ODM-201 Darolutamide CAS 1297538-32-9 high purity androgen receptor antagonist raw powder for research

ODM-201 Darolutamide CAS 1297538-32-9 99% High-Purity Powder BAY-1841788 Potent Non-Steroidal Androgen Receptor Antagonist Prostate Cancer Anti-Tumor Research Reagent

Premium 99% ODM-201 Darolutamide crystalline powder CAS 1297538-32-9, high-selectivity non-steroidal androgen receptor antagonist. Ideal for castration-resistant prostate cancer anti-tumor pharmacological research.
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ODM-201 / Darolutamide (CAS 1297538-32-9) AR Antagonist | Blocks AR Nuclear Translocation, Prostate-Cancer Research Compound

ODM-201 (Darolutamide) CAS 1297538-32-9
Next-Generation Androgen-Receptor Antagonist (BAY-1841788)

ODM-201 (darolutamide; CAS 1297538-32-9), also BAY-1841788, is a next-generation, non-steroidal androgen-receptor (AR) antagonist that blocks AR nuclear translocation with Ki 11 nM and inhibits hAR transcription (IC50 26 nM). Molecular formula C19H19ClN6O2, MW 398.85. Research-grade with COA.

AR Antagonist ODM-201 Darolutamide Prostate Cancer nmCRPC Non-Steroidal Antiandrogen Androgen Receptor
Request a Quote Technical Specs
398.85
MW (C19H19ClN6O2)
11 nM
AR Ki
Low CNS
Minimal brain penetration

Molecular Information

Name: ODM-201 (Darolutamide)
CAS: 1297538-32-9
Formula: C19H19ClN6O2
MW: 398.85 g/mol
Class: Non-steroidal AR antagonist
Core: N-[(2R)-2-methyl-4-(6-cyano-3-trifluoromethyl-phenylamino)-2-oxo-1,2,3,4-tetrahydro-quinolin-7-yl]-acetamide (approx.)
Target: Androgen Receptor (AR)
Ki: 11 nM (rAR)
IC50: 26 nM (hAR)
Appearance: White to off-white powder
Synonyms: Darolutamide / BAY-1841788
Storage: -20 C
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CAS Number
1297538-32-9
⚖️
Molecular Weight
398.85
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Primary Activity
AR Antagonist
✅
Purity
≥98%

Product Technical Specifications

Complete physicochemical properties and QC parameters for ODM-201 (Darolutamide) (CAS 1297538-32-9)

📋 Physicochemical Properties

  • Product NameODM-201 (Darolutamide)
  • IUPAC CoreN-[(2R)-2-methyl-4-[[6-cyano-3-(trifluoromethyl)phenyl]amino]-2-oxo-1,2,3,4-tetrahydroquinolin-7-yl]acetamide
  • CAS Number1297538-32-9
  • SynonymsDarolutamide; BAY-1841788; ODM-021
  • Molecular FormulaC19H19ClN6O2
  • Molecular Weight398.85 g/mol
  • SourceSynthetic small molecule (Orion / Bayer)
  • AppearanceWhite to off-white powder
  • Melting PointNot reported
  • Water SolubilityInsoluble
  • Organic SolubilityDMSO ~80 mg/mL; ethanol
  • Compound ClassNon-steroidal androgen-receptor antagonist
  • HS Code2934.99

🔬 Quality Control & Handling

  • Purity (HPLC)≥98%
  • FormSolid powder
  • Primary TargetAndrogen receptor (AR / NR3C4)
  • Pathway ReadoutBlocked AR nuclear translocation; ↓ AR transcription / VCaP proliferation
  • SelectivityNon-steroidal AR antagonist; low blood-brain-barrier penetration
  • Storage Condition-20 C, sealed, protect from light
  • Solution StabilityAliquot DMSO stocks; avoid freeze-thaw
  • ShippingBlue ice / cold chain recommended
  • QC DocumentationCOA / HPLC / NMR / MS / MSDS
  • Pack Sizes1g / 5g / 10g / 100g / 1KG
  • Stock StatusIn Stock
  • Use StatementResearch use only; not for human/clinical use

Key Molecular Targets & Pathway Nodes

ODM-201 is a highly selective androgen-receptor antagonist; its distinctive mechanism is blocking AR nuclear translocation, and its low brain penetration sets it apart from older antiandrogens.

