2. Neuronal Signaling Membrane Transporter/Ion Channel MAPK/ERK Pathway GPCR/G Protein Immunology/Inflammation Autophagy
  3. Calcium Channel Ras STING Autophagy
  4. Fendiline

Fendiline  (Synonyms: 芬他林)

目录号: HY-B0984A 纯度: 99.41%
COA 产品使用指南 技术支持

Fendiline 是一种二苯烷基胺类抗心绞痛剂，是一种 L 型钙通道 (L-type calcium channel) 阻滞剂 (IC50 为 17 μM)。Fendiline 也是一种选择性 K-Ras 抑制剂，对 H-Ras 和 N-Ras 无作用。Fendiline 可抑制 K-Ras 质膜定位 (IC50 为 9.64 μM)，抑制 K-Ras 信号输出，并阻断表达致癌突变 K-Ras 的胰腺癌、结肠癌、肺癌和子宫内膜癌细胞系的增殖。Fendiline 还是一种 STING 激动剂，能够抑制多种难治性冷肿瘤 (MC38、CT26 和 B16F10) 的生长。

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Fendiline

Fendiline Chemical Structure

CAS No. : 13042-18-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥220
In-stock
5 mg ￥200
In-stock
10 mg ￥352
In-stock
25 mg ￥744
In-stock
50 mg ￥1200
In-stock
100 mg ￥1920
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500 mg   询价  

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Customer Review

Other Forms of Fendiline:

Fendiline 相关抗体

Top Publications Citing Use of Products

查看 Calcium Channel 亚型特异性产品:

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

查看 Ras 亚型特异性产品:

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K-Ras H-Ras N-Ras Ras

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Fendiline, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC50 of 17 µM). Fendiline is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline inhibits K-Ras plasma membrane localization (IC50 of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10)[1][2][4].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BXPC-3 IC50
28.6 μM
Compound: 6
Antiproliferative activity against human BXPC-3 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human BXPC-3 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
Caco-2 IC50
14.5 μM
Compound: 6
Antiproliferative activity against human Caco-2 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human Caco-2 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
CHO EC50
1000 nM
Compound: Fendiline
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
[PMID: 23465611]
HEC-1-A IC50
9.48 μM
Compound: 6
Antiproliferative activity against human HEC-1-A cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human HEC-1-A cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
HEC-1B cell line IC50
9.8 μM
Compound: 6
Antiproliferative activity against human HEC-1B cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human HEC-1B cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
Ishikawa IC50
> 30 μM
Compound: 6
Antiproliferative activity against human Ishikawa cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human Ishikawa cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
MEF IC50
13.1 μM
Compound: 6
Antiproliferative activity against mouse MEF cells expressing KRAS G12D mutant assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against mouse MEF cells expressing KRAS G12D mutant assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
MEF IC50
17.8 μM
Compound: 6
Cytotoxicity against mouse MEF cells expressing BRAF V600E mutant and wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Cytotoxicity against mouse MEF cells expressing BRAF V600E mutant and wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
MEF IC50
8.1 μM
Compound: 6
Antiproliferative activity against mouse MEF cells expressing KRAS G12V mutant assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against mouse MEF cells expressing KRAS G12V mutant assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
MIA PaCa-2 IC50
9.2 μM
Compound: 6
Antiproliferative activity against human MIA PaCa-2 cells expressing KRAS mutant assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human MIA PaCa-2 cells expressing KRAS mutant assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
NCI-H1299 IC50
24.3 μM
Compound: 6
Antiproliferative activity against human NCI-H1299 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human NCI-H1299 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
NCI-H1975 IC50
> 30 μM
Compound: 6
Antiproliferative activity against human NCI-H1975 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human NCI-H1975 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
NCI-H23 IC50
11.4 μM
Compound: 6
Antiproliferative activity against human NCI-H23 cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human NCI-H23 cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
NCI-H522 IC50
29.6 μM
Compound: 6
Antiproliferative activity against human NCI-H522 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human NCI-H522 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
SK-CO-1 IC50
7.8 μM
Compound: 6
Antiproliferative activity against human SK-CO-1 cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human SK-CO-1 cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
[PMID: 33756124]
Ventricular myocyte IC50
17 μM
Compound: Fendiline
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
体外研究
(In Vitro)

