ODM-201 (Synonyms: BAY 1841788) |
Catalog No.GC11386
One-Click Copy Product Info
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ODM-201 is a potent antagonist of the androgen receptor (AR) with a Ki value of 11nM and an IC50 value of 26nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1297538-32-9
Sample solution is provided at 25 µL, 10mM.
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ODM-201 is a potent antagonist of the androgen receptor (AR) with a Ki value of 11nM and an IC50 value of 26nM [1]. ODM-201 maintains the binding conformation in the F877L-mutated pocket through hydrogen and Van der Waals interactions, inhibiting transcriptional activity of AR mutants [2]. ODM-201 has been widely used in preclinical models to inhibit the progression of prostate cancer[3].
In vitro, ODM-201 treatment for 6 days significantly inhibited the viability of LNCaP/AR cells, with an IC50 value of 1.65µM[4]. Treatment with 10µM ODM-201 for 72 hours significantly inhibited the growth of C4-2 cells and induced cellular senescence, down-regulating the mRNA level of CDKN2A and the protein level of p16[5]. Treatment with 30µM ODM-201 for 4 days significantly reduced the expression of cyclin D1 in BT-549 cells, upregulated the phosphorylation of ERK, and inhibited cell proliferation[6].
In vivo, ODM-201 treatment via intraperitoneally injection at a dose of 20mg/kg/day for 14 days inhibited the tumor growth in mice with LNCaP cell xenografts[7]. Oral administration of 100mg/kg dose of ODM-201 daily for 2 months significantly inhibited tumor growth in the xenograft mouse model of KuCaP-1 prostate cancer carrying the AR W742C mutation, with limited weight loss[8].
References:
[1] Moilanen A M, Riikonen R, Oksala R, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies[J]. Scientific reports, 2015, 5(1): 12007.
[2] Borgmann H, Lallous N, Ozistanbullu D, et al. Moving towards precision urologic oncology: targeting enzalutamide-resistant prostate cancer and mutated forms of the androgen receptor using the novel inhibitor darolutamide (ODM-201)[J]. European urology, 2018, 73(1): 4-8.
[3] Bastos D A, Antonarakis E S. Darolutamide for castration-resistant prostate cancer[J]. OncoTargets and therapy, 2019: 8769-8777.
[4] Yu J, Zhou P, Hu M, et al. Discovery and biological evaluation of darolutamide derivatives as inhibitors and down-regulators of wild-type AR and the mutants[J]. European journal of medicinal chemistry, 2019, 182: 111608.
[5] Gupta S, Pungsrinont T, Ženata O, et al. Interleukin-23 represses the level of cell senescence induced by the androgen receptor antagonists enzalutamide and darolutamide in castration-resistant prostate cancer cells[J]. Hormones and Cancer, 2020, 11(3): 182-190.
[6] Kuroiwa Y, Ito K, Nakayama J, et al. Analysis of the responsiveness to antiandrogens in multiple breast cancer cell lines[J]. Genes to Cells, 2024, 29(4): 301-315.
[7] Li B, Cheng B, Huang H, et al. Darolutamide-mediated phospholipid remodeling induces ferroptosis through the SREBP1-FASN axis in prostate cancer[J]. International journal of biological sciences, 2024, 20(12): 4635.
[8] Sugawara T, Baumgart S J, Nevedomskaya E, et al. Darolutamide is a potent androgen receptor antagonist with strong efficacy in prostate cancer models[J]. International journal of cancer, 2019, 145(5): 1382-1394.
| Cell experiment [1]: | |
Cell lines | LNCaP/AR cells |
Preparation Method | LNCaP/AR cells were cultured in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS) and 1% penicillin-streptomycin at 37℃ in the presence of 5% CO2. 2×104 cells per well were seeded in a 96-well plate for 24h, and were treated with different concentrations of ODM-201 (0.1, 1, 2, 4, 6, 8, and 10µM). After a 6-day incubation with ODM-201, cell viability was measured. |
Reaction Conditions | 0.1, 1, 2, 4, 6, 8, and 10µM; 6 days |
Applications | ODM-201 treatment significantly reduced the cell viability of LNCaP/AR cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male BALB/c nude mice |
Preparation Method | Male BALB/c nude mice (4-week-old) were housed in temperature (23±2°C) and light-controlled (12:12-hour light-dark cycle) animal care facility. Subcutaneously inject 2×106 LNCaP cells into mice. When the average tumor volume reached approximately 100mm3, the mice were intraperitoneally injected with ODM-201 (20mg/kg/day), RSL-3 (10mg/kg/day), or vehicle. The procedure was continued for 14 days. Mice were monitored daily, and the tumor volume was calculated using the following equation: volume=length×width2×1/2. |
Dosage form | 20mg/kg/day for 14 days; i.p. |
Applications | ODM-201 treatment inhibited the tumor growth in mice with LNCaP cell xenografts. |
References: | |
| Cas No. | 1297538-32-9 | SDF | |
| Synonyms | BAY 1841788 | ||
| Chemical Name | N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide | ||
| Canonical SMILES | N#CC1=C(Cl)C=C(C2=NN(C[C@H](C)NC(C3=NNC(C(O)C)=C3)=O)C=C2)C=C1 | ||
| Formula | C19H19ClN6O2 | M.Wt | 398.85 |
| Solubility | ≥ 19.95mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5072 mL | 12.536 mL | 25.0721 mL |
| 5 mM | 501.4 μL | 2.5072 mL | 5.0144 mL |
| 10 mM | 250.7 μL | 1.2536 mL | 2.5072 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)