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Ketodarolutamide

CAT: 0804-HY-19337-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-19337-01Size:5 mg
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Description
Ketodarolutamide (ORM-15341) is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct. IC50 value: 38 nM Target: androgen receptor in vitro: In competitive AR binding assays, the inhibition constant (Ki) values of Ketodarolutamide (ORM-15341) was 8 nM. Ketodarolutamide (ORM-15341) functions as a full antagonist for all tested mutant ARs , with IC50 of 25, 51, 700, and 1160 nM for wtAR, AR (F876L), AR (T877A), and AR (W741L) .
CAS Number
1297537-33-7
Product Name Alternative
BAY 1896953; ORM-15341
UNSPSC
12352005
Target
Androgen Receptor
Type
Reference compound
Related Pathways
Vitamin D Related/Nuclear Receptor
Field of Research
Endocrinology
Assay Protocol
https://www.medchemexpress.com/ORM-15341.html
Purity
98.72
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
ClC1=C(C#N)C=CC(C2=NN(C[C@H](C)NC(C3=NNC(C(C)=O)=C3)=O)C=C2)=C1
Molecular Formula
C19H17ClN6O2
Molecular Weight
396.83
References & Citations
[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.|[2]Toermaekangas Olli, et al. Preparation of heteroaryl carboxamides as androgen receptor modulators. From PCT Int. Appl. (2012), WO 2012143599 A1 20121026.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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