Apalutamide (ARN-509)

Catalog No. A11923

Apalutamide (ARN-509)是一种具有潜在抗肿瘤活性的雄激素受体拮抗剂,IC50 为 16 nM。ARN-509与靶组织中的AR结合,从而阻止了雄激素诱导的受体激活,并促进了无法转运至细胞核的无活性复合物的形成。这防止了AR应答基因的结合和转录。
  • Frédérique Mittler, .et al. High-Content Monitoring of Drug Effects in a 3D Spheroid Model, Front Oncol, 2017, 7: 293 PMID: 29322028
Catalog Num A11923
M. Wt 477.4
Formula C21H15F4N5O2S
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 956104-40-8
Synonyms ARN509
SMILES CNC(=O)C1=C(C=C(C=C1)N2C(=S)N(C(=O)C23CCC3)C4=CN=C(C(=C4)C(F)(F)F)C#N)F
Apalutamide (ARN-509)是一种具有潜在抗肿瘤活性的雄激素受体拮抗剂,IC50 为 16 nM。ARN-509与靶组织中的AR结合,从而阻止了雄激素诱导的受体激活,并促进了无法转运至细胞核的无活性复合物的形成。这防止了AR应答基因的结合和转录。
Targets
Androgen Receptor (Cell-free assay) GABAA receptor (Cell-free assay)
16 nM3 μM
In vitro (25°C) DMSO 18 mg/mL (37.7 mM)
Water Insoluble
Ethanol 5 mg/mL (10.47 mM)
In vivo 2% DMSO+40% PEG 300+2% Tween 80+ddH2O 2 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 20.95 mL 104.73 mL 209.47 mL
0.5 mM 4.19 mL 20.95 mL 41.89 mL
1 mM 2.09 mL 10.47 mL 20.95 mL
5 mM 0.42 mL 2.09 mL 4.19 mL

*The above data is based on the productmolecular weight 477.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.