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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
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

发表于由
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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

发表于由
回复

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

PROTAC SOS1 degrader-2

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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。

PROTAC SOS1 degrader-2 

PROTAC SOS1 degrader-2 是一种有效的 PROTAC SOS1 降解剂。 PROTAC SOS1 Degrader-2 以剂量依赖性方式降低 pERK 和 RAS-GTP 的表达水平。PROTAC SOS1degrader-2 在体内显著抑制肿瘤生长。

PROTAC SOS1 degrader-2

PROTAC SOS1 degrader-2 Chemical Structure

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

PROTAC SOS1 degrader-2 is a potent PROTAC SOS1 degrader. PROTAC SOS1 degrader-2 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. PROTAC SOS1 degrader-2 significantly inhibits the tumor growth in vivo[1].

IC50 & Target[1]

K-RAS

 

体外研究
(In Vitro)

PROTAC SOS1 degrader-2 (compound 9d) (0.1, 1 µM) shows a potent SOSI degradation activity with an SOS1 protein degradation of 56.2 and 92.5% at 0.1 and 1 μM in NCI-H358 cells, respectively[1].
PROTAC SOS1 degrader-2 (24 h) degrades SOS1 in a dose- and time-dependent manner in NCI-H358 cells[1].
PROTAC SOS1 degrader-2 (9.8-2500 nM; 24 h) does not induce SOS2 and KRAS degradation in NCI-H358 cells[1].
PROTAC SOS1 degrader-2 (7.8-2000 nM; 24 h) decreases the expression of pERK and RAS-GTP level in NCI-H358 cells in a dose-dependent manner[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: NCI-H358 cells
Concentration: 7.8, 15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000 nM
Incubation Time: 24 h
Result: Showed a potent degradation activity with an EC50 of 98.4 nM in NCI-H358 cells.

RT-PCR[1]

Cell Line: NCI-H358 cells
Concentration: 1 µM
Incubation Time: 24, 48, 72 h
Result: Showed the SOS2 mRNA level remained constant during the incubation period.

Cell Proliferation Assay[1]

Cell Line: NCI-H358, MIA PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells
Concentration: 0-10000 nM
Incubation Time: 7 days
Result: Inhibited the cell growth with IC50s of 0.525, 0.218, 0.307, 0.115, 0.199, 0.232 µM (EC50s of 0.098, 0.255, 0.119, 0.104, 0.125, 0.022 µM)for NCI-H358, MIA PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells, respectively.

体内研究
(In Vivo)

PROTAC SOS1 degrader-2 (10, 20 mg/kg; i.p., daily for 21 days ) significantly inhibits the tumor growth in vivo with a good safety profile[1].

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

Animal Model: BALB/c nude mice (NCI-H358 tumor xenografts)[1]
Dosage: 10, 20 mg/kg
Administration: I.p.; daily, 21 days
Result: Significantly inhibited the tumor growth in vivo with a good safety profile.

分子量

1051.79

Formula

C57H76ClFN10O4S
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]. Zhou C,et al. Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations. J Med Chem. 2022; 65(5):3923-3942.

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 SOS1 degrader-2

发表于由
回复

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 SOS1 degrader-2 

PROTAC SOS1 degrader-2 是一种有效的 PROTAC SOS1 降解剂。 PROTAC SOS1 Degrader-2 以剂量依赖性方式降低 pERK 和 RAS-GTP 的表达水平。PROTAC SOS1degrader-2 在体内显著抑制肿瘤生长。

PROTAC SOS1 degrader-2

PROTAC SOS1 degrader-2 Chemical Structure

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

PROTAC SOS1 degrader-2 is a potent PROTAC SOS1 degrader. PROTAC SOS1 degrader-2 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. PROTAC SOS1 degrader-2 significantly inhibits the tumor growth in vivo[1].

IC50 & Target[1]

K-RAS

 

体外研究
(In Vitro)

PROTAC SOS1 degrader-2 (compound 9d) (0.1, 1 µM) shows a potent SOSI degradation activity with an SOS1 protein degradation of 56.2 and 92.5% at 0.1 and 1 μM in NCI-H358 cells, respectively[1].
PROTAC SOS1 degrader-2 (24 h) degrades SOS1 in a dose- and time-dependent manner in NCI-H358 cells[1].
PROTAC SOS1 degrader-2 (9.8-2500 nM; 24 h) does not induce SOS2 and KRAS degradation in NCI-H358 cells[1].
PROTAC SOS1 degrader-2 (7.8-2000 nM; 24 h) decreases the expression of pERK and RAS-GTP level in NCI-H358 cells in a dose-dependent manner[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: NCI-H358 cells
Concentration: 7.8, 15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000 nM
Incubation Time: 24 h
Result: Showed a potent degradation activity with an EC50 of 98.4 nM in NCI-H358 cells.

RT-PCR[1]

Cell Line: NCI-H358 cells
Concentration: 1 µM
Incubation Time: 24, 48, 72 h
Result: Showed the SOS2 mRNA level remained constant during the incubation period.

Cell Proliferation Assay[1]

Cell Line: NCI-H358, MIA PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells
Concentration: 0-10000 nM
Incubation Time: 7 days
Result: Inhibited the cell growth with IC50s of 0.525, 0.218, 0.307, 0.115, 0.199, 0.232 µM (EC50s of 0.098, 0.255, 0.119, 0.104, 0.125, 0.022 µM)for NCI-H358, MIA PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells, respectively.

体内研究
(In Vivo)

PROTAC SOS1 degrader-2 (10, 20 mg/kg; i.p., daily for 21 days ) significantly inhibits the tumor growth in vivo with a good safety profile[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 Model: BALB/c nude mice (NCI-H358 tumor xenografts)[1]
Dosage: 10, 20 mg/kg
Administration: I.p.; daily, 21 days
Result: Significantly inhibited the tumor growth in vivo with a good safety profile.

分子量

1051.79

Formula

C57H76ClFN10O4S
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]. Zhou C,et al. Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations. J Med Chem. 2022; 65(5):3923-3942.

