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Chemical Structure| 1297538-32-9 Chemical Structure| 1297538-32-9
Chemical Structure| 1297538-32-9

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CAS No.: 1297538-32-9

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ODM-201 is a competitive inhibitor of androgen receptor with IC50 value of 26 nM and inhibits AR nuclear translocation with Ki value of 11 nM.

Synonyms: ODM-201; BAY-1841788; Nubeqa.

4.5 *For Research Use Only !

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Product Details of Darolutamide

CAS No. :1297538-32-9
Formula : C19H19ClN6O2
M.W : 398.85
SMILES Code : O=C(C1=NNC(C(O)C)=C1)N[C@@H](C)CN2N=C(C3=CC=C(C#N)C(Cl)=C3)C=C2
Synonyms :
ODM-201; BAY-1841788; Nubeqa.
MDL No. :MFCD29472270
InChI Key :BLIJXOOIHRSQRB-PXYINDEMSA-N
Pubchem ID :67171867

Safety of Darolutamide

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Androgen Receptor

    Androgen receptor, Ki:11 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
LNCaP cells 10 μM 24 hours Darolutamide significantly induces ferroptosis in AR+ PCa cells by downregulating SREBP1, which inhibits FASN transcription, thereby modulating phospholipid remodeling and inducing ferroptosis. PMC11414384
C4-2 cells 50 μM 24 hours Darolutamide significantly induces ferroptosis in AR+ PCa cells by downregulating SREBP1, which inhibits FASN transcription, thereby modulating phospholipid remodeling and inducing ferroptosis. PMC11414384
LNCaP cells 36.6 nM –37.5 μM 4 days Evaluate the synergistic antiproliferative activity of PSMA-TTC with darolutamide, showing synergistic effects (combination index of 0.47) PMC9401501
VCaP cells 36.6 nM –37.5 μM 4 days Evaluate the synergistic antiproliferative activity of PSMA-TTC with darolutamide, showing synergistic effects (combination index of 0.36) PMC9401501
C4-2 10-100 μM 48 hours To evaluate the effect of Darolutamide on prostate cancer cell sensitivity, results showed that downregulation of circRBM33 increased prostate cancer cell sensitivity to Darolutamide PMC10086746
22Rv1 10-100 μM 48 hours To evaluate the effect of Darolutamide on prostate cancer cell sensitivity, results showed that downregulation of circRBM33 increased prostate cancer cell sensitivity to Darolutamide PMC10086746
LNCaP cells 7.72 μM 6 days To evaluate the suppressive effect of darolutamide and radium-223 on LNCaP cell proliferation, showing moderate synergism. PMC11677307
LNCaP 5,260 ± 2,510 nM (IC50) 6 days To evaluate the effect of Darolutamide on prostate cancer cell viability. Results showed that Darolutamide significantly inhibited LNCaP cell viability. PMC6766977
LAPC-4 500 ± 220 nM (IC50) 6 days To evaluate the effect of Darolutamide on prostate cancer cell viability. Results showed that Darolutamide significantly inhibited LAPC-4 cell viability. PMC6766977
VCaP 410 ± 150 nM (IC50) 6 days To evaluate the effect of Darolutamide on prostate cancer cell viability. Results showed that Darolutamide significantly inhibited VCaP cell viability. PMC6766977
DU145 11.0 μM (IC 50) 72 hours To evaluate the in vitro efficacy of darolutamide against castration-resistant prostate cancer, showing DU145 cells were sensitive to darolutamide with an IC50 of 11.0 μM. PMC11711516
PC3 32.3 μM (IC 50) 72 hours To evaluate the in vitro efficacy of darolutamide against castration-resistant prostate cancer, showing PC3 cells were sensitive to darolutamide with an IC50 of 32.3 μM. PMC11711516
LNCaP 33.8 μM (IC 50) 72 hours To evaluate the in vitro efficacy of darolutamide against castration-resistant prostate cancer, showing LNCaP cells were sensitive to darolutamide with an IC50 of 33.8 μM. PMC11711516
22RV1 46.6 μM (IC 50) 72 hours To evaluate the in vitro efficacy of darolutamide against castration-resistant prostate cancer, showing 22RV1 cells were sensitive to darolutamide with an IC50 of 46.6 μM. PMC11711516
LAPC4 cells 500 nM (low) or 2 μM (high) 8 or 22 hours To characterize the effects of darolutamide on the PCa transcriptome, it was observed that darolutamide strongly antagonized genome-wide AR binding and inhibited androgen-dependent gene regulation. PMC7463324
VCaP cells 500 nM (low) or 2 μM (high) 8 or 22 hours To characterize the effects of darolutamide on the PCa transcriptome, it was observed that darolutamide strongly antagonized genome-wide AR binding and inhibited androgen-dependent gene regulation. PMC7463324
LAPC4 cells 500 nM or 2 μM 8 or 22 hours To study the impact of Darolutamide on the PCa transcriptome, it was found that Darolutamide significantly inhibited R1881-induced AR signaling and blocked AR-driven transcriptional signaling. PMC7463324
VCaP cells 500 nM or 2 μM 8 or 22 hours To study the impact of Darolutamide on the PCa transcriptome, it was found that Darolutamide significantly inhibited R1881-induced AR signaling and blocked AR-driven transcriptional signaling. PMC7463324

