| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 500mg |
|
||
| Other Sizes |
| Targets |
Wnt/beta-catenin signaling pathway; p300 histone acetyltransferase. Windorphen specifically targets the C-terminal transactivation domain of beta-catenin-1 but not beta-catenin-2. It is also a selective p300 HAT inhibitor with an IC50 of 4.2 μM. p300 is a coactivator associated with beta-catenin.
|
|---|---|
| ln Vitro |
Windorphen demonstrates inhibition of Wnt/beta-catenin signaling in cellular assays. It potently and selectively kills cancer cells carrying Wnt-activating mutations. The compound inhibits p300 histone acetyltransferase activity with an IC50 of 4.2 μM. Detailed cellular IC50 values have not been disclosed.
|
| ln Vivo |
Windorphen potently and selectively kills cancer cells carrying Wnt-activating mutations in vivo, supporting the therapeutic potential of this class of Wnt inhibitors. In vivo activity has been demonstrated in cancer models. Additional in vivo studies would be needed to fully characterize its therapeutic potential.
|
| Enzyme Assay |
In vitro enzyme assays for p300 HAT inhibition are performed using recombinant p300 enzyme, acetyl-CoA, and a histone substrate. Windorphen is incubated at varying concentrations with the enzyme and substrate. Acetylation is detected by radioactivity or immunoassay. IC50 values are calculated from dose-response curves. For Wnt/beta-catenin signaling, reporter gene assays (e.g., TOPFlash) are used.
|
| Cell Assay |
Cells (e.g., cancer cell lines with Wnt-activating mutations) are cultured and treated with Windorphen at concentrations typically ranging from 0.1–50 μM for 24–72 hours. Wnt/beta-catenin signaling inhibition is assessed by measuring beta-catenin target gene expression (e.g., c-Myc, cyclin D1) by qPCR or Western blot. Cell viability and proliferation are assessed by standard assays.
|
| Animal Protocol |
In vivo animal studies for Windorphen have been conducted in xenograft models of Wnt-activated cancers. The compound is administered orally or intraperitoneally at doses typically ranging from 5–50 mg/kg. Tumor growth inhibition and survival are evaluated. Standard protocols for Wnt inhibitor studies in mice are used.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Windorphen have not been extensively published. The compound has a molecular weight of 302.75 and formula C17H15ClO3. Solubility information is limited. In vivo PK parameters such as half-life, bioavailability, and tissue distribution have not been fully characterized.
|
| Toxicity/Toxicokinetics |
Toxicology data for Windorphen have not been published. The compound is for research use only and not approved for human therapeutic applications. No systematic toxicological evaluation has been performed. Standard safety precautions for handling chemical inhibitors should be observed.
|
| References | |
| Additional Infomation |
Windorphen (CAS: 19881-70-0, molecular formula C17H15ClO3, molecular weight 302.75) is a Wnt/beta-catenin signaling inhibitor and p300 HAT inhibitor. It targets beta-catenin-1 C-terminal transactivation domain. It is not in clinical trials and has no regulatory approval. The compound is supplied as a research-grade inhibitor for laboratory use only.
|
| Molecular Formula |
C17H15CLO3
|
|---|---|
| Molecular Weight |
302.75
|
| Exact Mass |
302.071
|
| CAS # |
19881-70-0
|
| PubChem CID |
735820
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.198g/cm3
|
| Boiling Point |
468.1ºC at 760mmHg
|
| Melting Point |
160-163ºC
|
| Flash Point |
184.7ºC
|
| Vapour Pressure |
6.15E-09mmHg at 25°C
|
| Index of Refraction |
1.579
|
| LogP |
4.009
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
21
|
| Complexity |
364
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=CC=C(C=C1)/C(=C(\C2=CC=C(C=C2)OC)/Cl)/C=O
|
| InChi Key |
VNRALGZMXHFBPG-WUKNDPDISA-N
|
| InChi Code |
InChI=1S/C17H15ClO3/c1-20-14-7-3-12(4-8-14)16(11-19)17(18)13-5-9-15(21-2)10-6-13/h3-11H,1-2H3/b17-16+
|
| Chemical Name |
(Z)-3-chloro-2,3-bis(4-methoxyphenyl)prop-2-enal
|
| 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) |
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
|
|---|---|
| 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 | 3.3031 mL | 16.5153 mL | 33.0306 mL | |
| 5 mM | 0.6606 mL | 3.3031 mL | 6.6061 mL | |
| 10 mM | 0.3303 mL | 1.6515 mL | 3.3031 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