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 SOS1 degrader-2

发表于由
回复

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 SOS1 degrader-2 

PROTAC SOS1 degrader-2 是一种有效的 PROTAC SOS1 降解剂。 PROTAC SOS1 Degrader-2 以剂量依赖性方式降低 pERK 和 RAS-GTP 的表达水平。PROTAC SOS1degrader-2 在体内显著抑制肿瘤生长。

PROTAC SOS1 degrader-2

PROTAC SOS1 degrader-2 Chemical Structure

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

PROTAC SOS1 degrader-2 is a potent PROTAC SOS1 degrader. PROTAC SOS1 degrader-2 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. PROTAC SOS1 degrader-2 significantly inhibits the tumor growth in vivo[1].

IC50 & Target[1]

K-RAS

 

体外研究
(In Vitro)

PROTAC SOS1 degrader-2 (compound 9d) (0.1, 1 µM) shows a potent SOSI degradation activity with an SOS1 protein degradation of 56.2 and 92.5% at 0.1 and 1 μM in NCI-H358 cells, respectively[1].
PROTAC SOS1 degrader-2 (24 h) degrades SOS1 in a dose- and time-dependent manner in NCI-H358 cells[1].
PROTAC SOS1 degrader-2 (9.8-2500 nM; 24 h) does not induce SOS2 and KRAS degradation in NCI-H358 cells[1].
PROTAC SOS1 degrader-2 (7.8-2000 nM; 24 h) decreases the expression of pERK and RAS-GTP level in NCI-H358 cells in a dose-dependent manner[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: NCI-H358 cells
Concentration: 7.8, 15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000 nM
Incubation Time: 24 h
Result: Showed a potent degradation activity with an EC50 of 98.4 nM in NCI-H358 cells.

RT-PCR[1]

Cell Line: NCI-H358 cells
Concentration: 1 µM
Incubation Time: 24, 48, 72 h
Result: Showed the SOS2 mRNA level remained constant during the incubation period.

Cell Proliferation Assay[1]

Cell Line: NCI-H358, MIA PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells
Concentration: 0-10000 nM
Incubation Time: 7 days
Result: Inhibited the cell growth with IC50s of 0.525, 0.218, 0.307, 0.115, 0.199, 0.232 µM (EC50s of 0.098, 0.255, 0.119, 0.104, 0.125, 0.022 µM)for NCI-H358, MIA PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells, respectively.

体内研究
(In Vivo)

PROTAC SOS1 degrader-2 (10, 20 mg/kg; i.p., daily for 21 days ) significantly inhibits the tumor growth in vivo with a good safety profile[1].

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

Animal Model: BALB/c nude mice (NCI-H358 tumor xenografts)[1]
Dosage: 10, 20 mg/kg
Administration: I.p.; daily, 21 days
Result: Significantly inhibited the tumor growth in vivo with a good safety profile.

分子量

1051.79

Formula

C57H76ClFN10O4S
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]. Zhou C,et al. Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations. J Med Chem. 2022; 65(5):3923-3942.

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 EGFR degrader 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。

PROTAC EGFR degrader 3 

PROTAC EGFR degrader 3 是一种有效的 PROTAC EGFR 降解剂。PROTAC EGFR degrader 3 对 H1975 和 HCC827 细胞具有优异的细胞活性和高选择性。PROTAC EGFR degrader 3 表明溶酶体参与了 EGFR 突变体的降解过程。

PROTAC EGFR degrader 3

PROTAC EGFR degrader 3 Chemical Structure

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

PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation[1].

体外研究
(In Vitro)

PROTAC EGFR degrader 3 (compound CP17) shows anti-proliferative activity of PROTACs with IC50s of 32 nM, 1.60 nM, >10000nM for H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) cells, respectively[1].
PROTAC EGFR degrader 3 (0, 10, 100, 1000, 10000 nM) exhibits poor cellular activity with IC50 of 481 nM, 669 nM for Ba/F3 (EGFRdel19/T790M/C797S) and Ba/F3 (EGFRL858/T790M/C797S) cells, respectively[1].
PROTAC EGFR degrader 3 (0-10000 nM) suppresses the proliferation of the PC9 (EGFRdel19/T790M/C797S) and H1975 (EGFRL858/T790M/C797S) cells, respectively[1].
PROTAC EGFR degrader 3 (30 nM; 0-72 h) decreases the expression level of EGFRL858/T790M after 8h, and degradation rate maximizes after 48 h[1].
PROTAC EGFR degrader 3 (0.3, 1, 3, 10, 100, 300 nM; 24, 48 h) induces the degradation of EGFRL858/T790M and EGFRdel19 with DC50s of 1.56 nM and 0.49 nM, respectively[1].
PROTAC EGFR degrader 3 (100, 1000 nM; 24 h) shows selective against mutant EGFR in the H1975 and HCC827 cells[1].
PROTAC EGFR degrader 3 (0.3, 1, 3, 10, 100, 300 nM; 24 h) effectively blocks EGFR singnal transduction, leading to cell proliferation inhibition[1].
PROTAC EGFR degrader 3 (30 nM) induces EGFR mutant degradation, and the lysosome is involved in the degradation process[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: H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) cells
Concentration:
Incubation Time: 72 h
Result: Exhibited anti-proliferative activity of PROTACs with IC50s of 32 nM, 1.60 nM, >10000nM for H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) cells, respectively.

Western Blot Analysis[1]

Cell Line: H1975, HCC827 cells
Concentration: 0.3, 1, 3, 10, 30 nM
Incubation Time: 24 h
Result: Remarkably decreased the phosphorylated EGFR, ERK, AKT in the H1975 and HCC827 cells.

分子量

1092.40

Formula

C60H77N13O5S
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]. Zhao HY, et al. Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. J Med Chem. 2022; 65(6):4709-4726.

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 EGFR degrader 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。

PROTAC EGFR degrader 3 

PROTAC EGFR degrader 3 是一种有效的 PROTAC EGFR 降解剂。PROTAC EGFR degrader 3 对 H1975 和 HCC827 细胞具有优异的细胞活性和高选择性。PROTAC EGFR degrader 3 表明溶酶体参与了 EGFR 突变体的降解过程。

PROTAC EGFR degrader 3

PROTAC EGFR degrader 3 Chemical Structure

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

PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation[1].

