标签归档：sos

SOS1-IN-9

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。

SOS1-IN-9 

SOS1-IN-9 是一种有效的 SOS1 抑制剂，对 KRAS G12C-SOS1 的IC50 为 116.5 nM。

SOS1-IN-9

SOS1-IN-9 Chemical Structure

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生物活性

SOS1-IN-9 is a potent SOS1 inhibitor with an IC50 of 116.5 nM for SOS1-KRAS G12C (WO2022028506A1, compound 302)[1].

IC50 & Target[1]

KRAS G12C-SOS1

116.5 nM (IC50)

分子量

435.49

Formula

C22H28F3N5O
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]. Sos1 inhibitor, pharmaceutical composition containing same, and use therefor. WO2022028506A1.

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

SOS1-IN-10

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。

SOS1-IN-10 

SOS1-IN-10 是一种有效的 SOS1 抑制剂，对 KRAS G12C-SOS1 的IC50 为 13 nM。

SOS1-IN-10

SOS1-IN-10 Chemical Structure

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生物活性

SOS1-IN-10 is a potent SOS1 inhibitor with an IC50 of 13 nM for KRAS G12C-SOS1 (WO2022017519A1, compound 8)[1].

IC50 & Target[1]

KRAS G12C-SOS1

13 nM (IC50)

分子量

450.40

Formula

C22H19F5N4O
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]. Quinazoline compound. WO2022017519A1.

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

SOS1-IN-9

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。

SOS1-IN-9 

SOS1-IN-9 是一种有效的 SOS1 抑制剂，对 KRAS G12C-SOS1 的IC50 为 116.5 nM。

SOS1-IN-9

SOS1-IN-9 Chemical Structure

规格 是否有货
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生物活性

SOS1-IN-9 is a potent SOS1 inhibitor with an IC50 of 116.5 nM for SOS1-KRAS G12C (WO2022028506A1, compound 302)[1].

IC50 & Target[1]

KRAS G12C-SOS1

116.5 nM (IC50)

分子量

435.49

Formula

C22H28F3N5O
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]. Sos1 inhibitor, pharmaceutical composition containing same, and use therefor. WO2022028506A1.

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

SOS1-IN-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。

SOS1-IN-6 

SOS1-IN-6 (compound 33-P1) 是一种有效的 SOS1 抑制剂，对 SOS1-G12D 和 SOS1-G12V 的 IC50 分别为 14.9 和 73.3 nM。

SOS1-IN-6

SOS1-IN-6 Chemical Structure

CAS No. : 2751718-88-2

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生物活性

SOS1-IN-6 (compound 33-P1) is a potent SOS1 inhibitor with IC50s of 14.9 and 73.3 nM for SOS1-G12D and SOS1-G12V, respectively[1].

IC50 & Target[1]

SOS1-G12D

14.9 nM (IC50)

SOS1-G12V

73.3 nM (IC50)

分子量

471.51

Formula

C26H28F3N3O2
CAS 号

2751718-88-2
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]. Fused quinazoline derivative, preparation method therefor and application thereof in medicine. WO2021249475A1.

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

SOS1-IN-7

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。

SOS1-IN-7 

SOS1-IN-7 (compound 18-p1) 是一种有效的 SOS1 抑制剂，对 SOS1-G12D 和SOS1-G12V 的 IC50 分别为 20 和 67 nM。

SOS1-IN-7

SOS1-IN-7 Chemical Structure

CAS No. : 2755415-30-4

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生物活性

SOS1-IN-7 (compound 18-p1) is a potent SOS1 inhibitor with IC50s of 20 and 67 nM for SOS1-G12D and SOS1-G12V, respectively[1].

IC50 & Target[1]

SOS1-G12D

20 nM (IC50)

SOS1-G12V

67 nM (IC50)

分子量

462.46

Formula

C23H25F3N4O3
CAS 号

2755415-30-4
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]. Pyridine-pyrimidine derivative, preparation method therefor and pharmaceutical use thereof. WO2021249519A1.

