Darolutamide NEW

$0.00 1KG

$0.00 5KG

$0.00 10KG

Min. Order1KG
Purity99%
Cas No1297538-32-9
Supply Ability500kg
Update time2025-10-22

Shandong Hanjiang Chemical Co., Ltd

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China

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Chemical Properties

Product Name	Darolutamide
CAS No	1297538-32-9
EC-No
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 (K_i = 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, AR^F876L, AR^W741L, and AR^T877A, 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