体外研究
(In Vitro)

PROTAC EGFR degrader 3 (compound CP17) shows anti-proliferative activity of PROTACs with IC50s of 32 nM, 1.60 nM, >10000nM for H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) cells, respectively[1].
PROTAC EGFR degrader 3 (0, 10, 100, 1000, 10000 nM) exhibits poor cellular activity with IC50 of 481 nM, 669 nM for Ba/F3 (EGFRdel19/T790M/C797S) and Ba/F3 (EGFRL858/T790M/C797S) cells, respectively[1].
PROTAC EGFR degrader 3 (0-10000 nM) suppresses the proliferation of the PC9 (EGFRdel19/T790M/C797S) and H1975 (EGFRL858/T790M/C797S) cells, respectively[1].
PROTAC EGFR degrader 3 (30 nM; 0-72 h) decreases the expression level of EGFRL858/T790M after 8h, and degradation rate maximizes after 48 h[1].
PROTAC EGFR degrader 3 (0.3, 1, 3, 10, 100, 300 nM; 24, 48 h) induces the degradation of EGFRL858/T790M and EGFRdel19 with DC50s of 1.56 nM and 0.49 nM, respectively[1].
PROTAC EGFR degrader 3 (100, 1000 nM; 24 h) shows selective against mutant EGFR in the H1975 and HCC827 cells[1].
PROTAC EGFR degrader 3 (0.3, 1, 3, 10, 100, 300 nM; 24 h) effectively blocks EGFR singnal transduction, leading to cell proliferation inhibition[1].
PROTAC EGFR degrader 3 (30 nM) induces EGFR mutant degradation, and the lysosome is involved in the degradation process[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 Proliferation Assay[1]

Cell Line: H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) cells
Concentration:
Incubation Time: 72 h
Result: Exhibited anti-proliferative activity of PROTACs with IC50s of 32 nM, 1.60 nM, >10000nM for H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) cells, respectively.

Western Blot Analysis[1]

Cell Line: H1975, HCC827 cells
Concentration: 0.3, 1, 3, 10, 30 nM
Incubation Time: 24 h
Result: Remarkably decreased the phosphorylated EGFR, ERK, AKT in the H1975 and HCC827 cells.

分子量

1092.40

Formula

C60H77N13O5S
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]. Zhao HY, et al. Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. J Med Chem. 2022; 65(6):4709-4726.

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 EGFR degrader 3

发表于由
回复

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 EGFR degrader 3 

PROTAC EGFR degrader 3 是一种有效的 PROTAC EGFR 降解剂。PROTAC EGFR degrader 3 对 H1975 和 HCC827 细胞具有优异的细胞活性和高选择性。PROTAC EGFR degrader 3 表明溶酶体参与了 EGFR 突变体的降解过程。

PROTAC EGFR degrader 3

PROTAC EGFR degrader 3 Chemical Structure

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

PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation[1].

体外研究
(In Vitro)

PROTAC EGFR degrader 3 (compound CP17) shows anti-proliferative activity of PROTACs with IC50s of 32 nM, 1.60 nM, >10000nM for H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) cells, respectively[1].
PROTAC EGFR degrader 3 (0, 10, 100, 1000, 10000 nM) exhibits poor cellular activity with IC50 of 481 nM, 669 nM for Ba/F3 (EGFRdel19/T790M/C797S) and Ba/F3 (EGFRL858/T790M/C797S) cells, respectively[1].
PROTAC EGFR degrader 3 (0-10000 nM) suppresses the proliferation of the PC9 (EGFRdel19/T790M/C797S) and H1975 (EGFRL858/T790M/C797S) cells, respectively[1].
PROTAC EGFR degrader 3 (30 nM; 0-72 h) decreases the expression level of EGFRL858/T790M after 8h, and degradation rate maximizes after 48 h[1].
PROTAC EGFR degrader 3 (0.3, 1, 3, 10, 100, 300 nM; 24, 48 h) induces the degradation of EGFRL858/T790M and EGFRdel19 with DC50s of 1.56 nM and 0.49 nM, respectively[1].
PROTAC EGFR degrader 3 (100, 1000 nM; 24 h) shows selective against mutant EGFR in the H1975 and HCC827 cells[1].
PROTAC EGFR degrader 3 (0.3, 1, 3, 10, 100, 300 nM; 24 h) effectively blocks EGFR singnal transduction, leading to cell proliferation inhibition[1].
PROTAC EGFR degrader 3 (30 nM) induces EGFR mutant degradation, and the lysosome is involved in the degradation process[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: H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) cells
Concentration:
Incubation Time: 72 h
Result: Exhibited anti-proliferative activity of PROTACs with IC50s of 32 nM, 1.60 nM, >10000nM for H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) cells, respectively.

Western Blot Analysis[1]

Cell Line: H1975, HCC827 cells
Concentration: 0.3, 1, 3, 10, 30 nM
Incubation Time: 24 h
Result: Remarkably decreased the phosphorylated EGFR, ERK, AKT in the H1975 and HCC827 cells.

分子量

1092.40

Formula

C60H77N13O5S
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]. Zhao HY, et al. Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. J Med Chem. 2022; 65(6):4709-4726.

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 Axl Degrader 2

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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。

PROTAC Axl Degrader 2 

PROTAC Axl Degrader 2 是一种有效的选择性 PROTAC Axl 降解剂，IC50 为 1.61 µM。PROTAC Axl Degrader 2 显示出体外抗增殖活性、抗迁移活性。PROTAC Axl Degrader 2 诱导巨泡式细胞死亡 (mehuosis)。

PROTAC Axl Degrader 2

PROTAC Axl Degrader 2 Chemical Structure

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

PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC50 of 1.61 µM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis[1].

IC50 & Target

IC50: 1.61 µM (AXL)[1]
体外研究
(In Vitro)

PROTAC Axl Degrader 2 (compound 20) (72 h) shows anti-proliferation activity with IC50s of 6.23 µM, 2.06 µM, for MDA-MB-231, 4T1 cells, respectively[1].
PROTAC Axl Degrader 2 (0.5, 2 µM; 24, 48 h) decreases the abundance of AXL in MDA-MB-231 cells[1].
PROTAC Axl Degrader 2 (1, 2 µM) reduces the expression of AXL, can be restored in the presence of EPO (epoxymycin)[1].
PROTAC Axl Degrader 2 (1, 10 µM; 48 h) significantly inhibits the migration in MDA-MB-231 and 4T1 cells[1].
PROTAC Axl Degrader 2 (0.5 µM) induces cytoplasmic vacuolation (methuosis) in MDA-MB-231 and 4T1 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, 4T1, GES-1, MCF-10A cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferation activity with IC50s of 6.23 µM, 2.06 µM, for MDA-MB-231, 4T1 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 2 µM
Incubation Time: 24, 48 h
Result: Decreased AXL abundance in MDA-MB-231 cells.