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

SOS1-IN-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。

SOS1-IN-6 

SOS1-IN-6 (compound 33-P1) 是一种有效的 SOS1 抑制剂，对 SOS1-G12D 和 SOS1-G12V 的 IC50 分别为 14.9 和 73.3 nM。

SOS1-IN-6

SOS1-IN-6 Chemical Structure

CAS No. : 2751718-88-2

规格 是否有货
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250 mg   询价  
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生物活性

SOS1-IN-6 (compound 33-P1) is a potent SOS1 inhibitor with IC50s of 14.9 and 73.3 nM for SOS1-G12D and SOS1-G12V, respectively[1].

IC50 & Target[1]

SOS1-G12D

14.9 nM (IC50)

SOS1-G12V

73.3 nM (IC50)

分子量

471.51

Formula

C26H28F3N3O2
CAS 号

2751718-88-2
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]. Fused quinazoline derivative, preparation method therefor and application thereof in medicine. WO2021249475A1.

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

SOS1-IN-7

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。

SOS1-IN-7 

SOS1-IN-7 (compound 18-p1) 是一种有效的 SOS1 抑制剂，对 SOS1-G12D 和SOS1-G12V 的 IC50 分别为 20 和 67 nM。

SOS1-IN-7

SOS1-IN-7 Chemical Structure

CAS No. : 2755415-30-4

规格 是否有货
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生物活性

SOS1-IN-7 (compound 18-p1) is a potent SOS1 inhibitor with IC50s of 20 and 67 nM for SOS1-G12D and SOS1-G12V, respectively[1].

IC50 & Target[1]

SOS1-G12D

20 nM (IC50)

SOS1-G12V

67 nM (IC50)

分子量

462.46

Formula

C23H25F3N4O3
CAS 号

2755415-30-4
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]. Pyridine-pyrimidine derivative, preparation method therefor and pharmaceutical use thereof. WO2021249519A1.

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

SOS1-IN-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。

SOS1-IN-6 

SOS1-IN-6 (compound 33-P1) 是一种有效的 SOS1 抑制剂，对 SOS1-G12D 和 SOS1-G12V 的 IC50 分别为 14.9 和 73.3 nM。

SOS1-IN-6

SOS1-IN-6 Chemical Structure

CAS No. : 2751718-88-2

规格 是否有货
100 mg   询价  
250 mg   询价  
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生物活性

SOS1-IN-6 (compound 33-P1) is a potent SOS1 inhibitor with IC50s of 14.9 and 73.3 nM for SOS1-G12D and SOS1-G12V, respectively[1].

IC50 & Target[1]

SOS1-G12D

14.9 nM (IC50)

SOS1-G12V

73.3 nM (IC50)

分子量

471.51

Formula

C26H28F3N3O2
CAS 号

2751718-88-2
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]. Fused quinazoline derivative, preparation method therefor and application thereof in medicine. WO2021249475A1.

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

SOS1-IN-7

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。

SOS1-IN-7 

SOS1-IN-7 (compound 18-p1) 是一种有效的 SOS1 抑制剂，对 SOS1-G12D 和SOS1-G12V 的 IC50 分别为 20 和 67 nM。

SOS1-IN-7

SOS1-IN-7 Chemical Structure

CAS No. : 2755415-30-4

规格 是否有货
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250 mg   询价  
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生物活性

SOS1-IN-7 (compound 18-p1) is a potent SOS1 inhibitor with IC50s of 20 and 67 nM for SOS1-G12D and SOS1-G12V, respectively[1].

IC50 & Target[1]

SOS1-G12D

20 nM (IC50)

SOS1-G12V

67 nM (IC50)

分子量

462.46

Formula

C23H25F3N4O3
CAS 号

2755415-30-4
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]. Pyridine-pyrimidine derivative, preparation method therefor and pharmaceutical use thereof. WO2021249519A1.

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

SOS1 activator 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。

SOS1 activator 1 

SOS1 activator 1 (Compound 64) 是 SOS1 介导的核苷酸交换的激活剂，Kd 为 44 nM。SOS1 是一种鸟嘌呤核苷酸交换因子，能与 Ras 蛋白结合，并使原来与 Ras 结合的 GDP 交换成GTP。可催化 GDP 与 RAS 上的 GTP 交换。

SOS1 activator 1

SOS1 activator 1 Chemical Structure

CAS No. : 2245237-53-8

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生物活性

SOS1 activator 1 (Compound 64) is a potent activator of SOS1-mediated nucleotide exchange with a Kd of 44 nM. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP for GTP on RAS[1].