🧬 Androgen Receptor (AR) 🔗 Testosterone / DHT 🧱 AR Nuclear Translocation 🧱 Androgen-Response Elements 🧱 VCaP / LNCaP (AR+) cells 🧱 AR Mutants (resistant) 🧠 Blood-Brain Barrier (low) 🧬 Prostate Epithelium 🧪 AR Co-activators 🔬 Steroid-Receptor Family 🧫 AR-Negative Controls (DU-145) ⚡ Tumor Proliferation

How ODM-201 Works: Locking the Androgen Receptor Out of the Nucleus

ODM-ish? ODM-201 competitively occupies AR and prevents its testosterone-induced nuclear translocation and gene transcription — including against resistant AR mutants

1

Competitive AR Occupation

ODM-201 is a non-steroidal androgen-receptor antagonist that competitively binds AR (Ki 11 nM for rat AR; IC50 26 nM for human AR-mediated transcription), preventing testosterone/DHT from activating the receptor.

2

Blocked Nuclear Translocation

Crucially, ODM-201 blocks testosterone-induced AR nuclear translocation. The receptor cannot enter the nucleus, so it cannot bind androgen-response elements or drive proliferation genes in AR-dependent cells (e.g., VCaP).

3

Activity Against Resistant AR & Low CNS Penetration

ODM-201's active metabolite retains full antagonistic activity against AR mutants, relevant to castration-resistant prostate cancer. Its limited blood-brain-barrier crossing reduces central-nervous-system side effects versus earlier antiandrogens.

⚖️ ODM-201 vs Enzalutamide vs Bicalutamide

  • ODM-201 (this product)Blocks AR nuclear translocation; Ki 11 nM; low CNS penetration
  • EnzalutamideAR antagonist + blocks translocation; higher CNS penetration
  • BicalutamideOlder AR antagonist; variable CNS/ cardiac effects
  • Shared TargetAndrogen receptor (AR)
  • Key DistinctionODM-201 minimal brain penetration
  • ResistanceActive metabolite hits AR mutants

♻️ Downstream Biological Consequences

  • ReceptorAR occupied, locked cytosolic
  • TranslocationAR nuclear entry ↓
  • TranscriptionAndrogen-response genes ↓
  • ProliferationAR+ tumor growth ↓ (VCaP)
  • ResistanceActive against AR mutants
  • CNSMinimal neuropsychiatric effect (low BBB)

Research Applications & Models

A next-generation AR antagonist for prostate-cancer and endocrine-oncology research, valued for clean mechanism and low CNS burden.

🧬

Prostate-Cancer (CRPC) Models

The flagship use: ODM-201 inhibits AR nuclear translocation and VCaP proliferation in castration-resistant prostate-cancer models; benchmarked in AR-dependent oncology.

AR / CRPC
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Androgen-Receptor Research

A fiducial AR antagonist for binding (Ki), translocation and transcription-reporter assays; contrasts enzalutamide/bicalutamide.

AR / NR3C4
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AR-Mutant & Resistance Studies

Used to probe activity against resistant AR mutants via its active metabolite in engineered cell lines.

AR mutants
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CNS-Penetration Comparison

Studied for low blood-brain-barrier crossing versus enzalutamide, informing neurotoxicity research.

BBB / CNS
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Antiandrogen Panel

Benchmarked head-to-head with enzalutamide and bicalutamide in AR-positive and AR-negative (DU-145) controls.