体内研究
(In Vivo)

PROTAC Axl Degrader 2 (25 mg/kg, i.p.) dose not induce systemic toxicity[1].
PROTAC Axl Degrader 2 (20 mg/kg for o.p.; 2 mg/kg for i.v.) shows an oral bioavailability of 7.80%[1].
Pharmacokinetic Parameters of PROTAC Axl Degrader 2 in 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1].

Cmds Rout Dose (mg/kg) AUC0-t (ng·h/mL) Cmax (ng/mL) Tmax (h) T1/2 (h) CL (L/h/kg) BA (%)
20 i.v. 2 7581.3 279 0.82 1.18 0.72 –
p.o. 20 3592.1 144 2.25 4.43 – 7.80

6 weeks, 180-220g, male Sprague-Dawley (SD) rats; 20 mg/kg for o.p.; 2 mg/kg for i.v.

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

Animal Model: Female balb/c nude mice (MDA-MB-231 xenografts)[1]
Dosage: 25 mg/kg
Administration: Intraperitoneal injection
Result: Did not induce systemic toxicity.
Animal Model: 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1]
Dosage:
Administration: 20 mg/kg for o.p.; 2 mg/kg for i.v.
Result: Showed an oral bioavailability of 7.80%.

分子量

713.79

Formula

C38H39N11O4
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]. Shi W, et al. Structure-based discovery of receptor tyrosine kinase AXL degraders with excellent anti-tumor activity by selectively degrading AXL and inducing methuosis. Eur J Med Chem. 2022; 234:114253.

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 Axl Degrader 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。

PROTAC Axl Degrader 1 

PROTAC Axl Degrader 1 是一种有效的选择性 PROTAC Axl 降解剂，IC50 为 0.92 µM。PROTAC Axl Degrader 1 显示出体外抗增殖活性、抗迁移活性。PROTAC Axl Degrader 1 诱导巨泡式细胞死亡。

PROTAC Axl Degrader 1

PROTAC Axl Degrader 1 Chemical Structure

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

PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 µM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis[1].

IC50 & Target

IC50: 0.92 µM (AXL)[1]
体外研究
(In Vitro)

PROTAC Axl Degrader 1 (compound 22) (72 h) shows anti-proliferation activity with IC50s of 10.34 µM, 5.53 µM, for MDA-MB-231, 4T1 cells, respectively[1].
PROTAC Axl Degrader 1 (0.5, 2 µM; 24, 48 h) decreases the abundance of AXL in MDA-MB-231 cells[1].
PROTAC Axl Degrader 1 (1, 2 µM) reduces the expression of AXL, could be restored in the presence of EPO (epoxymycin)[1].
PROTAC Axl Degrader 1 (1, 10 µM; 48 h) significantly inhibits the migration in MDA-MB-231 and 4T1 cells[1].
PROTAC Axl Degrader 1 (0.5 µM) induces cytoplasmic vacuolation (methuosis) in MDA-MB-231 and 4T1 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, 4T1, GES-1, MCF-10A cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferation activity with IC50s of 10.34 µM, 5.53 µM, for MDA-MB-231, 4T1 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 2 µM
Incubation Time: 24, 48 h
Result: Decreased AXL abundance in MDA-MB-231 cells.

体内研究
(In Vivo)

PROTAC Axl Degrader 1 (25 mg/kg, i.p.) dose not induce systemic toxicity[1].
PROTAC Axl Degrader 1 (20 mg/kg for o.p.; 2 mg/kg for i.v.) shows an oral bioavailability of 4.93%[1].
Pharmacokinetic Parameters of PROTAC Axl Degrader 1 in 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1].

Cmds Rout Dose (mg/kg) AUC0-t (ng·h/mL) Cmax (ng/mL) Tmax (h) T1/2 (h) CL (L/h/kg) BA (%)
22 i.v. 2 2933.4 166 0.54 0.72 0.68 –
p.o. 20 864.7 92 1.89 2.37 – 4.93

6 weeks, 180-220g, male Sprague-Dawley (SD) rats; 20 mg/kg for o.p.; 2 mg/kg for i.v.[1].

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

741.84

Formula

C40H43N11O4
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]. Shi W, et al. Structure-based discovery of receptor tyrosine kinase AXL degraders with excellent anti-tumor activity by selectively degrading AXL and inducing methuosis. Eur J Med Chem. 2022; 234:114253.

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 Axl Degrader 2

发表于由
回复

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 Axl Degrader 2 

PROTAC Axl Degrader 2 是一种有效的选择性 PROTAC Axl 降解剂，IC50 为 1.61 µM。PROTAC Axl Degrader 2 显示出体外抗增殖活性、抗迁移活性。PROTAC Axl Degrader 2 诱导巨泡式细胞死亡 (mehuosis)。

PROTAC Axl Degrader 2

PROTAC Axl Degrader 2 Chemical Structure

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

PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC50 of 1.61 µM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis[1].

IC50 & Target

IC50: 1.61 µM (AXL)[1]
体外研究
(In Vitro)

PROTAC Axl Degrader 2 (compound 20) (72 h) shows anti-proliferation activity with IC50s of 6.23 µM, 2.06 µM, for MDA-MB-231, 4T1 cells, respectively[1].
PROTAC Axl Degrader 2 (0.5, 2 µM; 24, 48 h) decreases the abundance of AXL in MDA-MB-231 cells[1].
PROTAC Axl Degrader 2 (1, 2 µM) reduces the expression of AXL, can be restored in the presence of EPO (epoxymycin)[1].
PROTAC Axl Degrader 2 (1, 10 µM; 48 h) significantly inhibits the migration in MDA-MB-231 and 4T1 cells[1].
PROTAC Axl Degrader 2 (0.5 µM) induces cytoplasmic vacuolation (methuosis) in MDA-MB-231 and 4T1 cells[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 Proliferation Assay[1]

Cell Line: MDA-MB-231, 4T1, GES-1, MCF-10A cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferation activity with IC50s of 6.23 µM, 2.06 µM, for MDA-MB-231, 4T1 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 2 µM
Incubation Time: 24, 48 h
Result: Decreased AXL abundance in MDA-MB-231 cells.