分子量

483.02

Formula

C26H32ClFN6
CAS 号

2245237-53-8
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]. Timothy R Hodges, et al. Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS. J Med Chem. 2018 Oct 11;61(19):8875-8894.

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SOS1 activator 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。

SOS1 activator 1 

SOS1 activator 1 (Compound 64) 是 SOS1 介导的核苷酸交换的激活剂，Kd 为 44 nM。SOS1 是一种鸟嘌呤核苷酸交换因子，能与 Ras 蛋白结合，并使原来与 Ras 结合的 GDP 交换成GTP。可催化 GDP 与 RAS 上的 GTP 交换。

SOS1 activator 1

SOS1 activator 1 Chemical Structure

CAS No. : 2245237-53-8

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

SOS1 activator 1 (Compound 64) is a potent activator of SOS1-mediated nucleotide exchange with a Kd of 44 nM. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP for GTP on RAS[1].

分子量

483.02

Formula

C26H32ClFN6
CAS 号

2245237-53-8
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]. Timothy R Hodges, et al. Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS. J Med Chem. 2018 Oct 11;61(19):8875-8894.

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

SOS1 activator 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。

SOS1 activator 1 

SOS1 activator 1 (Compound 64) 是 SOS1 介导的核苷酸交换的激活剂，Kd 为 44 nM。SOS1 是一种鸟嘌呤核苷酸交换因子，能与 Ras 蛋白结合，并使原来与 Ras 结合的 GDP 交换成GTP。可催化 GDP 与 RAS 上的 GTP 交换。

SOS1 activator 1

SOS1 activator 1 Chemical Structure

CAS No. : 2245237-53-8

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

SOS1 activator 1 (Compound 64) is a potent activator of SOS1-mediated nucleotide exchange with a Kd of 44 nM. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP for GTP on RAS[1].

分子量

483.02

Formula

C26H32ClFN6
CAS 号

2245237-53-8
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]. Timothy R Hodges, et al. Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS. J Med Chem. 2018 Oct 11;61(19):8875-8894.

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

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
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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

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

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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

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-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 SOS1 degrader-1 

PROTAC SOS1degrader-1 是一种有效的 PROTAC SOS1 激动剂，DC50 为 98.4 nM。PROTAC SOS1 Degrader-1 在各种 KRAS 突变的癌细胞中显示出抗增殖活性。PROTAC SOS1 Degrader-1 具有抗肿瘤作用，且具有低毒性。

PROTAC SOS1 degrader-1

PROTAC SOS1 degrader-1 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

PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 agonist with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity[1].

IC50 & Target

DC50: 98.4 nM (SOS1)[1]
体外研究
(In Vitro)

PROTAC SOS1 degrader-1 (compound 9d) (0.1, 1 µM) shows SOSI degradation activity with an SOS1 protein degradation of 56.2 and 92.5% at 0.1 and 1 μM, respectively[1].
PROTAC SOS1 degrader-1 (0-2000 nM; 24 h) exhibits SOS1 degradation activity with an DC50 of 98.4 nM in a dose- and time-dependent manner in NCI-H358 cells[1].
PROTAC SOS1 degrader-1 (0-2500 nM; 24 h) dose-dependently reduced the SOS1 protein level but showed no effect on SOS2 and KRAS up to 2.5 μM in NCI-H358 and AsPc-1 cells[1].
PROTAC SOS1 degrader-1 (0-2000 nM; 24 h) reduces the expression of KRAS-GTP, induced ERK phosphorylation with an IC50value of 72.3 nM, and significantly increases the pERK level after 6-24 h[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: 0-2000 nM
Incubation Time: 0-24 h
Result: Decreased the expression of SOS1 in a dose- and time-dependent manner in NCI-H358 cells.

RT-PCR[1]

Cell Line: NCI-H358 cells
Concentration: 1 µM
Incubation Time: 24, 48, 72 h
Result: Showed no effffect on SOS2 mRNA expression.

