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Bcl-2-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。

Bcl-2-IN-5 

Bcl-2-IN-5 是一种 BCL-2 抑制剂，对 Bcl-2 野生型、Bcl-2 D103Y 和 Bcl-2 G101V 的 IC50 分别为 0.12 nM、0.14 nM 和 0.22 nM。Bcl-2-IN-5 抑制细胞生长，对 Bcl 2-G101V 敲入RS4; 11 和 RS4; 11 细胞的 IC50 值分别 0.2 nM 和 0.44 nM (WO2021208963A1; Example 155)。

Bcl-2-IN-5

Bcl-2-IN-5 Chemical Structure

CAS No. : 2728752-20-1

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生物活性

Bcl-2-IN-5 is a BCL-2 inhibitor with IC50s of 0.12 nM, 0.14 nM and 0.22 nM for Bcl-2 wild type, Bcl-2 D103Y and Bcl-2 G101V, respectively. Bcl-2-IN-5 inhibits the cell growth with IC50 values of 0.2 nM and 0.44 nM for Bcl 2-G101V knock-in RS4; 11 and RS4; 11 cells, respectively (WO2021208963A1; Example 155)[1].

IC50 & Target[1]

Bcl-2

0.12 nM (IC50)

Bcl-2 D103Y

0.14 nM (IC50)

Bcl-2 G101V

0.22 nM (IC50)

分子量

1015.20

Formula

C55H63FN8O8S
CAS 号

2728752-20-1
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]. Hai Xue, et al. Bcl-2 inhibitor. WO2021208963A1.

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Bcl-2-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。

Bcl-2-IN-4 

Bcl-2-IN-4 是一种有效的、具有口服活性的选择性 Bcl-2 抑制剂，IC50 为 1.5 nM。Bcl-2-IN-4 的选择性比 Bcl-xL 高于 200 倍 (IC50 为 411 nM)。Bcl-2-IN-4 抑制 RS4； 11 细胞增殖，IC50 为 2.7 nM (WO2021180040A1; compound 2)。

Bcl-2-IN-4

Bcl-2-IN-4 Chemical Structure

CAS No. : 2703134-40-9

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生物活性

Bcl-2-IN-4 is a potent, orally active and selective Bcl-2 inhibitor with an IC50 of 1.5 nM. Bcl-2-IN-4 displays >200-fold selectivity over Bcl-xL (IC50 of 411 nM). Bcl-2-IN-4 inhibits RS4; 11 cell proliferation with an IC50 of 2.7 nM (WO2021180040A1; compound 2)[1].

IC50 & Target[1]

Bcl-2

1.5 nM (IC50)

Bcl-xL

411 nM (IC50)

分子量

908.46

Formula

C46H50ClN9O7S
CAS 号

2703134-40-9
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]. Hongjian Wang, et al. Benzo five-membered cyclic compound. WO2021180040A1.

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Bcl-2-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。

Bcl-2-IN-4 

Bcl-2-IN-4 是一种有效的、具有口服活性的选择性 Bcl-2 抑制剂，IC50 为 1.5 nM。Bcl-2-IN-4 的选择性比 Bcl-xL 高于 200 倍 (IC50 为 411 nM)。Bcl-2-IN-4 抑制 RS4； 11 细胞增殖，IC50 为 2.7 nM (WO2021180040A1; compound 2)。

Bcl-2-IN-4

Bcl-2-IN-4 Chemical Structure

CAS No. : 2703134-40-9

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

Bcl-2-IN-4 is a potent, orally active and selective Bcl-2 inhibitor with an IC50 of 1.5 nM. Bcl-2-IN-4 displays >200-fold selectivity over Bcl-xL (IC50 of 411 nM). Bcl-2-IN-4 inhibits RS4; 11 cell proliferation with an IC50 of 2.7 nM (WO2021180040A1; compound 2)[1].

IC50 & Target[1]

Bcl-2

1.5 nM (IC50)

Bcl-xL

411 nM (IC50)

分子量

908.46

Formula

C46H50ClN9O7S
CAS 号

2703134-40-9
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]. Hongjian Wang, et al. Benzo five-membered cyclic compound. WO2021180040A1.

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(R)-MALT1-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。

(R)-MALT1-IN-3 

(R)-MALT1-IN-3 (compound 121) 是一种有效的 MALT1 蛋白酶抑制剂，IC50 为 20 nM。(R)-MALT1-IN-3 对于 OCI-LY3 细胞中的人 IL6/IL10 的 IC50 分别为 60 nM 和 40 nM。

(R)-MALT1-IN-3

(R)-MALT1-IN-3 Chemical Structure

CAS No. : 2504229-61-0

规格 是否有货
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250 mg   询价  
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生物活性

(R)-MALT1-IN-3 (compound 121) is a potent MALT1 protease inhibitor with an IC50 of 20 nM. (R)-MALT1-IN-3 has IC50 of 60 nM, 40 nM for human IL6/IL10 in OCI-LY3 cells, respectively[1].