体内研究
(In Vivo)

PROTAC Axl Degrader 2 (25 mg/kg, i.p.) dose not induce systemic toxicity[1].
PROTAC Axl Degrader 2 (20 mg/kg for o.p.; 2 mg/kg for i.v.) shows an oral bioavailability of 7.80%[1].
Pharmacokinetic Parameters of PROTAC Axl Degrader 2 in 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1].

Cmds Rout Dose (mg/kg) AUC0-t (ng·h/mL) Cmax (ng/mL) Tmax (h) T1/2 (h) CL (L/h/kg) BA (%)
20 i.v. 2 7581.3 279 0.82 1.18 0.72 –
p.o. 20 3592.1 144 2.25 4.43 – 7.80

6 weeks, 180-220g, male Sprague-Dawley (SD) rats; 20 mg/kg for o.p.; 2 mg/kg for i.v.

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 Model: Female balb/c nude mice (MDA-MB-231 xenografts)[1]
Dosage: 25 mg/kg
Administration: Intraperitoneal injection
Result: Did not induce systemic toxicity.
Animal Model: 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1]
Dosage:
Administration: 20 mg/kg for o.p.; 2 mg/kg for i.v.
Result: Showed an oral bioavailability of 7.80%.

分子量

713.79

Formula

C38H39N11O4
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]. Shi W, et al. Structure-based discovery of receptor tyrosine kinase AXL degraders with excellent anti-tumor activity by selectively degrading AXL and inducing methuosis. Eur J Med Chem. 2022; 234:114253.

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 Axl Degrader 2

发表于由
回复

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 Axl Degrader 2 

PROTAC Axl Degrader 2 是一种有效的选择性 PROTAC Axl 降解剂，IC50 为 1.61 µM。PROTAC Axl Degrader 2 显示出体外抗增殖活性、抗迁移活性。PROTAC Axl Degrader 2 诱导巨泡式细胞死亡 (mehuosis)。

PROTAC Axl Degrader 2

PROTAC Axl Degrader 2 Chemical Structure

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

PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC50 of 1.61 µM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis[1].

IC50 & Target

IC50: 1.61 µM (AXL)[1]
体外研究
(In Vitro)

PROTAC Axl Degrader 2 (compound 20) (72 h) shows anti-proliferation activity with IC50s of 6.23 µM, 2.06 µM, for MDA-MB-231, 4T1 cells, respectively[1].
PROTAC Axl Degrader 2 (0.5, 2 µM; 24, 48 h) decreases the abundance of AXL in MDA-MB-231 cells[1].
PROTAC Axl Degrader 2 (1, 2 µM) reduces the expression of AXL, can be restored in the presence of EPO (epoxymycin)[1].
PROTAC Axl Degrader 2 (1, 10 µM; 48 h) significantly inhibits the migration in MDA-MB-231 and 4T1 cells[1].
PROTAC Axl Degrader 2 (0.5 µM) induces cytoplasmic vacuolation (methuosis) in MDA-MB-231 and 4T1 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, 4T1, GES-1, MCF-10A cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferation activity with IC50s of 6.23 µM, 2.06 µM, for MDA-MB-231, 4T1 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 2 µM
Incubation Time: 24, 48 h
Result: Decreased AXL abundance in MDA-MB-231 cells.

体内研究
(In Vivo)

PROTAC Axl Degrader 2 (25 mg/kg, i.p.) dose not induce systemic toxicity[1].
PROTAC Axl Degrader 2 (20 mg/kg for o.p.; 2 mg/kg for i.v.) shows an oral bioavailability of 7.80%[1].
Pharmacokinetic Parameters of PROTAC Axl Degrader 2 in 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1].

Cmds Rout Dose (mg/kg) AUC0-t (ng·h/mL) Cmax (ng/mL) Tmax (h) T1/2 (h) CL (L/h/kg) BA (%)
20 i.v. 2 7581.3 279 0.82 1.18 0.72 –
p.o. 20 3592.1 144 2.25 4.43 – 7.80

6 weeks, 180-220g, male Sprague-Dawley (SD) rats; 20 mg/kg for o.p.; 2 mg/kg for i.v.

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

Animal Model: Female balb/c nude mice (MDA-MB-231 xenografts)[1]
Dosage: 25 mg/kg
Administration: Intraperitoneal injection
Result: Did not induce systemic toxicity.
Animal Model: 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1]
Dosage:
Administration: 20 mg/kg for o.p.; 2 mg/kg for i.v.
Result: Showed an oral bioavailability of 7.80%.

分子量

713.79

Formula

C38H39N11O4
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]. Shi W, et al. Structure-based discovery of receptor tyrosine kinase AXL degraders with excellent anti-tumor activity by selectively degrading AXL and inducing methuosis. Eur J Med Chem. 2022; 234:114253.

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 Axl Degrader 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。

PROTAC Axl Degrader 1 

PROTAC Axl Degrader 1 是一种有效的选择性 PROTAC Axl 降解剂，IC50 为 0.92 µM。PROTAC Axl Degrader 1 显示出体外抗增殖活性、抗迁移活性。PROTAC Axl Degrader 1 诱导巨泡式细胞死亡。

PROTAC Axl Degrader 1

PROTAC Axl Degrader 1 Chemical Structure

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

PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 µM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis[1].

IC50 & Target

IC50: 0.92 µM (AXL)[1]
体外研究
(In Vitro)

PROTAC Axl Degrader 1 (compound 22) (72 h) shows anti-proliferation activity with IC50s of 10.34 µM, 5.53 µM, for MDA-MB-231, 4T1 cells, respectively[1].
PROTAC Axl Degrader 1 (0.5, 2 µM; 24, 48 h) decreases the abundance of AXL in MDA-MB-231 cells[1].
PROTAC Axl Degrader 1 (1, 2 µM) reduces the expression of AXL, could be restored in the presence of EPO (epoxymycin)[1].
PROTAC Axl Degrader 1 (1, 10 µM; 48 h) significantly inhibits the migration in MDA-MB-231 and 4T1 cells[1].
PROTAC Axl Degrader 1 (0.5 µM) induces cytoplasmic vacuolation (methuosis) in MDA-MB-231 and 4T1 cells[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 Proliferation Assay[1]

Cell Line: MDA-MB-231, 4T1, GES-1, MCF-10A cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferation activity with IC50s of 10.34 µM, 5.53 µM, for MDA-MB-231, 4T1 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 2 µM
Incubation Time: 24, 48 h
Result: Decreased AXL abundance in MDA-MB-231 cells.

