CD437

CD437CAS号: 125316-60-1分子式: C27H26O3分子量: 398.49描述纯度储存/保存方法形态别名外观密度熔点沸点折射率IC50PK值Ki 数据可溶性/溶解性MDLPubChem CID靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

CD437 is a specifc Retinoic Acid Receptor γ (RARγ) agonist.

纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
形态
Solid
基本信息
别名
AHPN;CD 437;CD-437
外观
yellow solid
密度
~1.3 g/cm3 (Predicted)
熔点
271.6-276° C
沸点
~595.0° C at 760 mmHg (Predicted)
折射率
n20D 1.69 (Predicted)
IC50
OVCAR-3: IC50 = 0.13 µM (human); DU-145: IC50 = 0.28 µM (human); LNCaP: IC50 = 0.32 µM (human); ADMET: IC50 = 0.33 µM; IGROV-1: IC50 = 0.35 µM (human)
PK值
pKa: 4.17 (Predicted)
Ki 数据
RAR γ: Ki= 77 nM (human); RAR β: Ki= 2.48 µM (human); RAR α: Ki= 6.5 µM (human)
可溶性/溶解性
DMSO : 150 mg/mL (376.42 mM; Need ultrasonic and warming)
MDL
MFCD03106506
PubChem CID
135411
生物活性
靶点
RARγ
In vitro(体外研究)
CD437 is a selective RARγ agonist. Growth inhibition by CD437 in these lung cancer cell lines is apparent after 2 days of treatment with 10 μM CD437. Dose-response experiments demonstrate that CD437 reduces the numbers of H460, SK-MES-1, A549, and H292 cells with 50% inhibitory values of approximately 0.5, 0.4, 3, and 0.85 μM, respectively. Treatment for 72 h with CD437 causes a strong dose-dependent growth inhibition in all melanoma cell lines. At a concentration of 5 μM CD437, only about 5 to 25% of the cells remain viable after 3 d. The concentrations of CD437 required for 50% growth inhibition (IC50) range from 10 μM for MeWo to 0.1 μM for SK-Mel-23 showing the highest sensitivity.
In vivo(体内研究)
Tumors in CD437-treated mice stop growing, an effect that becomes already statistically significant (P<0.01) at day 13, 3 d after first administration of CD437, and is maintained for more than 3 wk after discontinuation of treatment. Further histologic analysis demonstrates marked c-fos mRNA levels at the tumor-stroma edge in CD437-treated tumors

分子结构图

CD437