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CD 437

CD 437用途

CD437 是一个选择性视黄酸受体 (Retinoic Acid Receptor γ (RARγ)) 激动剂。

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CD 437名称

[ CAS 号 ]:
125316-60-1

[ 中文名 ]:
6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸

[ 英文名 ]:
CD437

[英文别名 ]:

O-Desmethyl Adapalene
AHPN
Cd 437
CD437

CD 437生物活性

[ 描述 ]:

CD437 是一个选择性视黄酸受体 (Retinoic Acid Receptor γ (RARγ)) 激动剂。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> RAR/RXR

研究领域 >> 癌症

[ 靶点 ]

Retinoic Acid Receptor γ (RARγ)[1]

[体外研究]

CD437是选择性RARγ激动剂。在用10μMCD437处理2天后,这些肺癌细胞系中CD437的生长抑制是明显的。剂量-反应实验表明CD437分别减少H460,SK-MES-1,A549和H292细胞的数量,50％抑制值分别为约0.5,0.4,3和0.85μM[1]。用CD437处理72小时在所有黑素瘤细胞系中引起强烈的剂量依赖性生长抑制。在浓度为5μMCD437时,3天后仅约5-25％的细胞保持存活。 50％生长抑制所需的CD437浓度(IC50)范围从MeWo的10μM到SK-Mel-23的0.1μM,显示出最高的灵敏度[2]。

[体内研究]

CD437处理的小鼠中的肿瘤停止生长,这种作用在第13天,第一次施用CD437后3天已经具有统计学显着性(P <0.01),并且在停止治疗后维持超过3周。进一步的组织学分析显示CD437治疗的肿瘤中肿瘤基质边缘有明显的c-fos mRNA水平[2]。

[细胞实验]

对于形态学分析，细胞用10μMCD4处理，胰蛋白酶消化，用磷酸盐缓冲盐水（PBS）洗涤，用3.7％多聚甲醛固定，并用50μg4,6-二脒基-2-苯基吲哚（DAPI）每mL染色每毫升含有100微克不含DNA酶的RNase A，以观察细胞核。通过荧光显微镜检查染色细胞。对于末端脱氧核苷酸转移酶（TdT）测定，用或不用10μMCD437处理细胞。处理后，将细胞用胰蛋白酶消化，用PBS洗涤，在PBS中的1％甲醛中固定，用PBS洗涤，重悬于70％冰冷的乙醇中，并立即在-20℃下保存过夜。然后通过末端转移酶用生物素-16-dUTP标记细胞，并用抗生物素蛋白-FITC（异硫氰酸荧光素）染色。用流式细胞仪分析标记的细胞[1]。

[动物实验]

在该研究中使用重20至25g的雄性Swiss-nu / nu小鼠。将小鼠保持在无菌条件下，室温24℃至26℃，相对湿度50％，层流架中12小时光暗黑暗节律，并提供高压灭菌的食物和寝具。对于黑素瘤异种移植物的治疗，将先前建立的直径为1至2mm的MeWo黑素瘤肿瘤植入动物的右侧腹部。在肿瘤生长10天后，将小鼠组（n = 8）用生理盐水处理或者在肿瘤内注射3周或者喂食不同浓度的CD437（10mg / kg /体重和30mg / kg /体重）。另外，第五组的肿瘤每天注射CD437（10mg / kg /体重）。每天访问小鼠，每周用卡尺仪器测量肿瘤生长两次[2]。

[参考文献]

[1]. Li Y, et al. Molecular determinants of AHPN (CD437)-induced growth arrest and apoptosis in human lung cancer cell lines. Mol Cell Biol. 1998 Aug;18(8):4719-31.

[2]. Schadendorf D, et al. Treatment of melanoma cells with the synthetic retinoid CD437 induces apoptosis via activation of AP-1 in vitro, and causes growth inhibition in xenografts in vivo. J Cell Biol. 1996 Dec;135(6 Pt 2):1889-98.

[相关活性小分子]

CD 437物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
595.0±50.0 °C at 760 mmHg

[ 熔点 ]:
271.6-276ºC

[ 分子式 ]:
C₂₇H₂₆O₃

[ 分子量 ]:
398.493

[ 闪点 ]:
327.7±26.6 °C

[ 精确质量 ]:
398.188202

[ PSA ]:
57.53000

[ LogP ]:
7.45

[ 蒸汽压 ]:
0.0±1.8 mmHg at 25°C

[ 折射率 ]:
1.689

[ 储存条件 ]:
-20°C

CD 437MSDS

详细MSDS(安全技术说明书)

CD 437毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QJ1975900

CHEMICAL NAME :: 2-Naphthalenecarboxylic acid, 6-(4-hydroxy-3-tricyclo(3.3.1.1(3,7))dec-1-ylphenyl)-

CAS REGISTRY NUMBER :: 125316-60-1

LAST UPDATED :: 199806

DATA ITEMS CITED :: 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 15 mg/kg

SEX/DURATION :: female 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 53,158,1996

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 15 mg/kg

SEX/DURATION :: female 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 53,158,1996

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CD 437安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
S22

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
QJ1975900

CD 437合成路线

详细合成路线

CD 437上下游产品

CD 437上游产品

CD 437下游产品

CD 437文献

All-trans-retinoic acid regulates aquaporin-3 expression and related cellular membrane permeability in the human amniotic environment.

Placenta 36 , 881-7, (2015)

The aquaporins (AQP1, 3, 8, 9 and 11) are known to be expressed, and involved in the transport of water and small molecules through fetal membranes. To exert these crucial functions, these AQPs have t...

Signalling Through Retinoic Acid Receptors is Required for Reprogramming of Both Mouse Embryonic Fibroblast Cells and Epiblast Stem Cells to Induced Pluripotent Stem Cells.

Stem Cells 33(5) , 1390-404, (2015)

We previously demonstrated that coexpressing retinoic acid (RA) receptor gamma and liver receptor homolog-1 (LRH1 or NR5A2) with OCT4, MYC, KLF4, and SOX2 (4F) rapidly reprograms mouse embryonic fibro...

Preclinical efficacy of the synthetic retinoid ST1926 for treating adult T-cell leukemia/lymphoma.

Blood 124(13) , 2072-80, (2014)

Adult T-cell leukemia/lymphoma (ATL) is an aggressive neoplasm caused by human T-cell leukemia virus type 1 (HTLV-1). The HTLV-1 oncoprotein Tax plays an important role in ATL pathogenesis. ATL carrie...

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