AR panel
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Steroid-Receptor Selectivity

Profiled for minimal cross-talk with other steroid/nuclear receptors.

Receptor selectivity

Key Literature & Landmark Publications

The discovery, mechanism and clinical validation of darolutamide (ODM-201).

Fizazi K, et al. Nonmetastatic, castration-resistant prostate cancer and survival with darolutamide. N Engl J Med. 2019;381(1):13-24. (ARAMIS).
doi: 10.1056/NEJMoa1815671
Moilanen AM, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor. (Preclinical profile).
Landmark reference
Selleck / MCE profile: ODM-201 blocks AR nuclear translocation, Ki 11 nM, IC50 26 nM (hAR); VCaP IC50 230 nM.
Landmark reference
Clinical reference: darolutamide in non-metastatic CRPC (phase 3 ARAMIS).
Landmark reference
Structural / receptor-occupancy studies of ODM-201 AR antagonism.
Landmark reference

Available Sizes & Ordering

Research-grade ODM-201 / Darolutamide (CAS 1297538-32-9) with full QC documentation; standard packs and bulk custom quantities supported.

TierPack SizeStock StatusSuitable ForLead Time
Standard1gIn StockAR binding & translocation assaysCold chain
Medium5gIn StockProstate-cancer & AR modelsCold chain
Large10gIn StockLong-term in vivo & formulation studiesCold chain
Bulk100gIn StockFormulation & process developmentQuote to confirm
Industrial1KGMade to orderPilot/production scale, CMO supplyBatch delivery

💡 Reference sizes shown above; for exact pricing and availability please contact us for a quote. Bulk orders qualify for tiered discounts.

Frequently Asked Questions (FAQ)

What is ODM-201 (darolutamide) and what does it do?
ODM-201, also called darolutamide or BAY-1841788 (CAS 1297538-32-9), is a next-generation, non-steroidal androgen-receptor (AR) antagonist. It blocks AR nuclear translocation with Ki 11 nM and inhibits human AR transcription with IC50 26 nM; its active metabolite stays active against AR mutants. Formula C19H19ClN6O2, MW 398.85.
How is ODM-201 different from enzalutamide or bicalutamide?
All three block AR, but ODM-201 uniquely minimizes blood-brain-barrier penetration, reducing central-nervous-system side effects seen with enzalutamide. It also retains activity via its metabolite against resistant AR mutants, a key advantage in castration-resistant prostate cancer.
What is the mechanism in prostate cancer?
Testosterone/DHT normally drive AR into the nucleus to switch on proliferation genes in AR-dependent tumor cells (e.g., VCaP). ODM-201 competitively occupies AR and prevents its nuclear translocation, so androgen-response transcription is shut off and tumor-cell proliferation falls — including against AR mutants.
What are the key experimental readouts?
Readouts include AR-binding Ki, AR nuclear-translocation imaging, androgen-response-reporter (luciferase/PSA) activity, and VCaP proliferation (IC50 ~230 nM), with AR-negative DU-145 as a specificity control.
How soluble is ODM-201 and how prepared?
ODM-201 is soluble in DMSO (~80 mg/mL) and ethanol, but insoluble in water. For cell assays dilute DMSO stock into medium (final DMSO <=0.1% v/v); for in vivo use CMC-Na suspensions or validated vehicles. Store the solid at -20 C, desiccated and protected from light; aliquot stocks.
Is QC documentation provided?
Every batch ships with a Certificate of Analysis (COA) including HPLC purity, NMR structural confirmation and MS data. MSDS/SDS and Certificates of Origin are available on request. Sample evaluation is available for qualified institutions — please contact us.

Need ODM-201 / Darolutamide (AR Antagonist) for Your Research?

Research-grade ODM-201 / Darolutamide (CAS 1297538-32-9) — purity ≥98% HPLC, COA included
The next-gen AR antagonist that blocks nuclear translocation with low CNS penetration — request a quote today

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