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CTX1

Alias: CTX1 CTX 1 CTX-1
Cat No.:V7527 Purity: ≥98%
CTX1 is a p53 activator that can overcome HdmX-mediated repression of p53.
CTX1
CTX1 Chemical Structure CAS No.: 501935-96-2
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
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Product Description
CTX1 is a p53 activator that can overcome HdmX-mediated repression of p53. CTX1 displays potent anti-cancer effect in mouse acute myeloid leukemia (AML) models.
Biological Activity I Assay Protocols (From Reference)
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].
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].
References

[1]. Identification of a Small Molecule That Overcomes HdmX-Mediated Suppression of p53. Mol Cancer Ther. 2016 Apr;15(4):574-582.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C14H10N4
Molecular Weight
234.26
Exact Mass
234.09
CAS #
501935-96-2
PubChem CID
435038
Appearance
Reddish brown to red solid powder
Density
1.4±0.1 g/cm3
Boiling Point
582.5±30.0 °C at 760 mmHg
Flash Point
306.1±24.6 °C
Vapour Pressure
0.0±1.6 mmHg at 25°C
Index of Refraction
1.797
LogP
0.54
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
0
Heavy Atom Count
18
Complexity
334
Defined Atom Stereocenter Count
0
InChi Key
PUMGFEMNXBLDKD-UHFFFAOYSA-N
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
Chemical Name
3,6-diaminoacridine-9-carbonitrile
Synonyms
CTX1 CTX 1 CTX-1
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 Data
Solubility (In Vitro)
DMSO : ~12.5 mg/mL (~53.36 mM)
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
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
Biological Data
  • Identification of novel HdmX inhibitors A. Identification of novel compounds that induce a p21/ConA-β-gal reporter in MCF7 cells. MCF7 cells were treated for 24hr with the indicated compounds (2μM) and β-gal activity was measured. B. CTX1 and CTX6 exhibit p53-dependent activation of the reporter construct. MCF7 and MCF7shp53 cells were treated with the indicated compounds and β-gal activity was measured as described in fig1a. C. CTX1 and CTX6 induce p53 and p21. MCF7 cells were treated with CTX1 (2μM), CTX6 (3μM), or nutlin-3 (10μM) for 6hr and a western blot was performed. D. Structure of CTX1 and CTX1-biotin. Error bars represent standard deviation.[1].Karan G, et al. Identification of a Small Molecule That Overcomes HdmX-Mediated Suppression of p53. Mol Cancer Ther. 2016 Apr;15(4):574-582
  • CTX1 rapidly induces p53 independent of DNA damage A–B. MCF7 cells were treated with CTX1 (3μM) or Doxorubicin (1μM) for the indicated times (hours) and western analysis was performed for markers of DNA damage (p-p53 (Ser15) and p-H2AX). C. HCT116 cells (left panel) or OCI cells (right panel) were treated with the indicated doses of CTX1 or Doxorubicin for 9 hours and western analysis was performed using the indicated antibodies.[1].Karan G, et al. Identification of a Small Molecule That Overcomes HdmX-Mediated Suppression of p53. Mol Cancer Ther. 2016 Apr;15(4):574-582
  • CTX1 specifically targets and directly binds to HdmX A. CTX1 preferentially kills cells transformed by HdmX and not Hdm2 or shp53. IMR90 cells overexpressing the indicated constructs were treated with increasing doses of CTX1 (1, 2.5 and 5μM) and assessed for cell death at 72hr by trypan blue staining. B. CTX1 binds HdmX and to a lesser extent p53. Recombinant p53, HdmX, and/or biotin-CTX1 were incubated in vitro and streptavidin beads were used to pull down the protein complex. The bound protein was eluted and analyzed by western blot with the indicated antibodies. C. Spectral studies suggest CTX1 and HdmX directly interact. CTX1 and HdmX alone represent the spectral pattern of both agents without purification. The CTX1+HdmX sample and CTX1 Postcolumn Residual samples underwent size exclusion chromatography to remove unbound CTX1. D–E. CTX1 disrupts the interaction of recombinant HdmX/p53 but not Hdm2/p53 by ELISA and co-immunoprecipitation. The indicated drugs were used as controls. F. CTX1 disrupts the interaction of HdmX/p53 in cells. Immunoprecipitations were performed as indicated using lysate from OCI cells treated with the indicated drugs or a DMSO control. Error bars represent standard deviation.[1].Karan G, et al. Identification of a Small Molecule That Overcomes HdmX-Mediated Suppression of p53. Mol Cancer Ther. 2016 Apr;15(4):574-582
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