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%
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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.
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形态 |
Solid
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基本信息 | |
别名 |
AHPN;CD 437;CD-437
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外观 |
yellow solid
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密度 |
~1.3 g/cm3 (Predicted)
|
熔点 |
271.6-276° C
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沸点 |
~595.0° C at 760 mmHg (Predicted)
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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)
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PK值 |
pKa: 4.17 (Predicted)
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Ki 数据 |
RAR γ: Ki= 77 nM (human); RAR β: Ki= 2.48 µM (human); RAR α: Ki= 6.5 µM (human)
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可溶性/溶解性 |
DMSO : 150 mg/mL (376.42 mM; Need ultrasonic and warming)
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MDL |
MFCD03106506
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PubChem CID |
135411
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生物活性 | |
靶点 |
RARγ
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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.
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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
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分子结构图