| Size | Price | Stock | Qty |
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| 10mg |
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| Targets |
XX-650-23 targets CREB, a transcription factor that regulates cell proliferation and survival. It blocks the CREB-CBP interaction, inhibiting CREB-driven gene expression. This disrupts downstream pathways involved in AML maintenance.
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| ln Vitro |
XX-650-23 (870 nM-2.3 μM) has an IC50 value of 870 nM, 910 nM, and 2.0 μM, respectively, and suppresses the proliferation of blank cell lines, HL-60, KG-1, MOLM-13, and MV-4-11. H3K27 noise accelerates less quickly when exposed to Xx-650-23 (5 μM; 6 or 24 hours) [1]. To induce cells to go through the internal channel pathway, Xx-650-23 (2 μM; 72 hours) activates caspase-3 and 2.3 μM [1] and detectable caspase-9 breakage. Reports of Mcl-1 and bcl-2 are also the result [1].
XX-650-23 disrupts the CREB/CBP interaction with an IC50 of 3.2 µM. It suppresses growth of AML cell lines with IC50 values of 0.87–2.3 µM. It induces apoptosis and causes cell cycle arrest. The compound specifically reduces expression of CREB target genes like BCL2 and cyclin D1. |
| ln Vivo |
Specific in vivo data are limited. As a CREB inhibitor, it is expected to show antitumor activity in AML xenografts. Further studies are needed to characterize its pharmacokinetics and pharmacodynamics in animal models.
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| Enzyme Assay |
The in vitro binding assay measures disruption of CREB-CBP interaction using fluorescence polarization or ELISA. The compound is incubated with the proteins, and inhibition is quantified to determine IC50.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: KG-1 cells Tested Concentrations: 5 μM Incubation Duration: 6 or 24 hrs (hours) Experimental Results: diminished H3K27 acetylation expression. Apoptosis analysis [1] Cell Types: HL-60 Cell Tested Concentrations: 2 μM Incubation Duration: 72 hrs (hours) Experimental Results: AML cell apoptosis was induced. The in vitro cellular assay involves culturing AML cell lines and treating with compound. Cell proliferation is measured by MTT. Apoptosis and cell cycle are assessed by flow cytometry. CREB target gene expression is analyzed by qPCR. |
| Animal Protocol |
In vivo studies would use mouse xenograft models of AML. Mice are treated with compound, and tumor growth is monitored. Biomarkers such as CREB activity in tumor tissues are assessed.
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| ADME/Pharmacokinetics |
XX-650-23 has a molecular weight of 341.43 g/mol and a molecular formula of C18H19N3O2S. It is soluble in DMSO and stored at -20°C. Detailed pharmacokinetic data are not publicly available.
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| Toxicity/Toxicokinetics |
Specific toxicology data are not available. The compound is for research use only. Standard safety assessments would be required for clinical translation.
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| References | |
| Additional Infomation |
XX-650-23 is a CREB-CBP interaction inhibitor with anti-AML activity. It is used in cancer research and is not yet in clinical trials.
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| Molecular Formula |
C18H12N2O2
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|---|---|
| Molecular Weight |
288.3
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| Exact Mass |
288.089
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| Elemental Analysis |
C, 74.99; H, 4.20; N, 9.72; O, 11.10
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| CAS # |
117739-40-9
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| Related CAS # |
117739-40-9;
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| PubChem CID |
14978997
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| Appearance |
Off-white to yellow solid powder
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
447
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C=C(C(=CC2=C1)C(=O)NC3=CC=C(C=C3)C#N)O
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| InChi Key |
DRBIYQSSEMTUJQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H12N2O2/c19-11-12-5-7-15(8-6-12)20-18(22)16-9-13-3-1-2-4-14(13)10-17(16)21/h1-10,21H,(H,20,22)
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| Chemical Name |
N-(4-cyanophenyl)-3-hydroxynaphthalene-2-carboxamide
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| Synonyms |
XX65023; XX 650 23; XX-650-23
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.4686 mL | 17.3430 mL | 34.6861 mL | |
| 5 mM | 0.6937 mL | 3.4686 mL | 6.9372 mL | |
| 10 mM | 0.3469 mL | 1.7343 mL | 3.4686 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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