体内研究
(In Vivo)

PROTAC Axl Degrader 1 (25 mg/kg, i.p.) dose not induce systemic toxicity[1].
PROTAC Axl Degrader 1 (20 mg/kg for o.p.; 2 mg/kg for i.v.) shows an oral bioavailability of 4.93%[1].
Pharmacokinetic Parameters of PROTAC Axl Degrader 1 in 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1].

Cmds Rout Dose (mg/kg) AUC0-t (ng·h/mL) Cmax (ng/mL) Tmax (h) T1/2 (h) CL (L/h/kg) BA (%)
22 i.v. 2 2933.4 166 0.54 0.72 0.68 –
p.o. 20 864.7 92 1.89 2.37 – 4.93

6 weeks, 180-220g, male Sprague-Dawley (SD) rats; 20 mg/kg for o.p.; 2 mg/kg for i.v.[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

741.84

Formula

C40H43N11O4
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]. Shi W, et al. Structure-based discovery of receptor tyrosine kinase AXL degraders with excellent anti-tumor activity by selectively degrading AXL and inducing methuosis. Eur J Med Chem. 2022; 234:114253.

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 Axl Degrader 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。

PROTAC Axl Degrader 1 

PROTAC Axl Degrader 1 是一种有效的选择性 PROTAC Axl 降解剂，IC50 为 0.92 µM。PROTAC Axl Degrader 1 显示出体外抗增殖活性、抗迁移活性。PROTAC Axl Degrader 1 诱导巨泡式细胞死亡。

PROTAC Axl Degrader 1

PROTAC Axl Degrader 1 Chemical Structure

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

PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 µM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis[1].

IC50 & Target

IC50: 0.92 µM (AXL)[1]
体外研究
(In Vitro)

PROTAC Axl Degrader 1 (compound 22) (72 h) shows anti-proliferation activity with IC50s of 10.34 µM, 5.53 µM, for MDA-MB-231, 4T1 cells, respectively[1].
PROTAC Axl Degrader 1 (0.5, 2 µM; 24, 48 h) decreases the abundance of AXL in MDA-MB-231 cells[1].
PROTAC Axl Degrader 1 (1, 2 µM) reduces the expression of AXL, could be restored in the presence of EPO (epoxymycin)[1].
PROTAC Axl Degrader 1 (1, 10 µM; 48 h) significantly inhibits the migration in MDA-MB-231 and 4T1 cells[1].
PROTAC Axl Degrader 1 (0.5 µM) induces cytoplasmic vacuolation (methuosis) in MDA-MB-231 and 4T1 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, 4T1, GES-1, MCF-10A cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferation activity with IC50s of 10.34 µM, 5.53 µM, for MDA-MB-231, 4T1 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 2 µM
Incubation Time: 24, 48 h
Result: Decreased AXL abundance in MDA-MB-231 cells.

体内研究
(In Vivo)

PROTAC Axl Degrader 1 (25 mg/kg, i.p.) dose not induce systemic toxicity[1].
PROTAC Axl Degrader 1 (20 mg/kg for o.p.; 2 mg/kg for i.v.) shows an oral bioavailability of 4.93%[1].
Pharmacokinetic Parameters of PROTAC Axl Degrader 1 in 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1].

Cmds Rout Dose (mg/kg) AUC0-t (ng·h/mL) Cmax (ng/mL) Tmax (h) T1/2 (h) CL (L/h/kg) BA (%)
22 i.v. 2 2933.4 166 0.54 0.72 0.68 –
p.o. 20 864.7 92 1.89 2.37 – 4.93

6 weeks, 180-220g, male Sprague-Dawley (SD) rats; 20 mg/kg for o.p.; 2 mg/kg for i.v.[1].

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

741.84

Formula

C40H43N11O4
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]. Shi W, et al. Structure-based discovery of receptor tyrosine kinase AXL degraders with excellent anti-tumor activity by selectively degrading AXL and inducing methuosis. Eur J Med Chem. 2022; 234:114253.

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 TTK degrader-2

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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。

PROTAC TTK degrader-2 

PROTAC TTK degrader-2 是一种有效的 TTK (苏氨酸酪氨酸激酶) PROTAC 降解剂，在 COLO-205 和 HCT-116 细胞中的 DC50 值分别为 3.1 和 12.4 nM。PROTAC TTK degrader-2 在 COLO-205 人结直肠癌细胞异种移植小鼠模型中显示出靶向降解和抗癌效果。

PROTAC TTK degrader-2

PROTAC TTK degrader-2 Chemical Structure

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

PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells[1].

IC50 & Target

DC50: 3.1 nM (TTK) in COLO-205, 12.4 nM (TTK) in HCT-116[1]
体外研究
(In Vitro)

PROTAC TTK degrader-2 (compound 8j) (0-10 μM, 96 h) inhibits cancer cell proliferation[1].
PROTAC TTK degrader-2 (5 and 50 nM, 6 h) induces degradation of TTK protein in a dose-dependent manner[1].

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

Cell Proliferation Assay

Cell Line: COLO-205 and HCT-116 cells[1]
Concentration: 0-10 μM
Incubation Time: 96 h
Result: Inhibited the growth of COLO-205 cancer cells with an IC50 of 0.2 μM.

Western Blot Analysis

Cell Line: COLO-205, HCT-116 LOVO, HCT-8, and HCT-29 human colon cancer cell lines[1]
Concentration: 5, 50 nM
Incubation Time: 6 h
Result: Induced degradation of TTK protein in a dose-dependent manner.

体内研究
(In Vivo)

PROTAC TTK degrader-2 (8j) (10 mg/kg, IP, single) demonstrates reasonable pharmacokinetics profiles[1].
PROTAC TTK degrader-2 (10, 20 mg/kg, IP, once daily for 16 days) significantly reduces the TTK protein levels, and exhibits tumor-growth inhibition[1].
Pharmacokinetic Parameters of PROTAC TTK degrader-2 in male SD rats[1].

