标签归档：fak

FAK-IN-3

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK-IN-3 

FAK-IN-3 (Compound 36) 是粘着斑激酶 (FAK) 的有效抑制剂。FAK-IN-3不仅降低了PA-1细胞的迁移和侵袭，还降低了MMP-2和MMP-9的表达。FAK-IN-3 抑制肿瘤生长和转移，无明显不良反应。FAK-IN-3 具有研究卵巢癌的潜力。

FAK-IN-3

FAK-IN-3 Chemical Structure

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生物活性

FAK-IN-3 (Compound 36) is a potent inhibitor of focal adhesion kinase (FAK). FAK-IN-3 not only decreases migration and invasion of PA-1 cells, but also reduces expression of MMP-2 and MMP-9. FAK-IN-3 inhibits tumor growth and metastasis, and no obvious adverse effects. FAK-IN-3 has the potential for the research of ovarian cancer[1].

分子量

512.56

Formula

C28H28N6O4
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.
参考文献

  • [1]. Wei W, et al. Design, synthesis and biological evaluation of 7-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-2,3-dihydro-1H-inden-1-one derivatives as potent FAK inhibitors for the treatment of ovarian cancer. Eur J Med Chem. 2022;228:113978.

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FAK-IN-3

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK-IN-3 

FAK-IN-3 (Compound 36) 是粘着斑激酶 (FAK) 的有效抑制剂。FAK-IN-3不仅降低了PA-1细胞的迁移和侵袭，还降低了MMP-2和MMP-9的表达。FAK-IN-3 抑制肿瘤生长和转移，无明显不良反应。FAK-IN-3 具有研究卵巢癌的潜力。

FAK-IN-3

FAK-IN-3 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

FAK-IN-3 (Compound 36) is a potent inhibitor of focal adhesion kinase (FAK). FAK-IN-3 not only decreases migration and invasion of PA-1 cells, but also reduces expression of MMP-2 and MMP-9. FAK-IN-3 inhibits tumor growth and metastasis, and no obvious adverse effects. FAK-IN-3 has the potential for the research of ovarian cancer[1].

分子量

512.56

Formula

C28H28N6O4
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.
参考文献

  • [1]. Wei W, et al. Design, synthesis and biological evaluation of 7-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-2,3-dihydro-1H-inden-1-one derivatives as potent FAK inhibitors for the treatment of ovarian cancer. Eur J Med Chem. 2022;228:113978.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

FAK-IN-5

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK-IN-5 

FAK-IN-5 (Compound 8l) 是一种 FAK signaling 抑制剂。FAK-IN-5 诱导细胞凋亡(apoptosis) 和自噬 (autophagy)。

FAK-IN-5

FAK-IN-5 Chemical Structure

CAS No. : 2408317-70-2

规格 是否有货
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生物活性

FAK-IN-5 (Compound 8l) is a FAK signaling inhibitor. FAK-IN-5 induces cell apoptosis and autophagy[1].

体外研究
(In Vitro)

FAK-IN-5 (Compound 8l) (0-50 µM, 72 h) shows antiproliferative activity against cancer cells[1].
FAK-IN-5 (Compound 8l) causes cell detachment[1].
FAK-IN-5 (Compound 8l) (0-25 µM, 24 h) induces autophagy and apoptosis in HCT-116 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: K562, CEM, G361, MCF-7 and HCT-116
Concentration: 0-50 µM
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50 values of 6.3, 7.9, 6.3, 5.5 and 5.3 µM against K562, CEM, G361, MCF-7 and HCT-116 cells, respectively.

Western Blot Analysis[1]

Cell Line: HCT-116
Concentration: 1.25, 2.5, 5, 7, 10, 11, 17 and 25 µM
Incubation Time: 1, 3, 5, 7 and 24 h
Result: Caused the dephosphorylation of FAK, p130Cas and paxillin in a dose-dependent manner. The dephosphorylation of FAK at Y397 was observed at a much earlier time point. Detected the fragments of activated caspase-7 as well as the dose-dependent cleavage of poly (ADP-ribose) polymerase (PARP).