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
NOD.scid mice LNCaP prostate cancer bone metastasis model Oral (Darolutamide), Intravenous (Radium-223) 100 mg/kg Darolutamide twice daily for 41 days; Radium-223 every four weeks for two doses To evaluate the antitumor efficacy of darolutamide in combination with radium-223, showing significant reduction in serum PSA levels and tumor-induced abnormal bone formation. PMC11677307
CB17-Scid mice VCaP prostate cancer xenograft model Orally 100 mg/kg Twice daily for 23 days Evaluate the in vivo synergistic antitumor efficacy of PSMA-TTC with darolutamide, showing significant tumor growth inhibition (T/C values of 0.56 and 0.55) and increased PSMA expression PMC9401501
CB17-SCID male mice LAPC-4 cell line-derived xenograft model Oral 100 mg/kg (bi-daily) or 200 mg/kg (once daily) Once or twice daily for 56 days Evaluate the inhibitory effect of Darolutamide on tumor growth in the LAPC-4 xenograft model PMC6766977
CB17-SCID male mice LAPC-4 cell line-derived xenograft model Oral 100 mg/kg (bi-daily) or 200 mg/kg (once daily) Once or twice daily for 56 days To evaluate the effect of Darolutamide on tumor growth in the LAPC-4 xenograft model. Results showed that oral Darolutamide significantly inhibited tumor growth. PMC6766977
NOD.scid mice LNCaP prostate cancer bone metastasis model Oral (Darolutamide), Intravenous (Radium-223) 100 mg/kg (Darolutamide), 330 kBq/kg (Radium-223) Twice daily (Darolutamide), Every four weeks (Radium-223), for 41 days To evaluate the antitumor efficacy of darolutamide in combination with radium-223, showing significant reduction in serum PSA levels and tumor-induced abnormal bone formation. PMC11677307
NOD.scid mice LNCaP prostate cancer bone metastasis model Oral (Darolutamide), Intravenous (Radium-223) 100 mg/kg (Darolutamide), 330 kBq/kg (Radium-223) Darolutamide twice daily for 41 days; Radium-223 every four weeks for two doses To evaluate the antitumor efficacy of darolutamide in combination with radium-223, showing significant reduction in serum PSA levels and tumor-induced abnormal bone formation. PMC11677307
BALB/c nude mice Prostate cancer xenograft model Intraperitoneal injection 20 mg/kg Once daily for 14 days Combination therapy of darolutamide with ferroptosis inducers (RSL-3) significantly inhibited prostate cancer tumor growth by inducing ferroptosis through the SREBP1-FASN axis. PMC11414384
BALB/c nude mice Prostate cancer xenograft model Oral 50 mg/kg Once daily for 28 days To evaluate the effect of Darolutamide on prostate cancer xenograft model, results showed that downregulation of circRBM33 enhanced the antitumor activity of Darolutamide PMC10086746
Male athymic mice 22RV1-LUC xenograft model Oral gavage 50 mg/kg or 100 mg/kg Twice weekly for 6 weeks To evaluate the anti-tumor efficacy of ONC201 in combination with darolutamide in the 22RV1 CRPC xenograft model, demonstrating therapeutic effects. PMC11711516

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01429064 Prostate Cancer PHASE2 COMPLETED 2025-11-15 The Urology Center of Colorado... More >>, Wheat Ridge, Colorado, 80211, United States|Eastern CT Hematology and Oncology Associates, Norwich, Connecticut, 06360, United States|Cleveland Clinic, Cleveland, Ohio, 44195, United States|Carolina Urologic Research Center, Myrtle Beach, South Carolina, 29572, United States|Klinika onkologie a radioterapie LFUK a FN, Hradec Králové, Czech Republic|East-Tallinn Central Hospital, Tallinn, Estonia|Helsinki University Central Hospital, Helsinki, Finland|Kuopio University Hospital, Kuopio, Finland|Oulu University Hospital, Oulu, Finland|Tampere University Hospital, Tampere, Finland|Turku University Hospital, Turku, Finland|Saint Louis Hospital, Paris, France|Institut Gustave Roussy, Villejuif, France|Queen Elizabeth Hospital, Birmingham, United Kingdom|Velindre Cancer Centre, Cardiff, United Kingdom|Christie Hospital, Manchester, United Kingdom|Churchill Hospital, Oxford, United Kingdom Less <<
NCT01317641 Prostate Cancer PHASE1|PHASE2 COMPLETED 2025-07-13 The Urology Center of Colorado... More >>, Wheat Ridge, Colorado, 80211, United States|Eastern CT Hematology and Oncology Associates, Norwich, Connecticut, 06360, United States|Urology Health Team PLLC, Ocala, Florida, 34474, United States|Chesapeake Urology Research Associates, Baltimore, Maryland, 21327, United States|Delaware Valley urology, LLC, Voorhees, New Jersey, 08043, United States|Brooklyn Urology Research Group, Brooklyn, New York, 11215, United States|Cleveland Clinic, Cleveland, Ohio, 44195, United States|Carolina Urologic Research Center, Myrtle Beach, South Carolina, 29572, United States|Klinika onkologie a radioterapie LFUK a FN, Hradec Králové, Czech Republic|Fakultni Nemonicnice Olomouc, Olomouc, Czech Republic|Oddeleni Radiacni a Klinicke Onkologie Nemocnice Znojmo, Znojmo, Czech Republic|East-Tallinn Central Hospital, Talinn, Estonia|Helsinki University Central Hospital, Helsinki, Finland|Kuopio University Hospital, Kuopio, Finland|Oulu University Hospital, Oulu, Finland|Tampere University Hospital, Tampere, Finland|Turku University Hospital, Turku, Finland|Saint Louis Hospital, Paris, France|Institut Gustave Roussy, Villejuif, France|Queen Elizabeth Hospital, Birmingham, United Kingdom|Velindre Cancer Centre, Cardiff, United Kingdom|Christie Hospital, Manchester, United Kingdom|Churchill Hospital, Oxford, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.51mL

0.50mL

0.25mL

12.54mL

2.51mL

1.25mL

25.07mL

5.01mL

2.51mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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