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Darolutamide
ODM-201 , BAY-1841788
100% made in European Union *(according to USP, EUP, Echa-Reach)
>99.99% (1st. quality virgin matter , extra pure, selected )
tech. / lab. / Receptor / antagonist
SMC16985E
1297538-32-9
C19H19ClN6O2
389.85
389.1258
>99.99%
white to off-white
solid, powder
(DMSO) ≥ 44 mg/mL * "<1 mg/mL" means slightly soluble or insoluble,
xxxxxxxx≥ means soluble, but saturation unknown
powderxx : -20 °C 3 years
xxxxxxxxxxxx.4 °C 2 years
in solvent : -80 °C 6 months
xxxxxxxxxxx-20 °C 1 month
androgen receptor
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)[1]
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[1].
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[1].
(Extracted from published papers and Only for reference)
Cell Assay: [1]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[1].
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 studies9 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[1].
according to government transport (IATA, ADR) rules
shipped and packaged in a non returnable cylinder for chemical products
C.O.A., MSDS, GMP, API, USP, EUP, ECHA-REACH, ORIGIN, etc...
(originals will be delivered with good , and copies after confirmed order )
the price of the product is NO NEGOTIABLE , already around 25% lower than the official price
of the International Chemical Stock Exchange / ICIS |