分子量

576.01

Formula

C29H29ClF3N3O4
CAS 号

2408317-70-2
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.
参考文献

  • [1]. Jorda R, et al. Novel modified leucine and phenylalanine dipeptides modulate viability and attachment of cancer cells. Eur J Med Chem. 2020 Feb 15;188:112036.

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FAK-IN-4

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK-IN-4 

FAK-IN-4 (Compound 7d) 是具有抗癌活性的潜在 FAK 抑制剂。FAK-IN-4 诱导细胞凋亡 (apoptosis)。

FAK-IN-4

FAK-IN-4 Chemical Structure

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生物活性

FAK-IN-4 (Compound 7d) is potential FAK inhibitor with anticancer activities. FAK-IN-4 induces cell apoptosis[1].

体外研究
(In Vitro)

FAK-IN-4 (Compound 7d) (0-200 μM, 72 h) shows antiproliferative activity against triple-negative breast cancer (TNBC) cells[1].
FAK-IN-4 (0-20 μM, 24 h) inhibits cell invasion and migration of MDA-MB-231 cells[1].
FAK-IN-4 (0-20 μM, 72 h) causes dose-dependent Y925 dephosphorylation of FAK, and induces apoptosis in MDA-MB-231 cells[1].
FAK-IN-4 inhibits the formation of focal adhesions (FAs) and stress fibers (SFs) in MDA-MB-231 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, MDA-MB-157, MDA-MB-453 and MCF10A
Concentration: 0.78, 1.56, 3.13, 5, 6.25, 100, 12.5, 25, 50, 100 and 200 μM
Incubation Time: 72 h
Result: Inhibited the growth of TNBC cells with IC50 values of 8.37, 12.09, 9.07 and 40.63 μM against MDA-MB-231, MDA-MB-157, MDA-MB-453 and MCF10A cells.

Cell Invasion Assay[1]

Cell Line: MDA-MB-231
Concentration: 5, 10 and 20 μM
Incubation Time: 24 h
Result: Significantly inhibited the invasion of MDA-MB-231 cells in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MDA-MB-231
Concentration: 5, 10 and 20 μM
Incubation Time: 72 h
Result: Caused an obvious dose-dependent Y925 dephosphorylation of FAK.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231
Concentration: 5, 10 and 20 μM
Incubation Time: 72 h
Result: Increased the percentage of apoptotic MDA-MB-231 cells ranging from 13.10% to 41.59% in a dose-dependent manner.

分子量

334.41

Formula

C20H22N4O
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.
参考文献

  • [1]. Fei Yang, et al. Discovery of novel chloropyramine-cinnamic acid hybrids as potential FAK inhibitors for intervention of metastatic triple-negative breast cancer. Bioorg Med Chem. 2022 Jul 15;66:116809.

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FAK PROTAC B5

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK PROTAC B5 

FAK PROTAC B5 (Compound B5) 是 FAK PROTAC 降解剂，IC50 值为14.9 nM。FAK PROTAC B5 具有很强的 FAK 降解活性，抗增殖活性，血浆稳定性。FAK PROTAC B5 抑制细胞迁移与侵袭。

FAK PROTAC B5

FAK PROTAC B5 Chemical Structure

CAS No. : 2471525-44-5

规格 是否有货
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250 mg   询价  
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生物活性

FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion[1].

IC50 & Target

IC50: 14.9 nM (FAK)[1]
体外研究
(In Vitro)

FAK PROTAC B5 (Compound B5) displays strong antiproliferative activity (IC50 = 0.14 ± 0.01 μM) against A549 cells[1].
FAK PROTAC B5 displays excellent FAK degradation activity (86.4% at 10 nM) and the degradation is realized through proteasome degradation pathway[1].
FAK PROTAC B5 (0-1.8 μM, 72 h) has the significant ability to inhibit the migration of A549 cells[1].
FAK PROTAC B5 (0-1.8 μM, 72 h) inhibits the invasion of A549 cells in a concentration-dependent manner[1].
FAK PROTAC B5 exhibits a moderate membrane permeability[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: A549
Concentration: 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 8 h
Result: Reduced the level of FAK protein in a dose-dependent manner. Displayed excellent FAK degradation activity (86.4% at 10 nM).

