1. Protein Tyrosine Kinase/RTK Apoptosis
  2. FAK Apoptosis
  3. FAK-IN-29

FAK-IN-29 是一种选择性 FAK 抑制剂,IC50 为 0.5 nM。FAK-IN-29 可抑制 MDA-MB-231 细胞增殖、克隆形成,并诱导细胞周期阻滞和凋亡 (apoptosis)。FAK-IN-29 具有抗肿瘤的活性,可用于三阴性乳腺癌等肿瘤的研究。

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FAK-IN-29

FAK-IN-29 Chemical Structure

CAS No. : 3104566-26-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FAK-IN-29 is a selective FAK inhibitor with an IC50 of 0.5 nM. FAK-IN-29 can inhibit the proliferation and colony formation of MDA-MB-231 cells, and induce cell cycle arrest and apoptosis. FAK-IN-29 exhibits antitumor activity and can be used for the research of tumors such as triple-negative breast cancer[1].

体外研究
(In Vitro)

FAK-IN-29 (Compound 7h) (3 μM;24 小时) 在 MDA-MB-231 细胞中诱导 G2/M 期细胞周期阻滞[1]
FAK-IN-29 (0.15625-50 μM, 48 小时) 对 MDA-MB-231、SKOV3 和 HepG2 细胞的 IC50 分别为 0.18、0.17 和 0.15 μM[1]
FAK-IN-29 (0.3-3 μM;24 小时) 在 MDA-MB-231 细胞中诱导浓度依赖性凋亡[1]
FAK-IN-29 (0.3-3 μM;24 小时) 在 MDA-MB-231 细胞中显著抑制克隆形成[1]

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

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231
Concentration: 3 μM
Incubation Time: 24 h
Result: Caused a significant accumulation of MDA-MB-231 cells in the G2/M phase, with a corresponding decrease in the G0/G1 phase. The G2/M phase population increased from 10.4% to 35.7%, while the G0/G1 phase decreased from 68.3% to 45.2%.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231
Concentration: 0.3, 1, and 3 μM
Incubation Time: 24 h
Result: Induced apoptosis in a concentration-dependent manner. The total apoptotic rates were 5.62 %, 33.15 %, and 62.48 % at concentrations of 0.3, 1, and 3 μM, respectively.
体内研究
(In Vivo)

FAK-IN-29 (5-10 mg/kg,静脉注射, 14 天) 在 MDA-MB-231 肿瘤异种移植裸鼠模型中表现出强效的抗肿瘤活性,并具有良好的安全特性[1]

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

Animal Model: BALB/c nude mice (MDA-MB-231 tumor xenograft model)[1]
Dosage: 5 mg/kg, 10 mg/kg
Administration: i.v.
Result: Achieved 61.8% tumor growth inhibition in MDA-MB-231 xenograft models, comparable to Paclitaxel (HY-B0015) (54.8%) at 10 mg/kg.
Significantly reduced Tumor volumes in both 5 mg/kg and 10 mg/kg groups.
Caused no observable toxicity, and body weights and organ weights remained stable.
Caused no histopathological abnormalities.
分子量

502.54

Formula

C26H27FN8O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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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.

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产品名称:
FAK-IN-29
目录号:
HY-179679
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