1. Cytoskeleton Cell Cycle/DNA Damage Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis
  2. Microtubule/Tubulin Reactive Oxygen Species (ROS) Apoptosis PERK Eukaryotic Initiation Factor (eIF) IRE1
  3. FC-116

FC-11 是一种 tubulin 抑制剂。FC-11 抑制结直肠癌 (CRC) 细胞的增殖,对 HCT116 细胞的 IC50 值为 4.52 nM,对 CT26 细胞的 IC50 值为 18.69 nM。FC-11 可诱导内质网应激,产生过量的 ROS,导致线粒体损伤,从而通过靶向微管促进结直肠癌 (CRC) 细胞的凋亡 (apoptosis)。FC-11 在体内发挥强效的抗肿瘤作用。FC-11 可用于结直肠癌研究。

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FC-116

FC-116 Chemical Structure

CAS No. : 2417298-29-2

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10 mM * 1 mL in DMSO ¥1422
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1 mg ¥735
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FC-11 is a tubulin inhibitor. FC-116 inhibits the proliferation of colorectal cancer (CRC) cells, with IC50 values of 4.52 nM for HCT116 cells and 18.69 nM for CT26 cells. FC-11 can induce ER stress to generate excess ROS, leading to mitochondrial damage, thereby promoting apoptosis in colorectal cancer (CRC) cells by targeting microtubules. FC-116 exerts potent anti-tumor effects in vivo. FC-11 can be used for the study of colorectal cancer[1].

体外研究
(In Vitro)

FC-116 (24 h) 对 HCT116 细胞 (IC50 = 4.52 nM) 和 CT26 细胞 (IC50 = 18.69 nM) 表现出优异的抗增殖活性,且在相同剂量下对正常 NCM460 细胞和 PC12 细胞无细胞毒性[1]
FC-116 (2.5-40 nM, 24 h) 显著诱导 HCT116 和 CT26 细胞的凋亡、内质网应激、ROS 产生,并阻断细胞周期于 G2/M 期[1]
FC-116 (12.5-100 μM, 24 h) 通过 Cys239 和 Cys354 直接结合微管蛋白的秋水仙碱结合位点 (Kd = 136 nM),以剂量依赖方式抑制微管聚合作用,并破坏 HCT116 和 CT26 细胞的微管网络[1]
FC-116 (2.5-40 nM, 24 h) 降低 HCT116 细胞和 CT26 细胞的线粒体膜电位,抑制线粒体呼吸,并引起线粒体肿胀和空泡化[1]
FC-116 (0.3-30 nM, 3 days) 对三种结直肠癌类器官模型(21JW91CRT1、21Q4MGCRT1、22G5AECRT1)表现出强效的抑制活性,其 IC50 值分别为 2.5 nM、1.8 nM 和 1.9 nM[1]

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

Apoptosis Analysis[1]

Cell Line: HCT116 and CT26 cells
Concentration: 2.5, 5, 10, 20, 40 nM
Incubation Time: 24 h
Result: Increased the apoptosis rate.
Up-regulated the expression of apoptosis-related protein Cleaved-Caspase 3.

Cell Cycle Analysis[1]

Cell Line: HCT116 and CT26 cells
Concentration: 2.5, 5, 10, 20, 40 nM
Incubation Time: 24 h
Result: Blocked the cell cycle of HCT116 and CT26 cells in the G2/M phase.

Western Blot Analysis[1]

Cell Line: HCT116 and CT26 cells
Concentration: 2.5, 5, 10, 20, 40 nM
Incubation Time: 24 h
Result: Increased phosphorylation of PERK, eIF2α, and IRE1α.
体内研究
(In Vivo)

FC-116 (1.5-3 mg/kg,腹腔注射,每日一次,21 天) 在 HCT116 异种移植模型中显示出显著的抗肿瘤疗效[1]
FC-116 (1.5-3 mg/kg,腹腔注射,每日一次,45 天) 在 C57BL/6-APCmin/+ 小鼠中对肠道肿瘤形成表现出强效的抑制作用[1]

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

Animal Model: HCT116 cells (5 × 106) were subcutaneously injected into the right flank of 5-week-old male BALB/c nude mice[1].
Dosage: 1.5, 3 mg/kg
Administration: i.p., once daily, 21 days
Result: Achieved tumor growth inhibition.
Showed no significant changes in body weight.
Reduced the Ki67 expression.
Animal Model: C57BL/6-APCmin/+ mice with a mutation (replacing amino acid L at position 850 of the Apc gene with a termination codon X) were used[1].
Dosage: 1.5, 3 mg/kg
Administration: i.p., once daily, 45 days
Result: Achieved adenoma number inhibition.
Showed no significant changes in body weight.
Increased phosphorylation of endoplasmic reticulum (ER) stress-related molecules eIF2α and IRE1α in intestinal tissues.
Increased the necrotic area and apoptosis in tumor tissues.
分子量

369.39

Formula

C21H20FNO4

CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -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 : 66.67 mg/mL (180.49 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 2.7072 mL 13.5358 mL 27.0717 mL
5 mM 0.5414 mL 2.7072 mL 5.4143 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。

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

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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

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动物的平均体重

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工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

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 2.7072 mL 13.5358 mL 27.0717 mL 67.6791 mL
5 mM 0.5414 mL 2.7072 mL 5.4143 mL 13.5358 mL
10 mM 0.2707 mL 1.3536 mL 2.7072 mL 6.7679 mL
15 mM 0.1805 mL 0.9024 mL 1.8048 mL 4.5119 mL
20 mM 0.1354 mL 0.6768 mL 1.3536 mL 3.3840 mL
25 mM 0.1083 mL 0.5414 mL 1.0829 mL 2.7072 mL
30 mM 0.0902 mL 0.4512 mL 0.9024 mL 2.2560 mL
40 mM 0.0677 mL 0.3384 mL 0.6768 mL 1.6920 mL
50 mM 0.0541 mL 0.2707 mL 0.5414 mL 1.3536 mL
60 mM 0.0451 mL 0.2256 mL 0.4512 mL 1.1280 mL
80 mM 0.0338 mL 0.1692 mL 0.3384 mL 0.8460 mL
100 mM 0.0271 mL 0.1354 mL 0.2707 mL 0.6768 mL
Help & FAQs
  • 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.

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产品名称:
FC-116
目录号:
HY-155068
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