Cell Invasion Assay[1]

Cell Line: A549
Concentration: 0.20, 0.60 and 1.80 μM
Incubation Time: 72 h
Result: Significantly reduced the number of A549 cells in a concentration-dependent manner.

体内研究
(In Vivo)

FAK PROTAC B5 (Compound B5) possesses favorable plasma stability with the half-life value greater than 289.1 min[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

823.30

Formula

C41H43ClN10O7
CAS 号

2471525-44-5
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.
参考文献

  • [1]. Yin Sun, et al. Identification of novel and potent PROTACs targeting FAK for non-small cell lung cancer: Design, synthesis, and biological study. Eur J Med Chem. 2022 Apr 23;237:114373.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

FAK PROTAC B5

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK PROTAC B5 

FAK PROTAC B5 (Compound B5) 是 FAK PROTAC 降解剂，IC50 值为14.9 nM。FAK PROTAC B5 具有很强的 FAK 降解活性，抗增殖活性，血浆稳定性。FAK PROTAC B5 抑制细胞迁移与侵袭。

FAK PROTAC B5

FAK PROTAC B5 Chemical Structure

CAS No. : 2471525-44-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion[1].

IC50 & Target

IC50: 14.9 nM (FAK)[1]
体外研究
(In Vitro)

FAK PROTAC B5 (Compound B5) displays strong antiproliferative activity (IC50 = 0.14 ± 0.01 μM) against A549 cells[1].
FAK PROTAC B5 displays excellent FAK degradation activity (86.4% at 10 nM) and the degradation is realized through proteasome degradation pathway[1].
FAK PROTAC B5 (0-1.8 μM, 72 h) has the significant ability to inhibit the migration of A549 cells[1].
FAK PROTAC B5 (0-1.8 μM, 72 h) inhibits the invasion of A549 cells in a concentration-dependent manner[1].
FAK PROTAC B5 exhibits a moderate membrane permeability[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: A549
Concentration: 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 8 h
Result: Reduced the level of FAK protein in a dose-dependent manner. Displayed excellent FAK degradation activity (86.4% at 10 nM).

Cell Invasion Assay[1]

Cell Line: A549
Concentration: 0.20, 0.60 and 1.80 μM
Incubation Time: 72 h
Result: Significantly reduced the number of A549 cells in a concentration-dependent manner.

体内研究
(In Vivo)

FAK PROTAC B5 (Compound B5) possesses favorable plasma stability with the half-life value greater than 289.1 min[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

823.30

Formula

C41H43ClN10O7
CAS 号

2471525-44-5
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.
参考文献

  • [1]. Yin Sun, et al. Identification of novel and potent PROTACs targeting FAK for non-small cell lung cancer: Design, synthesis, and biological study. Eur J Med Chem. 2022 Apr 23;237:114373.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

FAK PROTAC B5

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK PROTAC B5 

FAK PROTAC B5 (Compound B5) 是 FAK PROTAC 降解剂，IC50 值为14.9 nM。FAK PROTAC B5 具有很强的 FAK 降解活性，抗增殖活性，血浆稳定性。FAK PROTAC B5 抑制细胞迁移与侵袭。

FAK PROTAC B5

FAK PROTAC B5 Chemical Structure

CAS No. : 2471525-44-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion[1].

IC50 & Target

IC50: 14.9 nM (FAK)[1]
体外研究
(In Vitro)

FAK PROTAC B5 (Compound B5) displays strong antiproliferative activity (IC50 = 0.14 ± 0.01 μM) against A549 cells[1].
FAK PROTAC B5 displays excellent FAK degradation activity (86.4% at 10 nM) and the degradation is realized through proteasome degradation pathway[1].
FAK PROTAC B5 (0-1.8 μM, 72 h) has the significant ability to inhibit the migration of A549 cells[1].
FAK PROTAC B5 (0-1.8 μM, 72 h) inhibits the invasion of A549 cells in a concentration-dependent manner[1].
FAK PROTAC B5 exhibits a moderate membrane permeability[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: A549
Concentration: 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 8 h
Result: Reduced the level of FAK protein in a dose-dependent manner. Displayed excellent FAK degradation activity (86.4% at 10 nM).

