Ketodarolutamide (Synonyms: BAY 1896953; ORM-15341)

Name: Ketodarolutamide
Brand: MedChemExpress
SKU: HY-19337
Rating: 5.0 (1 reviews)

Cat. No.: HY-19337 Purity: 98.72%: Data Sheet
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Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a K_i value of 8 nM for rat wild-type AR and an IC₅₀ value of 38 nM in AR-HEK293 cells. Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs. Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer.

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

Ketodarolutamide Chemical Structure

CAS No. : 1297537-33-7

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

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Ketodarolutamide:

Ketodarolutamide-d₃ Get quote
Ketodarolutamide-d₆ Get quote

1 Publications Citing Use of MCE Ketodarolutamide

•Int J Cancer. 2024 Jul 15;155(2):314-323.

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Biological Activity
Purity & Documentation
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Description

Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a K_i value of 8 nM for rat wild-type AR and an IC₅₀ value of 38 nM in AR-HEK293 cells^[1]. Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs^[1]. Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) ^[1]^[2]. Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer^[1]^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	> 30 μM Compound: 1c; ORM-15341	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]
LNCaP	IC₅₀	1.13 μM Compound: 1c; ORM-15341	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: 1c; ORM-15341	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

Ketodarolutamide (ORM-15341) (24 h) exhibits a K_i value of 8 nM for rat wild-type AR (wtAR) and an IC₅₀ value of 38 nM for human AR (hAR) in AR-HEK293 cells and shows IC₅₀ values of 51 nM, 1160 nM and 700 nM against mutant AR variants (F876L, W741L, T877A) in U2-OS cells^[1].
Ketodarolutamide (0.3 μM; 4 h) inhibits testosterone-induced nuclear translocation of AR in HS-HEK293 cells and LNCaP cells^[1].
Ketodarolutamide (10-10000 nM; 4 days) suppresses androgen-induced proliferation of VCaP cells more potently than Enzalutamide (HY-70002) and has no effect on the viability of AR-negative DU-145 prostate cancer cells and H1581 lung cancer cells, as determined by cell proliferation assay^[1].

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

Immunofluorescence^[1]

Cell Line:	HS-HEK293 cells
Concentration:	0.3 μM, 1 μM
Incubation Time:	4 h (HCS reader), 5 h (confocal imaging)
Result:	Inhibited testosterone-induced nuclear translocation of overexpressed AR.

Immunofluorescence^[1]

Cell Line:	HS-HEK293 cells
Concentration:	3 μM
Incubation Time:	4 h
Result:	Blocked testosterone-induced AR nuclear translocation.

Cell Viability Assay^[1]

Cell Line:	VCaP cells, DU-145 cells, H1581 cells
Concentration:	10 nM, 100 nM, 1000 nM, 10000 nM (increasing concentration gradient)
Incubation Time:	4 days
Result:	Suppressed androgen-induced cell proliferation more potently than enzalutamide. Had no effect on the viability of AR-negative cells.

Parmacokinetics

Species	Dose	Route	AUC_0-∞	C₀	T_1/2
Mice^[2]	1 mg/kg	i.v.	4636 ng·h/mL	1372 ng/mL	2.70 h

In Vivo

Ketodarolutamide (ORM-15341) (metabolized from oral administration of ODM-201 (HY-16985) ) (50 mg/kg; oral administration; once or twice a day; for 37 days) exhibits potent antitumor activity in castrated male BALB/c nude mice bearing subcutaneous VCaP xenografts^[1].
Ketodarolutamide (metabolized from oral administration of ODM-201) (50 mg/kg; oral administration; twice a day; for 3 weeks) does not increase serum testosterone levels in intact nude mice bearing orthotopic VCaP tumors^[1].
Ketodarolutamide (metabolized from oral administration of ODM-201) (25, 50, 100 mg/kg; oral administration; twice a day; for 7 days) shows negligible blood-brain barrier penetration with a brain/plasma ratio of 1.9-2.8% in mice^[1].

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

Molecular Weight

396.83

Formula

C₁₉H₁₇ClN₆O₂

CAS No.

1297537-33-7

Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(C#N)C=CC(C2=NN(C[C@H](C)NC(C3=NNC(C(C)=O)=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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (252.00 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	2.5200 mL	12.5999 mL	25.1997 mL
5 mM	0.5040 mL	2.5200 mL	5.0399 mL
10 mM	0.2520 mL	1.2600 mL	2.5200 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 2.5 mg/mL (6.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (6.30 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: 98.72%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (247 KB) LCMS (87 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]

[2]. Sulochana SP, et al. Validation of an LC-MS/MS method for simultaneous quantitation of enzalutamide, N-desmethylenzalutamide, apalutamide, darolutamide and ORM-15341 in mice plasma and its application to a mice pharmacokinetic study. J Pharm Biomed Anal. 2018 Jul 15;156:170-180. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.5200 mL	12.5999 mL	25.1997 mL	62.9993 mL
	5 mM	0.5040 mL	2.5200 mL	5.0399 mL	12.5999 mL
	10 mM	0.2520 mL	1.2600 mL	2.5200 mL	6.2999 mL
	15 mM	0.1680 mL	0.8400 mL	1.6800 mL	4.2000 mL
	20 mM	0.1260 mL	0.6300 mL	1.2600 mL	3.1500 mL
	25 mM	0.1008 mL	0.5040 mL	1.0080 mL	2.5200 mL
	30 mM	0.0840 mL	0.4200 mL	0.8400 mL	2.1000 mL
	40 mM	0.0630 mL	0.3150 mL	0.6300 mL	1.5750 mL
	50 mM	0.0504 mL	0.2520 mL	0.5040 mL	1.2600 mL
	60 mM	0.0420 mL	0.2100 mL	0.4200 mL	1.0500 mL
	80 mM	0.0315 mL	0.1575 mL	0.3150 mL	0.7875 mL
	100 mM	0.0252 mL	0.1260 mL	0.2520 mL	0.6300 mL

Ketodarolutamide 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.

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Ketodarolutamide (Synonyms: BAY 1896953; ORM-15341)

Customer Review

Other Forms of Ketodarolutamide:

Ketodarolutamide Related Antibodies

1 Publications Citing Use of MCE Ketodarolutamide

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Ketodarolutamide Related Antibodies

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Complete Stock Solution Preparation Table

Ketodarolutamide Related Classifications

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