ODM-201
- Product Name
- ODM-201
- CAS No.
- 1297538-32-9
- Chemical Name
- ODM-201
- Synonyms
- Darolutamide;BAY-1841788;0DM021;ODM-201;ODM-021;ODM 021;CS-1565;Darotaxime;Darolutamid;Darrolumide
- CBNumber
- CB43052901
- Molecular Formula
- C19H19ClN6O2
- Formula Weight
- 398.85
- MOL File
- 1297538-32-9.mol
ODM-201 Property
- Melting point:
- 169 - 171°C
- Boiling point:
- 719.5±60.0 °C(Predicted)
- Density
- 1.41±0.1 g/cm3(Predicted)
- storage temp.
- -20°C Freezer, Under inert atmosphere
- solubility
- DMSO (Slightly), Methanol (Slightly)
- pka
- 11.10±0.10(Predicted)
- form
- Solid
- color
- White to Off-White
- InChIKey
- BLIJXOOIHRSQRB-PXYINDEMSA-N
- SMILES
- N1C(C(O)C)=CC(C(N[C@@H](C)CN2C=CC(C3=CC=C(C#N)C(Cl)=C3)=N2)=O)=N1
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H400Very toxic to aquatic life
H410Very toxic to aquatic life with long lasting effects
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P273Avoid release to the environment.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P330Rinse mouth.
P391Collect spillage. Hazardous to the aquatic environment
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 25643
- Product name
- ODM-201
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 25643
- Product name
- ODM-201
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $172
- Updated
- 2024/03/01
- Product number
- 25643
- Product name
- ODM-201
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $321
- Updated
- 2024/03/01
- Product number
- 25643
- Product name
- ODM-201
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $692
- Updated
- 2024/03/01
- Product number
- O006500
- Product name
- ODM-201
- Packaging
- 100mg
- Price
- $1890
- Updated
- 2021/12/16
ODM-201 Chemical Properties,Usage,Production
Description
ODM-201 is an androgen receptor (AR) antagonist (Ki = 11 nM). It inhibits AR transactivation in U2OS osteosarcoma cells expressing human wild-type and mutant ARs (IC50s = 65, 66, 1,500, and 1,782 nM for wild-type, ARF876L, ARW741L, and ART877A, respectively). ODM-201 prevents androgen-induced AR nuclear translocation in AR-overexpressing HS-HEK293 and LNCaP cells and suppresses androgen-induced proliferation of VCaP cells (IC50 = 230 nM). In vivo, ODM-201 (50 mg/kg per day) reduces tumor growth in a VCaP castrated mouse xenograft model. It also inhibits tumor growth without increasing serum testosterone levels in a VCaP intact mouse xenograft model.
Description
ODM-201 is a novel androgen receptor (AR) inhibit designed to inhibit the growth of prostate cancer cells through binding to the AR to inhibit the testosterone-induced AR nuclear translocation. It is particularly used in patients with progressive metastatic castration-resistant prostate cancer. It is effective in inhibiting the activity of some mutant ARs emerging during antiandrogen therapies, including the F876L mutation version which is resistant to enzalutamide and ARN-509 (the second-generation antiandrogens).Therefore, it has potential to overcome the resistance issue occurring upon AR-targeted therapies.
Uses
ODM-201 is a compound being used as a novel next-generation androgen receptor-directed therapy for prostate cancer.
Biological Activity
As a ligand-dependent transcription factor, androgen receptor(AR) controls the expression of multiple genes involved in cell growth and survival. Darolutamide is able to inhibit multiple AR variants that confer resistance to first-generation antagonists.
Synthesis
Synthesis of Darolutamide
in vivo
Darolutamide (ODM-201) showes a significant antitumor activity with both doses, 50 mg/kg twice daily being more efficacious compared to castrated, untreated mice (p<0.001), which also showes inhibition of tumor growth (p<0.05) vs. castrated, untreated mice. Further, there is no sign of treatment-related toxicities; the body weights of mice treated with Darolutamide twice daily do not decrease significantly during the treatment[1].
References
Moilanen, Anu Maarit, et al. "Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies." Sci Rep 5.2(2015):12007. Fizazi, Karim, et al. "ODM-201, a new generation androgen receptor inhibitor for castration-resistant prostate cancer: Preclinical and phase I data." Genitourinary Cancers Symposium of the Conquer-Cancer-Foundation of 2013. Fizazi, K, et al. "Activity and safety of ODM-201 in patients with progressive metastatic castration-resistant prostate cancer (ARADES): an open-label phase 1 dose-escalation and randomised phase 2 dose expansion trial." Lancet Oncology 5.9(2014):975-85.
ODM-201 Preparation Products And Raw materials
Raw materials
Preparation Products
ODM-201 Suppliers
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- +86-19182167371 +86-19182167371;
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- China
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View Lastest Price from ODM-201 manufacturers
- Product
- Darolutamide 1297538-32-9
- Price
- US $0.00-0.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 500kg
- Release date
- 2025-10-16
- Product
- ODM-201 1297538-32-9
- Price
- US $1000.00-400.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 5000
- Release date
- 2024-08-12
- Product
- ODM-201 1297538-32-9
- Price
- US $40.00-35.00/Gram
- Min. Order
- 1Gram
- Purity
- 99.99%
- Supply Ability
- 50Tons
- Release date
- 2023-04-11