Product Details
| Product Name: Darolutamide | CAS No.: 1297538-32-9 |
| Min. Order: 1KG | Purity: 99% |
| Supply Ability: 500kg | Release date: 2025/10/22 |
| Product Name: | ODM-201 |
| Synonyms: | CS-1565;ODM-201(Darolutamide);N-{(2S)-1-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]propan-2-yl}-5-[(1RS)-1-hydroxyethyl]-1H-pyrazole-3-carboxamide;0DM021;BAY-1841788;ODM-021;0DM021;ODM 021;ODM 021;ODM-021;ODM-201 |
| CAS: | 1297538-32-9 |
| MF: | C19H19ClN6O2 |
| MW: | 398.85 |
| EINECS: | 829-313-8 |
| Product Categories: | API |
| Mol File: | 1297538-32-9.mol |
 | |
| ODM-201 Chemical Properties |
| 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 |
| Safety Information |
| MSDS Information |
| ODM-201 Usage And Synthesis |
| 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. |
| 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. |
| 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 | 4-Acetyl-2-chlorobenzonitrile-->(S)-4-(1-(2-aminopropyl)-1H-pyrazol-3-yl)-2-chlorobenzonitrile-->5-(1-Hydroxyethyl)-1H-pyrazole-3-carboxylic acid-->2-chloro-4-(1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-5-yl)benzonitrile-->2-Chloro-4-(1H-Pyrazol-5-Yl)Benzonitrile-->ORM-15341-->4-Bromo-2-chlorobenzonitrile-->Ethanol-->Sodium borohydride |
Company Profile Introduction
Shandong Hanjiang Chemical Co., Ltd. is located in Zibo City, Shandong Province, China.
It is a biotechnology enterprise engaged in the R&D, production and sales of drugs, steroids, peptides, raw materials, vitamins, food additives, animal and plant extracts, cosmetics, pharmaceutical raw materials and intermediates. The company has complete experimental facilities. Advanced testing instruments ensure the stability of product quality from all aspects. The company has a complete sales service system, and its products are exported to countries all over the world. It has won a good international reputation for its excellent quality and excellent service. The company has been adhering to the basic principles of "integrity, quality, service, and win-win" to serve customers, and constantly strict requirements,
Advantages:
1. Samples are provided for test;
2. Good quality products;
3. 100% secure delivery.
4. secure your money, lower the risk
Payment ways: Western Union, Moneygram, Bitcoin, T/T
Delivery: EMS/ EUB/ USPS/ UPS/ TNT/ FEDEX/ DHL etc
Packaging:safe and discreet packaging
Our company Superiority
1 Best service, high quality and reasonable price
2. It's customers' right to choose the package (EMS, DHL, FedEx, UPS);
3. It's customers' right to choose the packing way for his products from many recent effective packing ways
4. Specials are possible when client's order is big enough, including the discount policy;
5.Our company promise to deliver clients' package to his hands safely, or we'll cover the total loss and reship in time;
Our company supply high quality chemical products with the most competitive prices.
If have any need or question, contact us freely.
Hope we can have chances to build good long-term cooperation.
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