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ODM-201

CAT: 0013-GTR19163907-08Size: 500 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19163907-08Size:500 mg
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Description
A potent wt/mutant androgen receptor (AR) inhibitor with Ki of 11 nM; inhibits wtAR/AR (F876L) with IC50 of 65/66 nM respectively, weak inhibition on AR (W741L) and AR (T877A) ; inhibits the nuclear translocation of AR and more efficaciously than enzalutamide or ARN-509 in VCaP cell line proliferation assay; reduces the growth of AR-overexpressing VCaP prostate cancer cells both in vitro and in a castration-resistant VCaP xenograft model.Prostate Cancer Phase 3 Clinical (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. (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.
CAS Number
1297538-32-9
Product Name Alternative
BAY-1841788 | Darolutamide
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 44 mg/mL
Smiles
O=C (C1=NNC (C (O) C) =C1) N[C@@H] (C) CN2N=C (C3=CC=C (C#N) C (Cl) =C3) C=C2
Molecular Formula
C19H19ClN6O2
Molecular Weight
398.8462
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1H-Pyrazole-3-carboxamide, N-[ (1S) -2-[3- (3-chloro-4-cyanophenyl) -1H-pyrazol-1-yl]-1-methylethyl]-5- (1-hydroxyethyl) -

Chemical Information

Darolutamide

Darolutamide is a nonsteroidal androgen receptor antagonist for the treatment of castrate-resistant, non-metastatic prostate cancer (nmCRPC). This condition occurs in the majority of patients with advanced prostate cancer who have been treated with androgen receptor antagonists. Though prior treatment for prostate cancer has been successful for these patients, the cancer eventually progresses to become resistant to existing therapies. This warrants further treatment. The goal of treatment with darolutamide is to delay the progression of prostate cancer to metastatic disease, increasing quality of life and life expectancy for those with advanced prostate cancer. Darolutamide was developed by Bayer HealthCare Pharmaceuticals Inc. and approved by the FDA on July 30th, 2019.

CAS Number1297538-32-9
PubChem CID67171867
IUPAC NameN-[(2S)-1-[3-(3-chloro-4-cyanophenyl)pyrazol-1-yl]propan-2-yl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide
Molecular FormulaC19H19ClN6O2
Molecular Weight398.8
XLogP1.8
Topological Polar Surface Area120
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count5
Rotatable Bond Count6
Heavy Atom Count28
Formal Charge0
Complexity598
SMILES
C[C@@H](CN1C=CC(=N1)C2=CC(=C(C=C2)C#N)Cl)NC(=O)C3=NNC(=C3)C(C)O
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
InChIKey
BLIJXOOIHRSQRB-PXYINDEMSA-N
Chemical Structure
2D Structure
2D structure of Darolutamide
CAS: 1297538-32-9
CID: 67171867
Formula: C19H19ClN6O2
MW: 398.8
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight398.8
XLogP31.8
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count5
Rotatable Bond Count6
Exact Mass398.1258016
Monoisotopic Mass398.1258016
Topological Polar Surface Area120 Ų
Heavy Atom Count28
Formal Charge0
Complexity598
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count1
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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