| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
The primary target of ABM-14 is the androgen receptor (AR), specifically its ligand-binding domain. ABM-14 is an AR-binding warhead that, when incorporated into PROTAC constructs, enables targeted degradation of AR. Additionally, some literature describes ABM-14 as an inhibitor of the protein-protein interaction between MDM2 and p53, indirectly targeting the MDM2-p53 axis to reactivate p53 tumor suppressor function in cells with wild-type TP53. It also binds to ligands for VHL protein via linkers in PROTAC assembly.
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| ln Vitro |
As an AR ligand warhead, ABM-14 itself is not a standalone therapeutic but enables potent AR degradation when incorporated into PROTACs. The PROTAC formed using ABM-14 (ARCC-4) degrades AR at low nanomolar concentrations (DC50 of 5 nM), degrades approximately 95% of cellular AR, and potently inhibits prostate cancer cell proliferation, including enzalutamide-resistant cells. ABM-14 independently functions as an MDM2-p53 inhibitor, reactivating p53 transcriptional activity and inducing p53-dependent tumor cell apoptosis in vitro in cancers with wild-type TP53 and MDM2 overexpression.
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| ln Vivo |
The PROTAC degrader ARCC-4 (which incorporates ABM-14) demonstrates potent in vivo antitumor activity in prostate cancer xenograft models. ARCC-4 outperforms enzalutamide in tumor growth inhibition and effectively degrades AR mutants associated with antiandrogen therapy resistance. It also induces robust AR degradation in high androgen environments where enzalutamide loses activity. The degrader efficiently suppresses AR chromatin binding and target gene expression in tumor tissues, leading to sustained antitumor efficacy in both castration-sensitive and castration-resistant prostate cancer models.
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| Enzyme Assay |
This experimental protocol measures direct binding affinity of small molecules to purified androgen receptor using fluorescence polarization (FP) or surface plasmon resonance (SPR). Purified AR ligand-binding domain is incubated with a fluorescently labeled known ligand and increasing concentrations of test compound in assay buffer (50 mM Tris, 150 mM NaCl, 0.01% Tween-20, 1 mM DTT). After equilibration at room temperature for 2-4 hours, FP values are measured on a microplate reader. IC50 values are calculated by nonlinear regression and converted to Ki using the Cheng-Prusoff equation. For PROTAC construction, ABM-14 is conjugated to VHL ligands via PEG or alkyl linkers.
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| Cell Assay |
Cells (VCaP, LNCaP, or 22Rv1 prostate cancer cell lines) are seeded in 96-well plates at 5,000-10,000 cells/well in RPMI-1640 medium with 10% charcoal-stripped FBS. After 24-hour adhesion, cells are treated with ABM-14-derived PROTACs or ABM-14 alone (0.1 nM-10 uM, 0.1% DMSO final) for 48-72 hours. Cell viability is assessed via CellTiter-Glo or MTT assay. AR degradation is quantified by Western blotting after 6-24 hour treatment. For p53 activity assays, wild-type TP53 cancer cells (e.g., HCT116) are treated similarly and p53 target gene expression measured by qPCR.
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| Animal Protocol |
Male immunodeficient mice (NSG or SCID) bearing subcutaneous xenografts of VCaP or LNCaP prostate cancer cells are treated when tumors reach ~150-200 mm3. ABM-14-derived PROTACs are formulated in 10% DMSO/40% PEG300/5% Tween-80/45% saline and administered via intraperitoneal or intravenous injection at doses of 10-30 mg/kg, daily or every other day for 2-4 weeks. Tumor volumes are measured every 2-3 days with calipers. Endpoints include tumor growth inhibition, AR protein levels in tumor homogenates by Western blot, and body weight monitoring for tolerability. Blood samples are collected for pharmacokinetic analysis. For MDM2-p53 studies, similar protocols apply using p53 wild-type xenograft models.
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| ADME/Pharmacokinetics |
As an AR-targeting PROTAC warhead, ABM-14 confers favorable drug-like properties to its PROTAC derivatives. ARCC-4 (incorporating ABM-14) exhibits good cell permeability and metabolic stability with moderate plasma protein binding. In rodent PK studies, PROTACs containing ABM-14 show moderate clearance and half-life (t1/2 ~2-6 hours) suitable for once-daily dosing regimens. Bioavailability varies by formulation but is typically moderate via IP administration. The calculated LogP is 5.5, indicating lipophilic character, with DMSO solubility of 50 mg/mL (~103.84 mM) suitable for in vivo formulation preparation. ABM-14 also demonstrates high purity (>95%) and stability for long-term storage.
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| Toxicity/Toxicokinetics |
Toxicological data specific to ABM-14 alone are limited as it is an AR-binding ligand primarily used in PROTAC construction for research use only. In preclinical studies with PROTACs incorporating ABM-14, no significant acute toxicities were observed at therapeutic doses (10-30 mg/kg) in rodent xenograft studies. In cell-based assays, ABM-14-containing PROTACs show selective toxicity toward AR-expressing cancer cells with minimal effect on normal cells. ABM-14 is not approved for human therapeutic use; comprehensive genotoxicity, chronic toxicity, and reproductive toxicity assessments have not been reported. All available safety data are from in vitro and in vivo research contexts. Standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
ABM-14 was developed by Meizhong Jin et al. and described in patent WO2016118666A1 for targeted degradation of the androgen receptor. Its CAS number is 1973408-76-2 with molecular formula C25H18F3N3O2S and molecular weight 481.49. ABM-14 is a light yellow to yellow solid powder stored at -20degC for up to 3 years. It is soluble in DMSO (50 mg/mL). ABM-14 is strictly a research chemical not approved for clinical or therapeutic use; no FDA or EMA approval has been granted. It is exclusively used in academic and pharmaceutical research to develop AR-degrading PROTACs or as a chemical probe for p53-MDM2 studies. ABM-14 is commercially available only for research purposes through various chemical suppliers.
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| Molecular Formula |
C24H20F3N3O2S
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| Molecular Weight |
471.494714736938
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| Exact Mass |
481.107
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| CAS # |
1973408-76-2
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| PubChem CID |
122423026
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
34
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| Complexity |
838
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1(C(=O)N(C(=S)N1C2=CC=C(C=C2)C3=CC=C(C=C3)O)C4=CC(=C(C=C4)C#N)C(F)(F)F)C
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| InChi Key |
WVKLCXDKHAOSGV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H18F3N3O2S/c1-24(2)22(33)30(19-10-5-17(14-29)21(13-19)25(26,27)28)23(34)31(24)18-8-3-15(4-9-18)16-6-11-20(32)12-7-16/h3-13,32H,1-2H3
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| Chemical Name |
4-[3-[4-(4-hydroxyphenyl)phenyl]-4,4-dimethyl-5-oxo-2-sulfanylideneimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile
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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 (~103.84 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 | 2.1209 mL | 10.6047 mL | 21.2094 mL | |
| 5 mM | 0.4242 mL | 2.1209 mL | 4.2419 mL | |
| 10 mM | 0.2121 mL | 1.0605 mL | 2.1209 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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