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Darolutamide - 99%, high purity , Androgen Receptor antagonist, CAS No.1297538-32-9, Androgen Receptor antagonist

COA COA
In stock
Item Number
D413782
Grouped product items
SKU Size
Availability
 Price Qty
D413782-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$129.90
D413782-10mg
10mg
3
$205.90
D413782-50mg
50mg
3
$489.90
D413782-100mg
100mg
2
$924.90
D413782-250mg
250mg
3
$2,081.90
Wish List
Bulk Order  SDS  DATASHEET  Specification Sheet

Androgen Receptor Antagonists

View related series
Androgen Receptor (133) Androgen receptor Antagonist (15) Vitamin D Related/Nuclear Receptor (907)

Basic Description

Synonyms example 56 [US9657003] | N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-3-(1-hydroxyethyl)-1H-pyrazole-5-carboxamide | N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)propan-2-yl)-3-(1-hydroxyethyl)-1H-pyrazole-5-carboxamide | N-(
Specifications & Purity Moligand™, ≥99%
Biochemical and Physiological Mechanisms Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type ANTAGONIST
Mechanism of action Androgen Receptor antagonist
Product Description

Information

Darolutamide (ODM-201) Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K i of 11 nM. Phase 3.


Targets

Androgen receptor 11 nM(Ki)


In vitro

In AR-HEK293 cells stably expressing full-length hAR, ODM-201 inhibits human AR (hAR) with IC50 of 26 nM. ODM-201 inhibits VCaP cell proliferation with IC50 of 230 nM, while has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells.


In vivo

In mice bearing VCaP xenografts, ODM-201 (50\u2009mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth.


Cell Research(from reference)

Cell lines：DU-145, H1581, and VCaP cells 

Concentrations：~10 μM 

Incubation Time：4 days 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Azoles
Subclass Pyrazoles
Intermediate Tree Nodes Not available
Direct Parent Phenylpyrazoles
Alternative Parents Pyrazole-5-carboxamides  Benzonitriles  2-heteroaryl carboxamides  Chlorobenzenes  Aryl chlorides  Heteroaromatic compounds  Secondary carboxylic acid amides  Secondary alcohols  Nitriles  Azacyclic compounds  Organochlorides  Organic oxides  Hydrocarbon derivatives  Aromatic alcohols  
Molecular Framework Aromatic heteromonocyclic compounds
Substituents Phenylpyrazole - 2-heteroaryl carboxamide - Benzonitrile - Pyrazole-5-carboxamide - Chlorobenzene - Halobenzene - Aryl chloride - Aryl halide - Monocyclic benzene moiety - Benzenoid - Heteroaromatic compound - Carboxamide group - Secondary carboxylic acid amide - Secondary alcohol - Carboxylic acid derivative - Azacycle - Carbonitrile - Nitrile - Organic oxygen compound - Organic nitrogen compound - Aromatic alcohol - Alcohol - Hydrocarbon derivative - Organic oxide - Cyanide - Organohalogen compound - Organochloride - Organonitrogen compound - Organooxygen compound - Aromatic heteromonocyclic compound
Description This compound belongs to the class of organic compounds known as phenylpyrazoles. These are compounds containing a phenylpyrazole skeleton, which consists of a pyrazole bound to a phenyl group.
External Descriptors Not available

Product Properties

ALogP 3.034
hba_count 3
HBD Count 3
Rotatable Bond 6

Associated Targets(Human)

AR Tclin Androgen receptor (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
AR Tclin Androgen Receptor (11781 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PC-3 (62116 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LNCaP (8286 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CWR22R (2180 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
L02 (4864 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
VCaP (1078 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 504771879
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504771879
IUPAC Name N-[(2S)-1-[3-(3-chloro-4-cyanophenyl)pyrazol-1-yl]propan-2-yl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide
INCHI InChI=1S/C19H19ClN6O2/c1-11(22-19(28)18-8-17(12(2)27)23-24-18)10-26-6-5-16(25-26)13-3-4-14(9-21)15(20)7-13/h3-8,11-12,27H,10H2,1-2H3,(H,22,28)(H,23,24)/t11-,12?/m0/s1
InChIKey BLIJXOOIHRSQRB-PXYINDEMSA-N
Smiles CC(CN1C=CC(=N1)C2=CC(=C(C=C2)C#N)Cl)NC(=O)C3=NNC(=C3)C(C)O
Isomeric SMILES C[C@@H](CN1C=CC(=N1)C2=CC(=C(C=C2)C#N)Cl)NC(=O)C3=NNC(=C3)C(C)O
Molecular Weight 398.85
Reaxy-Rn 23068895
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23068895&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

4 results found

Lot Number Certificate Type Date Item
H2229239 Certificate of Analysis Jun 09, 2025 D413782
H2229238 Certificate of Analysis Jun 09, 2025 D413782
H2229237 Certificate of Analysis Jun 09, 2025 D413782
H2229236 Certificate of Analysis Jun 09, 2025 D413782

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 80 mg/mL (200.57 mM); Ethanol: 38 mg/mL warmed with 50ºC Water: bath (95.27 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility 80
DMSO(mM) Max Solubility 200.5766579
Water(mg / mL) Max Solubility ＜1
Molecular Weight 398.800 g/mol
XLogP3 1.800
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 5
Rotatable Bond Count 6
Exact Mass 398.126 Da
Monoisotopic Mass 398.126 Da
Topological Polar Surface Area 120.000 Ų
Heavy Atom Count 28
Formal Charge 0
Complexity 598.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 1
Undefined Atom Stereocenter Count 1
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

Reviews

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