Cell Invasion Assay[1]

Cell Line: A549
Concentration: 0.20, 0.60 and 1.80 μM
Incubation Time: 72 h
Result: Significantly reduced the number of A549 cells in a concentration-dependent manner.

体内研究
(In Vivo)

FAK PROTAC B5 (Compound B5) possesses favorable plasma stability with the half-life value greater than 289.1 min[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

823.30

Formula

C41H43ClN10O7
CAS 号

2471525-44-5
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.
参考文献

  • [1]. Yin Sun, et al. Identification of novel and potent PROTACs targeting FAK for non-small cell lung cancer: Design, synthesis, and biological study. Eur J Med Chem. 2022 Apr 23;237:114373.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

FAK ligand-Linker Conjugate 1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK ligand-Linker Conjugate 1  纯度: 98.28%

FAK ligand-Linker Conjugate 1 包含靶蛋白 FAK 配体和 PROTAC linker，可募集 E3 连接酶 (如 VHL，CRBN，MDM2 和 IAP 等类型)。FAK ligand-Linker Conjugate 1 可广泛用于 PROTAC 介导的蛋白降解。

FAK ligand-Linker Conjugate 1

FAK ligand-Linker Conjugate 1 Chemical Structure

CAS No. : 2307461-45-4

规格 价格 是否有货 数量
1 mg ￥5500 In-stock
5 mg ￥9800 In-stock
10 mg ￥15000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

生物活性

FAK ligand-Linker Conjugate 1 incorporates a ligand for FAK, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). FAK ligand-Linker Conjugate 1 can be extensively used for PROTAC-mediated protein degradation[1].

分子量

583.58

Formula

C25H28F3N5O6S
CAS 号

2307461-45-4
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
参考文献

  • [1]. Cromm PM, et al. Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation. J Am Chem Soc. 2018 Dec 12;140(49):17019-17026.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PROTAC FAK degrader 1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PROTAC FAK degrader 1  纯度: 99.87%

PROTAC FAK degrader 1 是一种基于 von Hippel-Lindau E3 配体的粘附斑激酶 (FAK) 的有效选择性降解剂，IC50 为 6.5 nM，DC50 为 3 nM。

PROTAC FAK degrader 1

PROTAC FAK degrader 1 Chemical Structure

CAS No. : 2301916-69-6

规格 价格 是否有货 数量
1 mg ￥5500 In-stock
5 mg ￥9800 In-stock
10 mg ￥15000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

PROTAC FAK degrader 1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

PROTAC FAK degrader 1 is a selective and potent von Hippel-Lindau-based focal adhesion kinase (FAK) degrader with an IC50 of 6.5 nM, DC50 of 3 nM[1].

IC50 & Target

IC50: 6.5 nM (Focal adhesion kinase)
DC50: 3 nM (Focal adhesion kinase)[1]
分子量

996.13

Formula

C47H56F3N9O8S2
CAS 号

2301916-69-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 200 mg/mL (200.78 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0039 mL 5.0194 mL 10.0389 mL
5 mM 0.2008 mL 1.0039 mL 2.0078 mL
10 mM 0.1004 mL 0.5019 mL 1.0039 mL

*

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 (stored under nitrogen)。-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。

In Vivo:

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

  • 1.

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

    Solubility: ≥ 5 mg/mL (5.02 mM); Suspended solution

    此方案可获得 ≥ 5 mg/mL (5.02 mM，饱和度未知) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (5.02 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (5.02 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Cromm PM, et al. Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation. J Am Chem Soc. 2018 Dec 12;140(49):17019-17026.

