| CAS |
90357-06-5 |
| Chinese Name |
比卡鲁胺 |
| English Name |
Bicalutamide |
| Synonyms |
ICI-176334 |
| Molecular Formula |
C18H14F4N2O4S |
| Molecular Weight |
430.37 |
| Solubility |
Soluble in DMSO |
| Purity |
HPLC≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 200-001-8 |
| MDL |
MFCD00869971 |
| SMILES |
FC1=CC=C(S(=O)(CC(O)(C(NC2=CC=C(C#N)C(C(F)(F)F)=C2)=O)C)=O)C=C1 |
| InChIKey |
LKJPYSCBVHEWIU-UHFFFAOYSA-N |
| InChI |
InChI=1S/C18H14F4N2O4S/c1-17(26,10-29(27,28)14-6-3-12(19)4-7-14)16(25)24-13-5-2-11(9-23)15(8-13)18(20,21)22/h2-8,26H,10H2,1H3,(H,24,25) |
| PubChem CID |
2375 |
| Target Point |
Androgen Receptor |
| Passage |
Endocrinology & Hormones |
| Background |
Bicalutamide is a nonsteroidal androgen receptor inhibitor. |
| Biological Activity |
Bicalutamide (ICI-176334) 是一种androgen receptor (AR)拮抗剂，在LNCaP/AR(cs)细胞系中IC50为0.16 μM。Bicalutamide 可诱导自噬。[1] |
| In Vitro |
Bicalutamide 经过一个拮抗剂到激活剂的转变，刺激AR活性。在缺乏合成雄激素R1881的情况下，Bicalutamide处理LNCaP/AR(cs)细胞，改变基因表达，与其记录的良好激活剂活性相符合。Bicalutamide诱导细胞增殖，这种作用存在剂量依赖性，且只部分抗R1881的效果。Bicalutamide 处理呀显著产生大量核AR，虽然比R1881处理的少。Bicalutamide通过诱导DNA在AR靶基因结合，而具有部分激活剂活性，且不完全抗 R1881的效果。在R1881存在时，Bicalutamide部分激活 VP16-AR调节的转录，指导AR 结合到DNA上。使用AR驱动的荧光素酶报告结构稳定整合到LNCaP/AR-luc细胞中。在R1881存在时，Bicalutamide只微弱且部分抗 VP16-AR调节的转录，IC50 为 0.35 μM。[1] 微摩尔 Bicalutamide显著降低集落形成，这种作用存在剂量依赖性。[2] 双重抑制 AR 和 mTOR信号通路产生进一步好处，在体外，Ridaforolimus-Bicalutamide联用作用于前列腺癌细胞，与单独药剂处理相比，产生协同抗增殖效果。[3] |
| In Vivo |
Bicalutamide按规定的次最大剂量单独处理，降低79%肿瘤生长。Ridaforolimus-Bicalutamide 联用具有改进的和有效的抗肿瘤活性，几乎完全废除肿瘤生长。联合使用具有良好耐受性，在处理过程中体重没有明显改变。联用处理的小鼠中，血浆PSA水平与肿瘤生长紧密相关。[3] |
| Animal Experiment |
Animal Models: 携带C4-2细胞的雄性裸鼠; Dosages: 10 mg/kg; Administration: 口服处理[3] |
| Kinase Experiment |
Whole-cell competitive binding assays are performed in LNCaP/AR(codon-switch)(LNCaP/AR(cs))(harbors a mixture of exogenous wild-type AR and endogenous mutant AR(T877A))and cells propagated in Iscove's or RPMI media supplemented with 10% fetal bovine serum，or during the assay with 10% charcoal-stripped，dextran-treated fetal bovine serum(CSS). Cells are pre-incubated with 18F-FDHT，increasing concentrations(1pM to 1μM)of cold Bicalutamide are added，and the assay is performed to measure specific uptake of 18F-FDHT(4). IC50 values are determined using a one site binding model with least squares curve fitting and R2 > 0.99.[1] |
| Data Literature Source |
[1] Clegg NJ，et al. Cancer Res. 2012，72(6)，1494-1503.
[2] Colquhoun AJ，et al. Prostate Cancer Prostatic Dis. 2012.
[3] Squillace RM，et al. Int J Oncol. 2012. |
| Unit |
Bottle |
| Specification |
50mg 10mM*1mL in DMSO 100mg |
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