| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Androgen receptor[1]
Masofaniten is an orally active androgen receptor (AR) inhibitor that targets the N-terminal domain (NTD) of the receptor. Unlike classical antiandrogens that bind the ligand-binding domain (LBD), it binds to the intrinsically disordered NTD, which is critical for transcriptional activation and remains a druggable target in therapy-resistant splice variants. |
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| ln Vitro |
Masofaniten (compound A109) inhibits androgen binding to the androgen receptor with an IC50 of 535 nM in the androgen-induced PSA-Luciferase assay[1]. In LNCaP and LNCaP95 cells, mastofaniten inhibits cell proliferation (IC50: 0.44 μM and 3.78 μM, respectively)[1]. In hepatocytes with a t1/2 of more than 360 minutes and in liver microsomes with a t1/2 of more than 120 minutes, mastopaniten exhibits metabolic stability[1].
In cell-free assays, Masofaniten inhibits androgen binding to the androgen receptor with an IC50 of 535 nM in the androgen-induced PSA-Luciferase assay. In LNCaP and LNCaP95 (AR-V7 expressing) cells, it inhibits cell proliferation with IC50s of 0.44 uM and 3.78 uM, respectively, demonstrating activity in both wild-type and resistant models. |
| ln Vivo |
In NCG mice with LNCaP tumors, maselfaniten (compound A109) (60 mg/kg, po) causes partial regressions of tumor growth[1]. In male CD-1 mice, Masofaniten (5 mg/kg, po, single dose) exhibits a t1/2 of 8.1 h, Cmax of 2673.3 ng/mL, and F (%) of 33.6[1].
Masofaniten is an orally active AR inhibitor with demonstrated antitumor activity in vivo. By targeting the AR N-terminal domain, it can suppress the transcriptional activity of both full-length AR and constitutively active splice variants like AR-V7, making it a promising tool for investigating resistance mechanisms in prostate cancer. |
| Enzyme Assay |
Cell-free AR N-terminal domain (NTD) assays are performed using purified AR-NTD and a fluorescently-labeled coactivator peptide. The compound is incubated with the protein, and the displacement of the peptide is measured by fluorescence polarization (FP). The IC50 for inhibiting this protein-protein interaction, which is essential for AR transcriptional activity, is calculated.
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| Cell Assay |
Cellular proliferation assays are performed in androgen-dependent (e.g., LNCaP) and castration-resistant (e.g., 22Rv1) prostate cancer cell lines. Cells are seeded in 96-well plates and treated with Masofaniten for 5-7 days. Cell viability is measured using CellTiter-Glo to calculate the half-maximal inhibitory concentration (IC50) for growth inhibition.
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| Animal Protocol |
Animal/Disease Models: LNCaP Xenografts Model[1]
Doses: 60 mg/kg Route of Administration: Oral administration (po) Experimental Results: Inhibited tumor growth no obvious drug related toxicity (bodyweight change). In vivo efficacy is evaluated in xenograft mouse models of prostate cancer, including those with AR-V7 expression. Masofaniten is administered via daily oral gavage. Tumor volumes are measured with calipers. At study termination, tumors are harvested for analysis of AR target genes (e.g., PSA, TMPRSS2) by qPCR and for AR protein levels by Western blot. |
| ADME/Pharmacokinetics |
Masofaniten is characterized by its favorable oral bioavailability. Its pharmacokinetic profile supports once-daily oral dosing in preclinical species. Systemic exposure and tissue distribution are key metrics being optimized to ensure adequate tumor penetration and sustained suppression of AR transcriptional activity.
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| Toxicity/Toxicokinetics |
Preclinical toxicology data shows that Masofaniten is well-tolerated at efficacious doses. As an AR inhibitor, its primary effects are on-target and related to androgen deprivation. No significant off-target toxicities have been reported, and its unique NTD-binding mechanism may offer a favorable safety profile in certain tissues.
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| References | |
| Additional Infomation |
Masofaniten is a highly bioavailable, orally administered second-generation androgen receptor (AR) N-terminal domain (NTD) inhibitor with potential antitumor activity. After oral administration, Masofaniten specifically binds to the AR NTD, thereby inhibiting AR activation and its mediated signaling pathways. This may suppress the growth of AR-overexpressing tumor cells. AR is overexpressed in prostate cancer and is involved in tumor cell proliferation, survival, and chemoresistance. Compared to first-generation AR NTD inhibitors, Masofaniten may exhibit higher activity and metabolic stability.
Masofaniten, also known as EPI-7386, is a research compound representing a new class of antiandrogens that target the AR N-terminal domain. It has been investigated in clinical trials as a potential treatment for prostate cancer, including mCRPC resistant to enzalutamide. It is an important tool for validating NTD inhibition as a therapeutic strategy. |
| Molecular Formula |
C24H24CL2N4O4S
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|---|---|
| Molecular Weight |
535.442762374878
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| Exact Mass |
534.089
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| CAS # |
2416716-62-4
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| PubChem CID |
146484310
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| Appearance |
Light yellow to light brown solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
35
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| Complexity |
823
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CS(NC1=NC=CC(COC2=CC=C(C(C3=CC(C#N)=C(OCCCl)C(Cl)=C3)(C)C)C=C2)=N1)(=O)=O
|
| InChi Key |
GVCZSODXLFBYSS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H24Cl2N4O4S/c1-24(2,18-12-16(14-27)22(21(26)13-18)33-11-9-25)17-4-6-20(7-5-17)34-15-19-8-10-28-23(29-19)30-35(3,31)32/h4-8,10,12-13H,9,11,15H2,1-3H3,(H,28,29,30)
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| Chemical Name |
N-[4-[[4-[2-[3-chloro-4-(2-chloroethoxy)-5-cyanophenyl]propan-2-yl]phenoxy]methyl]pyrimidin-2-yl]methanesulfonamide
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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: 50 mg/mL (93.38 mM)
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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 | 1.8676 mL | 9.3381 mL | 18.6762 mL | |
| 5 mM | 0.3735 mL | 1.8676 mL | 3.7352 mL | |
| 10 mM | 0.1868 mL | 0.9338 mL | 1.8676 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.
Link: https://clinicaltrials.gov/ct2/show/NCT06312670
Conditions:Metastatic Hormone-sensitive Prostate Cancer (mHSPC)|Prostate Cancer|Prostate AdenocarcinomaLink: https://clinicaltrials.gov/ct2/show/NCT04421222
Conditions:Prostate CancerLink: https://clinicaltrials.gov/ct2/show/NCT05295927
Conditions:Prostatic NeoplasmsProducts are for research use only; We do not sell to patients
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