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: Showed anti-proliferation activity with an IC50s of 0.525, 0.218, 0.307, 0.115, 0.199, 0.232 µM and DC50s 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-1 (10 mg/kg; i.p.) shows good PK profile with low toxicity[1].
PROTAC SOS1 degrader-1 (0, 10, 20 mg/kg; i.p.; once a day for 3 weeks) shows significant anti-tumor activities in the xenograft mouse model[1].
Pharmacokinetic Parameters of PROTAC SOS1 degrader-1 in BALB/c mice[1].

compound dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUClast (h*ng/mL) AUCINF (h*ng/mL) MRTINF-obs(h)
9d 10 8.64±0.31 0.250v±0 1221±132 3895±335 4420±363 10.2±0.4

Male BALB/c mice; 10 mg/kg for i.p.[1].

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

Animal Model: Male BALB/c mice[1]
Dosage: 10 mg/kg (dissolved in solution containing dimethyl sulfoxide, PEG400, and 10% hydroxypropyl-β-cyclodextrin in water (5/5/90, v/v/v))
Administration: I.p.
Result: Showed good PK profile with high exposure (AUC0‑∞ = 4420 h*ng/mL) and maximum concentration (Cmax = 1221 ng/mL) in mouse plasma.
Animal Model: 6-8 weeks, BALB/c mice [1]
Dosage: 0, 10, 20 mg/kg
Administration: I.p.; once a day for a week
Result: Showed low toxicity for mouse.
Animal Model: 6-8 weeks, BALB/c nude mice (NCI-H358 tumor xenografts) [1]
Dosage: 0, 10, 20 mg/kg
Administration: I.p.; once a day for 3 weeks;
Result: Inhibited the tumor growth by 72.5 and 86.1% at 10 and 20 mg/kg, respectively.
Animal Model: 6-8 weeks, BALB/c nude mice (NCI-H358 tumor xenografts)[1]
Dosage: 0, 20, 50 mg/kg
Administration: Intratumoral injection; twice-weekly for 5 weeks
Result: Significantly prevented 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 Mar 10;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

BAY-293

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。

BAY-293  纯度: 98.06%

BAY-293 是一种有价值的化学探针，通过破坏 KRAS-SOS1 相互作用从而阻断 RAS 活化，IC50 为 21 nM。BAY-293 是一种有效的 SOS1 抑制剂。SOS1 是一种鸟苷酸交换因子 (GEF)，也是 RAS 的激活剂。

BAY-293

BAY-293 Chemical Structure

CAS No. : 2244904-70-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2530 In-stock
5 mg ￥2300 In-stock
10 mg ￥4150 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

BAY-293 相关产品

•相关化合物库:

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生物活性

BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS[1].

IC50 & Target[1]

KRAS-SOS1

21 nM (IC50)

体外研究
(In Vitro)

BAY-293 inhibits the activation of RAS in HeLa cells, with IC50 values in the submicromolar range[1].
BAY-293 (595 nM-3580 nM; 72 hours) shows efficient antiproliferative activity against wild-type KRAS cell lines (K-562, MOLM-13) and cell lines with KRASG12C mutation (NCI-H358, Calu-1)[1].
BAY-293 efficiently inhibits pERK levels in K-562 cells after incubation for 60 min without affecting total protein levels of ERK[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: K-562, MOLM-13, H358 and Calu-1 cell lines
Concentration: 595-3580 nM
Incubation Time: 72 hours
Result: IC50s of 1,090±170 nM, 995±400 nM, 3,480±100 nM and 3,190±50 nM for K-562, MOLM-13, H358 and Calu-1 cells, respectively.

分子量

448.58

Formula

C25H28N4O2S
CAS 号

2244904-70-7
运输条件

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

DMSO : ≥ 125 mg/mL (278.66 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2293 mL 11.1463 mL 22.2926 mL
5 mM 0.4459 mL 2.2293 mL 4.4585 mL
10 mM 0.2229 mL 1.1146 mL 2.2293 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。-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: ≥ 2.08 mg/mL (4.64 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.64 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.64 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.64 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 20.8 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]. Hillig RC, et al. Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1interaction. Proc Natl Acad Sci U S A. 2019 Feb 12;116(7):2551-2560.

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