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Y15(Synonyms: FAK Inhibitor 14)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Y15 (Synonyms: FAK Inhibitor 14) 纯度: 98.22%

Y15是一种有效，特异性的粘着斑激酶抑制剂 (FAK)，可抑制其自身磷酸化活性，降低癌细胞的活力，阻断肿瘤生长。

Y15(Synonyms: FAK Inhibitor 14)

Y15 Chemical Structure

CAS No. : 4506-66-5

规格 价格 是否有货 数量
10 mM * 1 mL in Water ￥440 In-stock
10 mg ￥400 In-stock
50 mg ￥850 In-stock
100 mg ￥1550 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Y15 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Cytoskeleton Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Targeted Diversity Library

生物活性

Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.

IC50 & Target

FAK[1]
体外研究
(In Vitro)

Y15 directly blocks autophosphorylation activity of FAK. Y15 inhibits Y397 phosphorylation of FAK starting at 0.1 μM in Panc-1 cells. At a dose of 100 μM, Y15 has the same or better inhibition as TAE226. Of note, total FAK is downregulated at higher doses of Y15. Y15 also blocks phosphorylation of the FAK downstream substrate, paxillin. Total paxillin is decreased at higher doses similar to FAK. Thus, Y15 inhibits FAK phosphorylation in a dose-dependent manner[1]. MTS assay is completed using a range of Y15 doses on all cell lines (TT, K1, BCPAP, and TPC1, respectively).Y15 inhibited cell viability in a dose-dependent manner across all thyroid cell lines evaluated. IC50 is 2.05, 5.74, 9.99, and 17.54 μM for TT, TPC1, BCPAP, and K1, respectively[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Nude mice bearing Panc si-ctrl xenografts are treated with TAE226, a dual FAK and IGF-1R tyrosine kinase inhibitor, to provide a reference for the antitumor effect of dual inhibition of FAK and IGF-1R. Without drug treatment, Panc si5-IGF-1R xenografts grew slower than Panc si-ctrl xenografts (Panc si5-IGF-1R/PBS vs. Panc si-ctrl/PBS), suggesting moderate tumor suppression by inhibiting the IGF-1R pathway only. Further inhibition of FAK activity by Y15 treatment suppresses the growth of Panc si5-IGF-1R xenografts more drastically (Panc si5-IGF-1R/PBS vs. Panc si5-IGF-1R/Y15). A similar antitumor effect is seen in Panc si-ctrl xenografts treated with TAE226 (Panc si5-IGF-1R/Y15 vs. Panc si-ctrl/TAE226). Mice demonstrates normal grooming and eating habits throughout the experiment[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

284.01

Formula

C6H14Cl4N4
CAS 号

4506-66-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

H2O : 50 mg/mL (176.05 mM; ultrasonic and warming and heat to 50°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5210 mL 17.6050 mL 35.2100 mL
5 mM 0.7042 mL 3.5210 mL 7.0420 mL
10 mM 0.3521 mL 1.7605 mL 3.5210 mL

*

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 (sealed storage, away from moisture)。-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。
参考文献

  • [1]. Hochwald SN, et al. A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle. 2009 Aug;8(15):2435-43.

    [2]. O’Brien S, et al. FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Oncotarget. 2014 Sep 15;5(17):7945-59.

    [3]. Zheng D, et al. A novel strategy to inhibit FAK and IGF-1R decreases growth of pancreatic cancer xenografts. Mol Carcinog. 2010 Feb;49(2):200-9.
Kinase Assay
[1]

10 μCi of [γ-32P]-ATP in a kinase buffer 20 mM HEPES, pH 7.4, 5 mM MgCl2, 5 mM MnCl2, 0.1 mM Na3VO4 with 0.1 μg of purified FAK protein are incubated in a kinase buffer with 10 μCi of [γ-32P]-ATP. The kinase reaction is performed for 5 minutes at room temperature and stopped by addition of 2× Laemmli buffer. Proteins are separated on a Ready SDS-10% PAGE gel, and the phosphorylated enolase is visualized by autoradiography[1]

