Darolutamide, ACS – CAS 1297538-32-9

Price f.o.b. for gr.1

CAS Number: 1297538-32-9 Category:

Additional information

Weight 1 g
product name

Darolutamide, ACS


ODM-201 ;
BAY-1841788 ;
N-((S)-1-(3-(3-Chloro-4-cyanophenyl)-1H-pyrazol-1-yl)propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide ;

product origin

100% made in European Union (according to USP, EUP, ECHA-REACH)

purity grade

>99.99% (raw virgin matter, ultra-pure, sterilized)


lab. / tech. / bio-research / receptor / antagonist / industrial

product code


C.A.S. number






ID PubChem substance


formula molecular


linear formula


formula weight

389.85 g/mol

boiling point

719.50 °C

axact mass



DMF: 25 mg/ml
DMSO: 25 mg/ml
DMSO: PBS(pH 7.2) (1:3): 0.25 mg/ml
Ethanol: 10 mg/ml


(DMSO) ≥ 44 mg/mL * "<1 mg/mL" means slightly soluble or insoluble,
≥ means soluble, but saturation unknown


≥ 4 years

sensitivity & storage

2 ° to 8°C refrigerator ;
powder :
-20 °C 3 years
>4 °C 2 years
in solvent :
-80 °C 6 months
-20 °C 1 month


androgen receptor

assay (HPLC)


appearance (color)

white to off-white



biological activity

ODM–201 is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in AR–HEK293 cells. IC50 & Target: IC50: 26 nM (AR–HEK293 cells, AR) In Vitro: In competitive AR binding assays, the inhibition constant (Ki) values of ODM–201 are 11 nM. ODM-201, ORM-15341 suppresse androgen-induced cell proliferation more efficaciously than enzalutamide or ARN–509, IC50 values being 230 and 170nM for ODM–201 and ORM–15341 vs. 410 and 420 nM for enzalutamide and ARN–509. ODM–201 has no effect on the viability of AR–negative cell lines tested, DU-145 prostate and H1581 lung cancer cells confirming that the antiproliferative properties of ODM-201 and ORM-15341 are specific to AR-dependent PC cells.
In Vivo: 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) or enzalutamide (p =0.0245), 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 ODM–201 twice daily do not decrease significantly during the treatment.


Cell Assay: To study the antiproliferative properties of ODM–201 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.
Animal Administration: [1]To elucidate the in vivo efficacy of ODM–201 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 studies 9 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 ODM–201 (50 mg/kg, bid). Moreover, enzalutamide exhibited a long plasma half–life (18.3 hours) while the half–life of ODM–201 in mice is not optimal (1.6 hours) supporting once daily dosing for enzalutamide and higher dose and more frequent dosing for ODM–201.

note (1)

this product is for research use only, is not to be used for therapeutic ; not intended for animal or human or diagnostic or therapeutic use , and cannot be sold to patients.

note (2)

described price of the product is NOT NEGOTIABLE , already around 25% lower than the official price of the International Chemical Stock Exchange / ICIS .

* Possible additional discount for large quantity orders .

packaging / transport

special for chemical transport (according to IATA / ADR / ECHA-REACH rules / int.l laws) .


C.O.A., MSDS, GMP, API, USP, EUP, ECHA-REACH, ORIGIN, etc… (originals will be delivered with good , and copies after confirmed order)


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