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Darolutamide - 99%, high purity , Androgen Receptor antagonist, CAS No.1297538-32-9, Androgen Receptor antagonist

Moligand™
≥99%

CAS#: 1297538-32-9
Formula: C₁₉H₁₉ClN₆O₂
Molecular Weight: 398.85
PubChem CID: 67171867

Item Number

D413782

Grouped product items
SKU	Size	Availability	Price
D413782-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$129.90
D413782-10mg	10mg	In stock	$205.90
D413782-50mg	50mg	In stock	$489.90
D413782-100mg	100mg	In stock	$924.90
D413782-250mg	250mg	In stock	$2,081.90

Androgen Receptor Antagonists

View related series

Androgen receptor Antagonist

Basic Description

Synonyms	Darolutamide\|ODM-201\|1297538-32-9\|Nubeqa\|BAY-1841788\|BAY1841788\|N-((S)-1-(3-(3-Chloro-4-cyanophenyl)-1H-pyrazol-1-yl)propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide\|X05U0N2RCO\|BAY 1841788\|Darolutamide [USAN]\|UNII-X05U0N2RCO\|ODM201\|BAY-1841788)\|O
Specifications & Purity	Moligand™, ≥99%
Biochemical and Physiological Mechanisms	Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K_i of 11 nM. Phase 3.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	ANTAGONIST
Mechanism of action	Androgen Receptor antagonist
Product Description	Information Darolutamide (ODM-201) Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K i of 11 nM. Phase 3. Targets Androgen receptor 11 nM(Ki) In vitro In AR-HEK293 cells stably expressing full-length hAR, ODM-201 inhibits human AR (hAR) with IC50 of 26 nM. ODM-201 inhibits VCaP cell proliferation with IC50 of 230 nM, while has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells. In vivo In mice bearing VCaP xenografts, ODM-201 (50\u2009mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth. Cell Research(from reference) Cell lines：DU-145, H1581, and VCaP cells Concentrations：~10 μM Incubation Time：4 days

ALogP

3.034

HBD Count

Rotatable Bond

Associated Targets

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

Discover Target: CYP3A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Discover Target: BRD4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Discover Target: HDAC6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AR Tclin Androgen receptor 2 Activities

Discover Target: AR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	N-[(2S)-1-[3-(3-chloro-4-cyanophenyl)pyrazol-1-yl]propan-2-yl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide
INCHI	InChI=1S/C19H19ClN6O2/c1-11(22-19(28)18-8-17(12(2)27)23-24-18)10-26-6-5-16(25-26)13-3-4-14(9-21)15(20)7-13/h3-8,11-12,27H,10H2,1-2H3,(H,22,28)(H,23,24)/t11-,12?/m0/s1
InChi Key	BLIJXOOIHRSQRB-PXYINDEMSA-N
Canonical SMILES	CC(CN1C=CC(=N1)C2=CC(=C(C=C2)C#N)Cl)NC(=O)C3=NNC(=C3)C(C)O
Isomeric SMILES	C[C@@H](CN1C=CC(=N1)C2=CC(=C(C=C2)C#N)Cl)NC(=O)C3=NNC(=C3)C(C)O
PubChem CID	67171867
Molecular Weight	398.85

PubChem CID

67171867

CAS Registry No.

1297538-32-9

BindingDB Ligand

309979

Certificates

Certificate of Analysis(COA)

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4 results found

Lot Number	Certificate Type	Date	Item
H2229236	Certificate of Analysis	Jun 20, 2022	D413782
H2229237	Certificate of Analysis	Jun 20, 2022	D413782
H2229238	Certificate of Analysis	Jun 20, 2022	D413782
H2229239	Certificate of Analysis	Jun 20, 2022	D413782

Solubility

Solubility (25°C) In vitro DMSO: 80 mg/mL (200.57 mM); Ethanol: 38 mg/mL warmed with 50ºC Water: bath (95.27 mM); Water: Insoluble;

DMSO(mg / mL) Max Solubility

DMSO(mM) Max Solubility

200.5766579

Water(mg / mL) Max Solubility

＜1

References

1. Moilanen AM, Riikonen R, Oksala R, Ravanti L, Aho E, Wohlfahrt G, Nykänen PS, Törmäkangas OP, Palvimo JJ, Kallio PJ. (2015) Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies.. Sci Rep, 5 (3): (12007). [PMID:26137992]
2. Fizazi K, Albiges L, Loriot Y, Massard C. (2015) ODM-201: a new-generation androgen receptor inhibitor in castration-resistant prostate cancer.. Expert Rev Anticancer Ther, 15 (9): (1007-17). [PMID:26313416]
3. Fizazi K, Shore N, Tammela TL, Ulys A, Vjaters E, Polyakov S, Jievaltas M, Luz M, Alekseev B, Kuss I et al.. (2019) Darolutamide in Nonmetastatic, Castration-Resistant Prostate Cancer.. N Engl J Med, 380 (13): (1235-1246). [PMID:30763142]

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