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

The cells are treated with Y15 or TAE226 at different concentrations for 24 hours. The 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium compound from Promega Viability kit is added, and the cells are incubated at 37°C for 1-2 hours. The optical density on 96-plate is analyzed with a microplate reader at 490 nm to determine cell viability. In addition, cells are stained with trypan blue after 24 hours of treatment with Y15 and the percent of cells that stained positive are determined with a hemacytometer[1]

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Mice[3]
Six-week-old, female nude mice are used. 5×106 Panc si5-IGF-1R cells are mixed with matrigel and injected subcutaneously into the flank of athymic nude mice (day 0). Animals are randomly divided into two groups on day 7. One group (n=5) received Y15 (30 mg/kg) and the other received PBS as control treatment (n=5). For Panc si-ctrl xenografts, 5×106 Panc si-ctrl cells are mixed with matrigel and injected subcutaneously into the flank of nude mice. These animals are also randomly divided into two groups on day 7, and one group (n=5) received TAE226 (30 mg/kg), the other group received PBS (n=5) as control treatment. The drugs and PBS are administered through intraperitoneal injection in a total volume of 0.1 mL. Tumor sizes are measured every 3 or 4 d in length (mm)×width (mm) starting from day 10. Tumor volume is calculated as volume (cm3)= 1/2×length (cm)×width(cm)2.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Hochwald SN, et al. A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle. 2009 Aug;8(15):2435-43.

    [2]. O’Brien S, et al. FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Oncotarget. 2014 Sep 15;5(17):7945-59.

    [3]. Zheng D, et al. A novel strategy to inhibit FAK and IGF-1R decreases growth of pancreatic cancer xenografts. Mol Carcinog. 2010 Feb;49(2):200-9.

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FAK inhibitor 2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK inhibitor 2 

FAK inhibitor 2 是一种有效的粘着斑激酶 (FAK) 抑制剂，IC50 值为 0.07 nM，有抗肿瘤和抗血管生成活性。

FAK inhibitor 2

FAK inhibitor 2 Chemical Structure

CAS No. : 2354405-14-2

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

FAK inhibitor 2 is a potent focal adhesion kinase (FAK) inhibitor with an IC50  of 0.07 nM, with antitumor and anti-angiogenesis activities[1].

IC50 & Target

IC50: 0.07 nM (FAK)[1]
分子量

646.75

Formula

C29H33F3N8O2S2
CAS 号

2354405-14-2
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.
参考文献

  • [1]. Su Y, et al. Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel FAK inhibitors with antitumor and anti-angiogenesis activities. Eur J Med Chem. 2019 May 18;177:32-46.

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GSK215

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GSK215 

GSK215 是一种有效且具有选择性的 PROTAC 粘着斑激酶 (FAK) 降解剂。GSK215是由VHL E3连接酶粘合剂和FAK抑制剂VS-4718联合设计的。GSK215 诱导 FAK 快速而持久性的降解，对 FAK 水平产生长期影响，并显著降低药代动力学/药效学 (PK/PD)。

GSK215

GSK215 Chemical Structure

CAS No. : 2743427-26-9

规格 是否有货
5 mg 询价
10 mg 询价
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

生物活性

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect[1].

IC50 & Target

PROTAC; DC50: 1.3 nM (FAK)
体外研究
(In Vitro)

GSK215 (0.1-1000 nM; 2 hours) effectively increases the FAK degradation by >90% and determines a DC50 of 1.3 nM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 0.1-1000 nM
Incubation Time: 2 hours
Result: Increased the FAK degradation.

体内研究
(In Vivo)

GSK215 (8mg/kg; i.h.) treatment shows the Cmax and tmax values of 526 ng/mL and 0.33 hours, respectively[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CD1 mice (P878/881A)[1]
Dosage: 8 mg/kg
Administration: I.u.(Pharmacokinetic Analysis)
Result: The Cmax and tmax were 526 ng/mL and 0.33 hours, respectively.