8j
AUC (ng/mL*h) 2333
T1/2 (h) 3.2

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

Animal Model: Male SD rats (, three animals per group)[1]
Dosage: 10 mg/kg, dissolved in mixed solvents (5% 20 mg/mL DMSO stock, 30% PG, 30% PEG400, and 35% Saline)
Administration: IP, single (Pharmacokinetic Analysis)
Result: Demonstrated reasonable pharmacokinetics profiles.
Animal Model: Male CB17-SCID mice (xenograft mouse model of COLO-205 cells)[1]
Dosage: 10, 20 mg/kg
Administration: IP, once daily for 16 days
Result: Significantly reduced the TTK protein levels in animal tumor tissues, exhibited tumor-growth inhibition value of 36.7% upon 20 mg/kg dosing, did not cause a significant body weight loss of the animal.

分子量

884.03

Formula

C49H57N9O7
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]. Lu J, Huang Y, Huang J, et al. Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders. J Med Chem. 2022;65(3):2313-2328.

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 TTK degrader-1

发表于由
回复

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 TTK degrader-1 

PROTAC TTK degrader-1 是一种有效的 TTK (苏氨酸酪氨酸激酶) PROTAC 降解剂，在 COLO-205 和 HCT-116 细胞中的 DC50 值分别为 1.7 和 5.8 nM。PROTAC TTK degrader-1 在 COLO-205 人结直肠癌细胞异种移植小鼠模型中显示出靶向降解和抗癌效果。

PROTAC TTK degrader-1

PROTAC TTK degrader-1 Chemical Structure

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

PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells[1].

IC50 & Target

DC50: 1.7 nM (TTK) in COLO-205, 5.8 nM (TTK) in HCT-116[1]
体外研究
(In Vitro)

PROTAC TTK degrader-1 (compound 8e) (0-10 μM, 96 h) inhibits cancer cell proliferation[1].
PROTAC TTK degrader-1 (5 and 50 nM, 6 h) induces degradation of TTK protein in a dose-dependent manner[1].

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

Cell Proliferation Assay

Cell Line: COLO-205 and HCT-116 cells[1]
Concentration: 0-10 μM
Incubation Time: 96 h
Result: Inhibited the growth of COLO-205 cancer cells with an IC50 of 0.1 μM.

Western Blot Analysis

Cell Line: COLO-205, HCT-116 LOVO, HCT-8, and HCT-29 human colon cancer cell lines[1]
Concentration: 5, 50 nM
Incubation Time: 6 h
Result: Induced degradation of TTK protein in a dose-dependent manner.

体内研究
(In Vivo)

PROTAC TTK degrader-1 (10 mg/kg, IP, single) demonstrates reasonable pharmacokinetics profiles[1].
PROTAC TTK degrader-1 (10, 20 mg/kg, IP, once daily for 16 days) significantly reduces the TTK protein levels, and exhibits tumor-growth inhibition[1].
Pharmacokinetic Parameters of PROTAC TTK degrader-1 in male SD rats[1].

8e
AUC (ng/mL*h) 2235
T1/2 (h) 4.3

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

Animal Model: Male SD rats[1]
Dosage: 10 mg/kg, dissolved in mixed solvents (5% 20 mg/mL DMSO stock, 30% PG, 30% PEG400, and 35% Saline)
Administration: IP, single (Pharmacokinetic Analysis)
Result: Demonstrated reasonable pharmacokinetics profiles.
Animal Model: Male CB17-SCID mice (bearing COLO-205 tumor xenografts)[1]
Dosage: 10, 20 mg/kg
Administration: IP, once daily for 16 days
Result: Significantly reduced the TTK protein levels in animal tumor tissues, exhibited tumor-growth inhibition value of 46.0% upon 20 mg/kg dosing, did not cause a significant body weight loss of the animal.

分子量

855.98

Formula

C47H53N9O7
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]. Lu J, Huang Y, Huang J, et al. Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders. J Med Chem. 2022;65(3):2313-2328.

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 TTK degrader-2

发表于由
回复

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 TTK degrader-2 

PROTAC TTK degrader-2 是一种有效的 TTK (苏氨酸酪氨酸激酶) PROTAC 降解剂，在 COLO-205 和 HCT-116 细胞中的 DC50 值分别为 3.1 和 12.4 nM。PROTAC TTK degrader-2 在 COLO-205 人结直肠癌细胞异种移植小鼠模型中显示出靶向降解和抗癌效果。

PROTAC TTK degrader-2

PROTAC TTK degrader-2 Chemical Structure

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

PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells[1].

IC50 & Target

DC50: 3.1 nM (TTK) in COLO-205, 12.4 nM (TTK) in HCT-116[1]
体外研究
(In Vitro)

PROTAC TTK degrader-2 (compound 8j) (0-10 μM, 96 h) inhibits cancer cell proliferation[1].
PROTAC TTK degrader-2 (5 and 50 nM, 6 h) induces degradation of TTK protein in a dose-dependent manner[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 Proliferation Assay

Cell Line: COLO-205 and HCT-116 cells[1]
Concentration: 0-10 μM
Incubation Time: 96 h
Result: Inhibited the growth of COLO-205 cancer cells with an IC50 of 0.2 μM.

Western Blot Analysis

Cell Line: COLO-205, HCT-116 LOVO, HCT-8, and HCT-29 human colon cancer cell lines[1]
Concentration: 5, 50 nM
Incubation Time: 6 h
Result: Induced degradation of TTK protein in a dose-dependent manner.

体内研究
(In Vivo)

PROTAC TTK degrader-2 (8j) (10 mg/kg, IP, single) demonstrates reasonable pharmacokinetics profiles[1].
PROTAC TTK degrader-2 (10, 20 mg/kg, IP, once daily for 16 days) significantly reduces the TTK protein levels, and exhibits tumor-growth inhibition[1].
Pharmacokinetic Parameters of PROTAC TTK degrader-2 in male SD rats[1].

8j
AUC (ng/mL*h) 2333
T1/2 (h) 3.2

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.

Animal Model: Male SD rats (, three animals per group)[1]
Dosage: 10 mg/kg, dissolved in mixed solvents (5% 20 mg/mL DMSO stock, 30% PG, 30% PEG400, and 35% Saline)
Administration: IP, single (Pharmacokinetic Analysis)
Result: Demonstrated reasonable pharmacokinetics profiles.
Animal Model: Male CB17-SCID mice (xenograft mouse model of COLO-205 cells)[1]
Dosage: 10, 20 mg/kg
Administration: IP, once daily for 16 days
Result: Significantly reduced the TTK protein levels in animal tumor tissues, exhibited tumor-growth inhibition value of 36.7% upon 20 mg/kg dosing, did not cause a significant body weight loss of the animal.

