Darolutamide (Synonyms: ODM-201; BAY-1841788)

Name: Darolutamide
Brand: MedChemExpress
SKU: HY-16985
Rating: 5.0 (5 reviews)

Cat. No.: HY-16985 Purity: 99.30%: FAQs
Data Sheet SDS COA Handling Instructions

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Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC₅₀ of 26 nM in in vitro assay.

For research use only. We do not sell to patients.

Darolutamide Chemical Structure

CAS No. : 1297538-32-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 145	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 145	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 209	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 690	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 5 publication(s) in Google Scholar

Other Forms of Darolutamide:

Darolutamide (Standard) Get quote

5 Publications Citing Use of MCE Darolutamide

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Protocol
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Description

Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC₅₀ of 26 nM in in vitro assay.

IC₅₀ & Target

IC50: 26 nM (AR-HEK293 cells, AR)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	> 30 μM Compound: 1a; ODM-201	Antiproliferative activity against human 22Rv1 expressing AR assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Antiproliferative activity against human 22Rv1 expressing AR assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 31437779]
L02	IC₅₀	> 30 μM Compound: 1a; ODM-201	Cytotoxicity against human L02 assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Cytotoxicity against human L02 assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 31437779]
LNCaP	IC₅₀	1.65 μM Compound: 1a; ODM-201	Antiproliferative activity against human LNCAP expressing AR assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Antiproliferative activity against human LNCAP expressing AR assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 31437779]
PC-3	IC₅₀	> 30 μM Compound: 1a; ODM-201	Cytotoxicity against human PC3 assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Cytotoxicity against human PC3 assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 31437779]

In Vitro

In competitive AR binding assays, the inhibition constant (Ki) values of Darolutamide (ODM-201) are 11 nM. ODM-201and ORM-15341 suppresse androgen-induced cell proliferation more efficaciously than ARN-509, IC50 values being 230 and 170 nM for Darolutamide and ORM-15341 vs. 420 nM for ARN-509. Darolutamide has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells confirming that the antiproliferative properties of Darolutamide and ORM-15341 are specific to AR-dependent PC cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

398.85

Formula

C₁₉H₁₉ClN₆O₂

CAS No.

1297538-32-9

Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(C#N)C=CC(C2=NN(C[C@H](C)NC(C3=NNC(C(O)C)=C3)=O)C=C2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (250.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5072 mL	12.5360 mL	25.0721 mL
5 mM	0.5014 mL	2.5072 mL	5.0144 mL
10 mM	0.2507 mL	1.2536 mL	2.5072 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.30%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (248 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Moilanen AM, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms toandrogen signaling-directed prostate cancer therapies. Sci Rep. 2015 Jul 3;5:12007. doi: 10.1038/srep12007. [Content Brief]

Cell Assay ^[1]	To study the antiproliferative properties of Darolutamide and ORM-15341, the VCaP cell line originally derived from a bone metastasis of a CRPC patient is used. The VCaP cell line is characterized with endogenous AR gene amplification and AR overexpression30, typical for CRPC. VCaP cells are cultured in RPMI-1640 medium and supplemented with 10% fetal bovine serum (FBS), 100 UI/mL penicillin, 100 μ g/mL streptomycin, and 4 mM VCaP^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	To elucidate the in vivo efficacy of Darolutamide in a CRPC mouse model, castrated male nude mice with subcutaneously injected VCaP cells are treated orally with ODM-201 (50 mg/kg) once (qd) or twice daily (bid), or with enzalutamide (20 mg/kg, qd) for 37 days. The dose for enzalutamide is selected based on previously published studies9 and our pharmacokinetic (PK) analyses which reveales that in mice the systemic exposure (AUC0–24) for this dose of enzalutamide is 2.5 times higher than that for Darolutamide (50 mg/kg, bid). Moreover, enzalutamide exhibited a long plasma half-life (18.3 hours) while the half-life of Darolutamide in mice is not optimal (1.6 hours) supporting once daily dosing for enzalutamide and higher dose and more frequent dosing for ODM-201^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Moilanen AM, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms toandrogen signaling-directed prostate cancer therapies. Sci Rep. 2015 Jul 3;5:12007. doi: 10.1038/srep12007. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5072 mL	12.5360 mL	25.0721 mL	62.6802 mL
	5 mM	0.5014 mL	2.5072 mL	5.0144 mL	12.5360 mL
	10 mM	0.2507 mL	1.2536 mL	2.5072 mL	6.2680 mL
	15 mM	0.1671 mL	0.8357 mL	1.6715 mL	4.1787 mL
	20 mM	0.1254 mL	0.6268 mL	1.2536 mL	3.1340 mL
	25 mM	0.1003 mL	0.5014 mL	1.0029 mL	2.5072 mL
	30 mM	0.0836 mL	0.4179 mL	0.8357 mL	2.0893 mL
	40 mM	0.0627 mL	0.3134 mL	0.6268 mL	1.5670 mL
	50 mM	0.0501 mL	0.2507 mL	0.5014 mL	1.2536 mL
	60 mM	0.0418 mL	0.2089 mL	0.4179 mL	1.0447 mL
	80 mM	0.0313 mL	0.1567 mL	0.3134 mL	0.7835 mL
	100 mM	0.0251 mL	0.1254 mL	0.2507 mL	0.6268 mL

Darolutamide Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Darolutamide1297538-32-9ODM-201 BAY-1841788ODM201ODM 201BAY1841788BAY 1841788BAY-1841788Androgen ReceptorInhibitorinhibitorinhibit

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Darolutamide (Synonyms: ODM-201; BAY-1841788)

Customer Review

Other Forms of Darolutamide:

Darolutamide Related Antibodies

5 Publications Citing Use of MCE Darolutamide

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Darolutamide Related Antibodies

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Complete Stock Solution Preparation Table

Darolutamide Related Classifications

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