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| Targets |
CTX1 targets the p53-HdmX (MDMX) interaction. p53 is a tumor suppressor protein that plays a critical role in regulating cell cycle arrest, DNA repair, and apoptosis in response to cellular stress. HdmX (also known as MDMX) is a negative regulator of p53 that binds to the p53 transactivation domain and inhibits its transcriptional activity. Overexpression of HdmX is a common mechanism by which cancer cells evade p53-mediated tumor suppression. CTX1 selectively binds to HdmX, preventing the formation of the p53-HdmX complex. This liberates p53 from HdmX-mediated repression, allowing it to activate the transcription of its target genes and induce cell cycle arrest and apoptosis. By targeting the p53-HdmX interaction, CTX1 reactivates the p53 pathway in cancer cells.
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| ln Vitro |
By directly binding to HdmX, CTX1 inhibits the development of the p53-HdmX complex and quickly induces p53 in a way that is independent of DNA damage [1].
In vitro studies have demonstrated that CTX1 is a potent activator of p53. It selectively binds to HdmX, preventing p53-HdmX complex formation. This results in rapid, DNA damage-independent induction of wild-type p53 transcriptional activity. CTX1 activates p53 in cancer cells, leading to the upregulation of p53 target genes involved in cell cycle arrest and apoptosis. The compound's ability to overcome HdmX-mediated p53 repression makes it a valuable tool for studying the p53 pathway. |
| ln Vivo |
In an AML model system, mice treated with CTX1 (30 mg/kg; intraperitoneal injection; five days per week; for three weeks) have a markedly higher survival rate [1]. Both by itself and in conjunction with nutlin-3, CTX1 exhibited strong anticancer activity[1].
In vivo studies have demonstrated that CTX1 exhibits potent anti-cancer activity. In a mouse acute myeloid leukemia (AML) model system, CTX1 has been shown to have potent anti-cancer activity. The compound overcomes HdmX-mediated p53 repression and activates the p53 pathway, leading to tumor suppression. These findings suggest that CTX1 may have therapeutic potential for cancers characterized by HdmX overexpression. CTX1 is used as a research tool to study the p53 pathway and to explore potential therapeutic strategies for cancer. |
| Enzyme Assay |
The in vitro assays for CTX1 measure its binding to HdmX and its ability to activate p53 transcriptional activity. The binding of CTX1 to HdmX can be measured using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). Alternatively, a fluorescence polarization or AlphaScreen assay can be used to measure the displacement of a labeled p53 peptide from HdmX. The activation of p53 transcriptional activity is measured using a reporter gene assay. Cells are transfected with a plasmid containing a luciferase gene under the control of a p53-responsive promoter. CTX1 is added, and the luciferase activity is measured. An increase in luciferase activity indicates activation of p53 transcriptional activity.
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| Cell Assay |
In vitro cell-based assays for CTX1 are used to study its effects on p53 signaling and cancer cell biology. A typical assay involves treating cancer cell lines with varying concentrations of CTX1. The expression of p53 target genes, such as p21 and PUMA, is measured by qPCR or Western blotting. Cell cycle analysis is performed by flow cytometry. Apoptosis is measured using Annexin V staining or caspase-3/7 activation assays. Cell viability is assessed using assays such as MTT or CellTiter-Glo. These cell-based assays confirm that CTX1 activates p53 and exerts anti-cancer effects in cancer cells.
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| Animal Protocol |
In vivo animal experiments for CTX1 have been conducted in mouse models of cancer. In a typical study, mice are implanted with cancer cells, such as AML cells, and CTX1 is administered. Tumor growth is monitored, and the survival of the mice is recorded. The anti-cancer activity of CTX1 is assessed by measuring tumor growth inhibition and survival benefit. These studies provide evidence for the in vivo efficacy of CTX1 and support its potential as a therapeutic agent for cancers characterized by HdmX overexpression.
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| ADME/Pharmacokinetics |
CTX1 has a molecular weight of 234.26 g/mol and a molecular formula of C14H10N4. For research use, CTX1 is typically supplied as a powder. It is soluble in DMSO and other organic solvents. For storage, it is recommended to keep the powder at -20°C in a dry, dark environment. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. CTX1 is a research compound and is not intended for human or veterinary use.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for CTX1 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. In vivo studies have used CTX1 at doses that exhibit anti-cancer activity without apparent toxicity. However, comprehensive toxicological studies, including acute and chronic toxicity studies, have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling CTX1. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References | |
| Additional Infomation |
CTX1 is a research compound and is not approved for any clinical or therapeutic use. It is a p53 activator that overcomes HdmX-mediated p53 repression. CTX1 selectively binds the HdmX (MDMX) protein to prevent p53-HdmX complex formation, resulting in rapid, DNA damage-independent induction of wild-type p53 transcriptional activity. CTX1 exhibits potent anti-cancer activity in a mouse acute myeloid leukemia (AML) model system. The compound is used to study the p53 pathway and to explore potential therapeutic strategies for cancer. Its mechanism of action involves activating p53 by inhibiting its interaction with HdmX.
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| Molecular Formula |
C14H10N4
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| Molecular Weight |
234.26
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| Exact Mass |
234.09
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| CAS # |
501935-96-2
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| PubChem CID |
435038
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| Appearance |
Reddish brown to red solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
582.5±30.0 °C at 760 mmHg
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| Flash Point |
306.1±24.6 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.797
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| LogP |
0.54
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
18
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| Complexity |
334
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PUMGFEMNXBLDKD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H10N4/c15-7-12-10-3-1-8(16)5-13(10)18-14-6-9(17)2-4-11(12)14/h1-6H,16-17H2
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| Chemical Name |
3,6-diaminoacridine-9-carbonitrile
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| Synonyms |
CTX1 CTX 1 CTX-1
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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 |
| 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) |
DMSO : ~12.5 mg/mL (~53.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (5.34 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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: 1.25 mg/mL (5.34 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2688 mL | 21.3438 mL | 42.6876 mL | |
| 5 mM | 0.8538 mL | 4.2688 mL | 8.5375 mL | |
| 10 mM | 0.4269 mL | 2.1344 mL | 4.2688 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02053753 | COMPLETEDWITH RESULTS | Drug: Denosumab CP4 Drug: Denosumab CP2 |
Healthy Volunteer | Amgen | 2014-02 | Phase 1 |
| NCT06395883 | NOT YET RECRUITING | Drug: Glucocorticoid Effect | Inflammatory Rheumatism Osteoporosis Osteoporosis, Steroid Induced |
Diakonhjemmet Hospital | 2024-09 | |
| NCT04259242 | COMPLETED | Procedure: SRP | Periodontitis | Postgraduate Institute of Dental Sciences Rohtak | 2020-01-01 | Not Applicable |
| NCT04213105 | UNKNOWN STATUS | Drug: QL1206 Drug: Prolia® |
Healthy People | Qilu Pharmaceutical Co., Ltd. | 2019-10-31 | Phase 1 |
| NCT04198636 | UNKNOWN STATUS | Drug: LY01011 Drug: Xgeva 120 MG in 1.7 ML Injection |
Healthy Adults | Luye Pharma Group Ltd. | 2019-12-16 | Phase 1 |
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