分子量

884.03

Formula

C49H57N9O7
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]. Lu J, Huang Y, Huang J, et al. Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders. J Med Chem. 2022;65(3):2313-2328.

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 TTK degrader-1

发表于由
回复

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 TTK degrader-1 

PROTAC TTK degrader-1 是一种有效的 TTK (苏氨酸酪氨酸激酶) PROTAC 降解剂，在 COLO-205 和 HCT-116 细胞中的 DC50 值分别为 1.7 和 5.8 nM。PROTAC TTK degrader-1 在 COLO-205 人结直肠癌细胞异种移植小鼠模型中显示出靶向降解和抗癌效果。

PROTAC TTK degrader-1

PROTAC TTK degrader-1 Chemical Structure

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

PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells[1].

IC50 & Target

DC50: 1.7 nM (TTK) in COLO-205, 5.8 nM (TTK) in HCT-116[1]
体外研究
(In Vitro)

PROTAC TTK degrader-1 (compound 8e) (0-10 μM, 96 h) inhibits cancer cell proliferation[1].
PROTAC TTK degrader-1 (5 and 50 nM, 6 h) induces degradation of TTK protein in a dose-dependent manner[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 Proliferation Assay

Cell Line: COLO-205 and HCT-116 cells[1]
Concentration: 0-10 μM
Incubation Time: 96 h
Result: Inhibited the growth of COLO-205 cancer cells with an IC50 of 0.1 μM.

Western Blot Analysis

Cell Line: COLO-205, HCT-116 LOVO, HCT-8, and HCT-29 human colon cancer cell lines[1]
Concentration: 5, 50 nM
Incubation Time: 6 h
Result: Induced degradation of TTK protein in a dose-dependent manner.

体内研究
(In Vivo)

PROTAC TTK degrader-1 (10 mg/kg, IP, single) demonstrates reasonable pharmacokinetics profiles[1].
PROTAC TTK degrader-1 (10, 20 mg/kg, IP, once daily for 16 days) significantly reduces the TTK protein levels, and exhibits tumor-growth inhibition[1].
Pharmacokinetic Parameters of PROTAC TTK degrader-1 in male SD rats[1].

8e
AUC (ng/mL*h) 2235
T1/2 (h) 4.3

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.

Animal Model: Male SD rats[1]
Dosage: 10 mg/kg, dissolved in mixed solvents (5% 20 mg/mL DMSO stock, 30% PG, 30% PEG400, and 35% Saline)
Administration: IP, single (Pharmacokinetic Analysis)
Result: Demonstrated reasonable pharmacokinetics profiles.
Animal Model: Male CB17-SCID mice (bearing COLO-205 tumor xenografts)[1]
Dosage: 10, 20 mg/kg
Administration: IP, once daily for 16 days
Result: Significantly reduced the TTK protein levels in animal tumor tissues, exhibited tumor-growth inhibition value of 46.0% upon 20 mg/kg dosing, did not cause a significant body weight loss of the animal.

分子量

855.98

Formula

C47H53N9O7
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]. Lu J, Huang Y, Huang J, et al. Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders. J Med Chem. 2022;65(3):2313-2328.

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 TTK degrader-2

发表于由
回复

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 TTK degrader-2 

PROTAC TTK degrader-2 是一种有效的 TTK (苏氨酸酪氨酸激酶) PROTAC 降解剂，在 COLO-205 和 HCT-116 细胞中的 DC50 值分别为 3.1 和 12.4 nM。PROTAC TTK degrader-2 在 COLO-205 人结直肠癌细胞异种移植小鼠模型中显示出靶向降解和抗癌效果。

PROTAC TTK degrader-2

PROTAC TTK degrader-2 Chemical Structure

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

PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells[1].

IC50 & Target

DC50: 3.1 nM (TTK) in COLO-205, 12.4 nM (TTK) in HCT-116[1]
体外研究
(In Vitro)

PROTAC TTK degrader-2 (compound 8j) (0-10 μM, 96 h) inhibits cancer cell proliferation[1].
PROTAC TTK degrader-2 (5 and 50 nM, 6 h) induces degradation of TTK protein in a dose-dependent manner[1].

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

Cell Proliferation Assay

Cell Line: COLO-205 and HCT-116 cells[1]
Concentration: 0-10 μM
Incubation Time: 96 h
Result: Inhibited the growth of COLO-205 cancer cells with an IC50 of 0.2 μM.

Western Blot Analysis

Cell Line: COLO-205, HCT-116 LOVO, HCT-8, and HCT-29 human colon cancer cell lines[1]
Concentration: 5, 50 nM
Incubation Time: 6 h
Result: Induced degradation of TTK protein in a dose-dependent manner.

体内研究
(In Vivo)

PROTAC TTK degrader-2 (8j) (10 mg/kg, IP, single) demonstrates reasonable pharmacokinetics profiles[1].
PROTAC TTK degrader-2 (10, 20 mg/kg, IP, once daily for 16 days) significantly reduces the TTK protein levels, and exhibits tumor-growth inhibition[1].
Pharmacokinetic Parameters of PROTAC TTK degrader-2 in male SD rats[1].

8j
AUC (ng/mL*h) 2333
T1/2 (h) 3.2

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

Animal Model: Male SD rats (, three animals per group)[1]
Dosage: 10 mg/kg, dissolved in mixed solvents (5% 20 mg/mL DMSO stock, 30% PG, 30% PEG400, and 35% Saline)
Administration: IP, single (Pharmacokinetic Analysis)
Result: Demonstrated reasonable pharmacokinetics profiles.
Animal Model: Male CB17-SCID mice (xenograft mouse model of COLO-205 cells)[1]
Dosage: 10, 20 mg/kg
Administration: IP, once daily for 16 days
Result: Significantly reduced the TTK protein levels in animal tumor tissues, exhibited tumor-growth inhibition value of 36.7% upon 20 mg/kg dosing, did not cause a significant body weight loss of the animal.

分子量

884.03

Formula

C49H57N9O7
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]. Lu J, Huang Y, Huang J, et al. Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders. J Med Chem. 2022;65(3):2313-2328.

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