分子量

985.13

Formula

C50H59F3N10O6S
CAS 号

2743427-26-9
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.
参考文献

  • [1]. Law RP, Nunes J, Chung CW, et al. Discovery and Characterisation of Highly Cooperative FAK-Degrading PROTACs [published online ahead of print, 2021 Aug 20]. Angew Chem Int Ed Engl. 2021;10.1002/anie.202109237.

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FAK inhibitor 5

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK inhibitor 5 

FAK inhibitor 5 (compound 2) 是新型的、FAK 的异构抑制剂，IC50 值在较低的μM 水平。

FAK inhibitor 5

FAK inhibitor 5 Chemical Structure

CAS No. : 1426683-30-8

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range[1].

IC50 & Target

1.6 μM (pre-incubation 5 min ATP 0.5 μM), 1.3 μM (pre-incubation 60 min ATP 0.5 μM), 3.0 μM (pre-incubation 5 min ATP 1000 μM), 1.0 μM (pre-incubation 60 min ATP 1000 μM).
体外研究
(In Vitro)

The binding interactions between FAK inhibitor 5 (compound 2) in the FAK allosteric site is mostly hydrophobic in nature. Exposure of the allosteric pocket by the dramatic movement of Ile547 is accompanied by an equally significant movement of Arg550 in toward the allosteric binding site, where it packs along the tricyclic core of compounds 2. Notably, the terminal ethylphenyl group of compounds 2 occupies the DFG-in pocket, thereby dislodging Phe565 and enabling the structural rearrangement of the activation loop and observed occlusion of the FAK active site[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

367.46

Formula

C20H21N3O2S
CAS 号

1426683-30-8
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.
参考文献

  • [1]. Iwatani M, et al. Discovery and characterization of novel allosteric FAK inhibitors. Eur J Med Chem. 2013 Mar;61:49-60.

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FAK inhibitor 5

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK inhibitor 5 

FAK inhibitor 5 (compound 2) 是新型的、FAK 的异构抑制剂，IC50 值在较低的μM 水平。

FAK inhibitor 5

FAK inhibitor 5 Chemical Structure

CAS No. : 1426683-30-8

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range[1].

IC50 & Target

1.6 μM (pre-incubation 5 min ATP 0.5 μM), 1.3 μM (pre-incubation 60 min ATP 0.5 μM), 3.0 μM (pre-incubation 5 min ATP 1000 μM), 1.0 μM (pre-incubation 60 min ATP 1000 μM).
体外研究
(In Vitro)

The binding interactions between FAK inhibitor 5 (compound 2) in the FAK allosteric site is mostly hydrophobic in nature. Exposure of the allosteric pocket by the dramatic movement of Ile547 is accompanied by an equally significant movement of Arg550 in toward the allosteric binding site, where it packs along the tricyclic core of compounds 2. Notably, the terminal ethylphenyl group of compounds 2 occupies the DFG-in pocket, thereby dislodging Phe565 and enabling the structural rearrangement of the activation loop and observed occlusion of the FAK active site[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

367.46

Formula

C20H21N3O2S
CAS 号

1426683-30-8
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.
参考文献

  • [1]. Iwatani M, et al. Discovery and characterization of novel allosteric FAK inhibitors. Eur J Med Chem. 2013 Mar;61:49-60.

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FAK inhibitor 5

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK inhibitor 5 

FAK inhibitor 5 (compound 2) 是新型的、FAK 的异构抑制剂，IC50 值在较低的μM 水平。

FAK inhibitor 5

FAK inhibitor 5 Chemical Structure

CAS No. : 1426683-30-8

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range[1].

IC50 & Target

1.6 μM (pre-incubation 5 min ATP 0.5 μM), 1.3 μM (pre-incubation 60 min ATP 0.5 μM), 3.0 μM (pre-incubation 5 min ATP 1000 μM), 1.0 μM (pre-incubation 60 min ATP 1000 μM).
体外研究
(In Vitro)

The binding interactions between FAK inhibitor 5 (compound 2) in the FAK allosteric site is mostly hydrophobic in nature. Exposure of the allosteric pocket by the dramatic movement of Ile547 is accompanied by an equally significant movement of Arg550 in toward the allosteric binding site, where it packs along the tricyclic core of compounds 2. Notably, the terminal ethylphenyl group of compounds 2 occupies the DFG-in pocket, thereby dislodging Phe565 and enabling the structural rearrangement of the activation loop and observed occlusion of the FAK active site[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

367.46

Formula

C20H21N3O2S
CAS 号

1426683-30-8
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.
参考文献

  • [1]. Iwatani M, et al. Discovery and characterization of novel allosteric FAK inhibitors. Eur J Med Chem. 2013 Mar;61:49-60.

