| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| B407813-1ml |
1ml |
现货  |
|
| 英文别名 | N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-propanamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Bicalutamide (ICI-176334) |
| 生化机理 | 比卡鲁胺（ICI-176334）是一种雄激素受体（AR）拮抗剂，在 LNCaP/AR(cs) 细胞系中的 IC50 值为 0.16 μM。比卡鲁胺可促进自噬。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 拮抗剂 |
| 作用机制 | 雄激素受体拮抗剂 |
| 产品介绍 |
不溶于水，溶于DMSO.比卡鲁胺（CDX）是一个非激素类雄激素受体（AR）拮抗剂和纯抗雄激素。它的作用通过平衡组蛋白乙酰化/脱乙酰化。比卡鲁胺（CDX）废除雄激素介导的表达。例如，MMP13在下列情况下上调，前列腺癌，PLZF（早幼粒细胞白血病锌指蛋白），和GADD45γ（生长抑制DNA损伤诱导，γ）。PI3K/AKT被雄激素磷酸化后，可抑制比卡鲁胺（CDX）的作用。 Information Bicalutamide (ICI-176334) Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy . Bicalutamide undergoes an antagonist-to-agonist switch, stimulating AR activity. Bicalutamide treatment of LNCaP/AR(cs) cells in absence of the synthetic androgen R1881 results in altered gene expression consistent with its well-documented agonist activity in context of AR overexpression. Bicalutamide induces cell proliferation in a dose-dependent manner, and only partially antagonized the effects of R1881. Bicalutamide treatment also results in a significant amount of nuclear AR, although less than that observed with R1881. Bicalutamide exhibits partial agonist activity as evidenced by induction of DNA binding at AR target genes and incomplete antagonism of the effects of R1881. In absence of R1881, Bicalutamide partially activates VP16-AR–mediated transcription, indicative of AR binding to DNA. In LNCaP/AR-luc cells with a stably integrates AR-driven luciferase reporter construct. In the presence of R1881, Bicalutamide shows only weak partial antagonism of VP16-AR–mediated transcription with an IC50 of 0.35 μM. Micromolar bicalutamide causes a significant dose-dependent reduction in clonogenicity. Dual inhibition of the AR and mTOR signaling pathways provides further benefit with the ridaforolimus-bicalutamide combination producing syner -gistic antiproliferative effects in prostate cancer cells in vitro when compared with each agent alone. In vivo Single bicalutamide reduces tumor growth by 79%, at defined submaximal doses. The ridaforolimus-bicalutamide combination exhibits improved and potent antitumor activity, almost completely abrogating tumor growth. The combination is also well tolerated, as evidenced by no significant changes in body weight over the course of treatment. Plasma PSA levels are again tightly linked to tumor growth in the combination-treated mice. cell lines： Concentrations：0-1 μM Incubation Time：72 hours Powder Purity:≥99% |
| ALogP | 2.926 |
|---|---|
| hba_count | 3 |
| HBD Count | 1 |
| Rotatable Bond | 6 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CC(O)(C[S](=O)(=O)C1=CC=C(F)C=C1)C(=O)NC2=CC=C(C#N)C(=C2)C(F)(F)F |
| 分子量 | 430.37 |
| Reaxy-Rn | 5364666 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=5364666&ln= |
| DMSO(mg / mL) Max Solubility | 86 |
|---|---|
| DMSO(mM) Max Solubility | 199.83 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 5364666 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=5364666&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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