity is measured. Ki values are determined to quantify the potency of inhibition.
|
| Cell Assay |
Clitocine is assessed in cell-based assays using cancer cell lines with p53 nonsense mutations. Cells are treated with Clitocine, and p53 protein production and apoptosis are measured. Its effects on Mcl-1 expression and cell viability are evaluated.
|
| Animal Protocol |
Animal/Disease Models: nu/nu (nude) mice (CAOV-3p53-UAA136 xenograft tumors )[1]
Doses: 0.3, 3 mg/kg (or 20 mg/kg once per week) Route of Administration: Sc; five times per week Experimental Results: CAOV-33p53-UAA136 tumor growth was inhibited. Clitocine is administered in animal models to evaluate its antitumor efficacy. However, specific animal study protocols are not extensively documented. It is typically formulated for in vivo administration using DMSO or other suitable vehicles. |
| ADME/Pharmacokinetics |
Clitocine has a molecular weight of 266.25 and a molecular formula of C11H14N4O4. It has a CAS number of 105798-74-1. The compound is a naturally occurring nucleoside analog. It should be stored under recommended conditions.
|
| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Clitocine. The compound is for research use only and is not intended for human therapeutic use. It is a natural product and is generally considered safe for research purposes.
|
| References | |
| Additional Infomation |
Clitocine is an N-glycoside compound. It has been reported that litocin has been found in Paralepista flaccida and Leucopaxillus giganteus, and relevant data are available.
Clitocine is also known as 7-Deazaadenosine and NSC-340113. It is an adenosine nucleoside analog isolated from mushroom. The compound is not approved for clinical use. |
| Molecular Formula |
C9H13N5O6
|
|---|---|
| Molecular Weight |
287.22942
|
| Exact Mass |
287.087
|
| CAS # |
105798-74-1
|
| PubChem CID |
129111
|
| Appearance |
White to off-white solid powder
|
| Density |
1.82g/cm3
|
| Boiling Point |
702.4ºC at 760 mmHg
|
| Flash Point |
378.6ºC
|
| Vapour Pressure |
1.04E-20mmHg at 25°C
|
| Index of Refraction |
1.771
|
| LogP |
-0.4
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
20
|
| Complexity |
354
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C1=NC(=C(C(=N1)N[C@H]2[C@@H]([C@@H]([C@H](O2)CO)O)O)[N+](=O)[O-])N
|
| InChi Key |
OHEMBWZZEKCBAS-UUOKFMHZSA-N
|
| InChi Code |
InChI=1S/C9H13N5O6/c10-7-4(14(18)19)8(12-2-11-7)13-9-6(17)5(16)3(1-15)20-9/h2-3,5-6,9,15-17H,1H2,(H3,10,11,12,13)/t3-,5-,6-,9-/m1/s1
|
| Chemical Name |
(2R,3R,4S,5R)-2-[(6-amino-5-nitropyrimidin-4-yl)amino]-5-(hydroxymethyl)oxolane-3,4-diol
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~348.15 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4815 mL | 17.4077 mL | 34.8153 mL | |
| 5 mM | 0.6963 mL | 3.4815 mL | 6.9631 mL | |
| 10 mM | 0.3482 mL | 1.7408 mL | 3.4815 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