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FAK inhibitor 6

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK inhibitor 6 

化合物26f不仅优化了有效抑制酶（IC50= 28.2 nM），也表现出相对较少的细胞毒性（IC50= 3.32 μM），并以剂量依赖性方式诱导MDA-MB-231细胞凋亡，有效阻断G0/G1期MDA-MB-231细胞。

FAK inhibitor 6

FAK inhibitor 6 Chemical Structure

规格 是否有货
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生物活性

Compound 26F not only optimized the effective inhibitory enzyme (ic50= 28.2 nm), but also showed relatively less cytotoxicity (ic50= 3.32 μ M) And induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in g0/g1 phase.

分子量

477.55

Formula

C25H24FN5O2S
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.
参考文献

  • [1]. Wang R,et al. Design, synthesis, biological evaluation and molecular docking study of novel thieno[3,2-d]pyrimidine derivatives as potent FAK inhibitors. Eur J Med Chem. 2020 Feb 15;188:112024.

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FAK-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK-IN-1 

FAK-IN-1 是一种具有抗癌活性的 FAK 抑制剂 (WO2020231726 (Example 27))。

FAK-IN-1

FAK-IN-1 Chemical Structure

CAS No. : 2553215-22-6

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

FAK-IN-1 is a FAK inhibitor with anticancer activities (WO2020231726 (Example 27))[1].

分子量

565.57

Formula

C24H26F3N7O4S
CAS 号

2553215-22-6
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.
参考文献

  • [1]. Nathanael Gray, et al. Small-molecule focal adhesion kinase (fak) inhibitors. WO2020231726A1.

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FAK-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK-IN-1 

FAK-IN-1 是一种具有抗癌活性的 FAK 抑制剂 (WO2020231726 (Example 27))。

FAK-IN-1

FAK-IN-1 Chemical Structure

CAS No. : 2553215-22-6

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

FAK-IN-1 is a FAK inhibitor with anticancer activities (WO2020231726 (Example 27))[1].

分子量

565.57

Formula

C24H26F3N7O4S
CAS 号

2553215-22-6
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.
参考文献

  • [1]. Nathanael Gray, et al. Small-molecule focal adhesion kinase (fak) inhibitors. WO2020231726A1.

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FAK-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK-IN-1 

FAK-IN-1 是一种具有抗癌活性的 FAK 抑制剂 (WO2020231726 (Example 27))。

FAK-IN-1

FAK-IN-1 Chemical Structure

CAS No. : 2553215-22-6

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

FAK-IN-1 is a FAK inhibitor with anticancer activities (WO2020231726 (Example 27))[1].

分子量

565.57

Formula

C24H26F3N7O4S
CAS 号

2553215-22-6
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.
参考文献

  • [1]. Nathanael Gray, et al. Small-molecule focal adhesion kinase (fak) inhibitors. WO2020231726A1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Y11

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Y11 

Y11 通过阻断 Y397 的磷酸化来抑制 FAK1的自身磷酸化，并抑制肿瘤生长。

Y11

Y11 Chemical Structure

CAS No. : 1086639-59-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

Y11 inhibits FAK1 autophosphorylation by blocking phosphorylation of Y397 and decreases tumor growth[1].

分子量

265.15

Formula

C8H17BrN4O
CAS 号

1086639-59-9
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.
参考文献

  • [1]. Golubovskaya VM, et al. A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the y397 site of focal adhesion kinase decreases tumor growth. J Med Chem. 2008 Dec 11;51(23):7405-16.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务