Fendiline (0.3-100 µM) 以浓度和时间依赖性的方式在细胞外抑制钙通道电流 (ICa)[1]。
Fendiline 不抑制 K-Ras 的翻译后加工，但显著降低 K-Ras 的聚集，并将 K-Ras 从质膜重新分布到内质网 (ER)、高尔基体、内体和胞质溶胶[2]。
Fendiline (17 µM; 48 小时) 显著抑制致癌 H-Ras 转化细胞中组成性活性 K-Ras 下游信号和内源性 K-Ras 信号[2]。
Fendiline (0-1.25 μM; 72 小时) 可阻断表达致癌突变 K-Ras 的胰腺癌、结肠癌、肺癌和子宫内膜癌细胞系的增殖[2]。
Fendiline 与 [3H]Yohimbine 竞争与人血小板 α2-肾上腺素受体的结合，Kd 为 2.6 µM[3]。
Fendiline (M335) (5-40 μM；4 小时) 在 THP-1 细胞中，以浓度依赖的方式激活 STING-TBK1-IRF3 轴并诱导自噬 (使 LC3-II 上调)[4]。
Fendiline (20 μM；4 小时) 在 THP-STING KO 细胞中，无法激活 pTBK1、pIRF3，也不能上调 IFNB、ISG15、CXCL10 和 IL6[4]。
Fendiline (10-30 μM；6 小时) 在感染 HSV-1-GFP 的 THP-1 细胞中，以剂量依赖的方式降低病毒感染效率[4]。
Fendiline (20 μM；6 小时) 在过表达 STING 的 HeLa-STOE 细胞中，对 HSV-1-GFP 的抗病毒活性比在 STING 缺陷的 HeLa 细胞中更强[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Fendiline 相关抗体:

Western Blot Analysis[2]

Cell Line: MDCK cells stably expressing K-RasG12V
Concentration: 2.5 µM, 5 µM, 7.5 µM, 10 µM, 12.5 µM, 15 µM
Incubation Time: 48 h
Result: Inhibited the ERK and Akt activation with IC50s of 9.49 μM and 6.97 μM, respectively.

Western Blot Analysis[2]

Cell Line: MDCK cells stably expressing K-RasG12V
Concentration: 17 µM
Incubation Time: 48 h
Result: Significantly reduced pMEK, pERK, and pAkt levels in BHK and MDCK cells expressing constitutively active H-RasG12V.

Western Blot Analysis[4]

Cell Line: THP-1 cells
Concentration: 5 μM, 10 μM, 20 μM, 40 μM
Incubation Time: 2 h, 4 h, 6 h, 8 h
Result: The protein expression of pTBK1, pIRF3, and LC3-II increased in a concentration-dependent manner, indicating the activation of the STING pathway and autophagy.
体内研究
(In Vivo)

Fendiline (300 μg；瘤内注射；每 2 天一次；20 天) 在接种 MC38 肿瘤的 C57BL/6J 小鼠中，使肿瘤生长抑制率达到 82% ，并增加了肿瘤和脾脏中的 CD8⁺T 细胞及 NK 细胞数量[4]。
Fendiline (5-20 mg/kg；腹腔注射；每 2 天一次；20 天) 在接种 CT26 或者 B16F10 肿瘤的 BALB/c 小鼠中，剂量依赖性地抑制肿瘤生长，并激活全身免疫 (使脾脏中的 CD45+、CD3+、CD8+、NK+ 细胞增多)[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (female, 6-8 weeks old,) with subcutaneous MC38 tumors[4].
Dosage: 300 μg
Administration: Intratumoral injection, every 2 days, for 20 days
Result: The tumor growth inhibition rate (TGI) was 82%.
There was no significant weight loss or organ toxicity.
Animal Model: BALB/c mice (female, 6-8 weeks old) with subcutaneous CT26 or B16F10 tumors[4].
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: Intraperitoneal injection, every 2 days, for 20 days
Result: There was a dose-dependent tumor growth inhibition.
There was no significant systemic toxicity.
分子量

315.45

Formula

C23H25N
CAS 号
性状

液体

颜色

Colorless to light yellow

中文名称

芬他林
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (317.01 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1701 mL 15.8504 mL 31.7007 mL
5 mM 0.6340 mL 3.1701 mL 6.3401 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.93 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.93 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

Fendiline 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1701 mL 15.8504 mL 31.7007 mL 79.2519 mL
5 mM 0.6340 mL 3.1701 mL 6.3401 mL 15.8504 mL
10 mM 0.3170 mL 1.5850 mL 3.1701 mL 7.9252 mL
15 mM 0.2113 mL 1.0567 mL 2.1134 mL 5.2835 mL
20 mM 0.1585 mL 0.7925 mL 1.5850 mL 3.9626 mL
25 mM 0.1268 mL 0.6340 mL 1.2680 mL 3.1701 mL
30 mM 0.1057 mL 0.5283 mL 1.0567 mL 2.6417 mL
40 mM 0.0793 mL 0.3963 mL 0.7925 mL 1.9813 mL
50 mM 0.0634 mL 0.3170 mL 0.6340 mL 1.5850 mL
60 mM 0.0528 mL 0.2642 mL 0.5283 mL 1.3209 mL
80 mM 0.0396 mL 0.1981 mL 0.3963 mL 0.9906 mL
100 mM 0.0317 mL 0.1585 mL 0.3170 mL 0.7925 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fendiline13042-18-7芬他林Calcium ChannelRasSTINGAutophagyCa2+ channelsCa channelsStimulator of Interferon GenesTMEM173MITAERISMPYSantianginal agentL-type calcium channelK-RasMC38CT26 and B16F10Inhibitorinhibitorinhibit

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