分子量

472.42

Formula

C21H19F3N8O2
CAS 号

2504229-61-0
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]. Johannes Wilhelmus J Thuring, et al. Pyridine rings containing derivatives as malt1 inhibitors

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Bcl-2-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。

Bcl-2-IN-5 

Bcl-2-IN-5 是一种 BCL-2 抑制剂，对 Bcl-2 野生型、Bcl-2 D103Y 和 Bcl-2 G101V 的 IC50 分别为 0.12 nM、0.14 nM 和 0.22 nM。Bcl-2-IN-5 抑制细胞生长，对 Bcl 2-G101V 敲入RS4; 11 和 RS4; 11 细胞的 IC50 值分别 0.2 nM 和 0.44 nM (WO2021208963A1; Example 155)。

Bcl-2-IN-5

Bcl-2-IN-5 Chemical Structure

CAS No. : 2728752-20-1

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

Bcl-2-IN-5 is a BCL-2 inhibitor with IC50s of 0.12 nM, 0.14 nM and 0.22 nM for Bcl-2 wild type, Bcl-2 D103Y and Bcl-2 G101V, respectively. Bcl-2-IN-5 inhibits the cell growth with IC50 values of 0.2 nM and 0.44 nM for Bcl 2-G101V knock-in RS4; 11 and RS4; 11 cells, respectively (WO2021208963A1; Example 155)[1].

IC50 & Target[1]

Bcl-2

0.12 nM (IC50)

Bcl-2 D103Y

0.14 nM (IC50)

Bcl-2 G101V

0.22 nM (IC50)

分子量

1015.20

Formula

C55H63FN8O8S
CAS 号

2728752-20-1
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]. Hai Xue, et al. Bcl-2 inhibitor. WO2021208963A1.

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Bcl-2-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。

Bcl-2-IN-5 

Bcl-2-IN-5 是一种 BCL-2 抑制剂，对 Bcl-2 野生型、Bcl-2 D103Y 和 Bcl-2 G101V 的 IC50 分别为 0.12 nM、0.14 nM 和 0.22 nM。Bcl-2-IN-5 抑制细胞生长，对 Bcl 2-G101V 敲入RS4; 11 和 RS4; 11 细胞的 IC50 值分别 0.2 nM 和 0.44 nM (WO2021208963A1; Example 155)。

Bcl-2-IN-5

Bcl-2-IN-5 Chemical Structure

CAS No. : 2728752-20-1

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

Bcl-2-IN-5 is a BCL-2 inhibitor with IC50s of 0.12 nM, 0.14 nM and 0.22 nM for Bcl-2 wild type, Bcl-2 D103Y and Bcl-2 G101V, respectively. Bcl-2-IN-5 inhibits the cell growth with IC50 values of 0.2 nM and 0.44 nM for Bcl 2-G101V knock-in RS4; 11 and RS4; 11 cells, respectively (WO2021208963A1; Example 155)[1].

IC50 & Target[1]

Bcl-2

0.12 nM (IC50)

Bcl-2 D103Y

0.14 nM (IC50)

Bcl-2 G101V

0.22 nM (IC50)

分子量

1015.20

Formula

C55H63FN8O8S
CAS 号

2728752-20-1
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]. Hai Xue, et al. Bcl-2 inhibitor. WO2021208963A1.

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(R)-MALT1-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。

(R)-MALT1-IN-3 

(R)-MALT1-IN-3 (compound 121) 是一种有效的 MALT1 蛋白酶抑制剂，IC50 为 20 nM。(R)-MALT1-IN-3 对于 OCI-LY3 细胞中的人 IL6/IL10 的 IC50 分别为 60 nM 和 40 nM。

(R)-MALT1-IN-3

(R)-MALT1-IN-3 Chemical Structure

CAS No. : 2504229-61-0

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

(R)-MALT1-IN-3 (compound 121) is a potent MALT1 protease inhibitor with an IC50 of 20 nM. (R)-MALT1-IN-3 has IC50 of 60 nM, 40 nM for human IL6/IL10 in OCI-LY3 cells, respectively[1].

分子量

472.42

Formula

C21H19F3N8O2
CAS 号

2504229-61-0
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]. Johannes Wilhelmus J Thuring, et al. Pyridine rings containing derivatives as malt1 inhibitors

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

(R)-MALT1-IN-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。

(R)-MALT1-IN-3 

(R)-MALT1-IN-3 (compound 121) 是一种有效的 MALT1 蛋白酶抑制剂，IC50 为 20 nM。(R)-MALT1-IN-3 对于 OCI-LY3 细胞中的人 IL6/IL10 的 IC50 分别为 60 nM 和 40 nM。

(R)-MALT1-IN-3

(R)-MALT1-IN-3 Chemical Structure

CAS No. : 2504229-61-0

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

(R)-MALT1-IN-3 (compound 121) is a potent MALT1 protease inhibitor with an IC50 of 20 nM. (R)-MALT1-IN-3 has IC50 of 60 nM, 40 nM for human IL6/IL10 in OCI-LY3 cells, respectively[1].

分子量

472.42

Formula

C21H19F3N8O2
CAS 号

2504229-61-0
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]. Johannes Wilhelmus J Thuring, et al. Pyridine rings containing derivatives as malt1 inhibitors

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

RET-IN-16

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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。

RET-IN-16 

RET-IN-16 是一种有效且具有选择性的 RET 抑制剂，对 RET(WT)，RET(M918T)，RET(V804L)，RET(V804M)，RET-CCDC6 和 RET-KIF5B 的 IC50 分别为 3.98 nM，8.42 nM，15.05 nM，7.86 nM，5.43 nM 和 8.86 nM。RET-IN-16 具有抗癌作用。

RET-IN-16

RET-IN-16 Chemical Structure

CAS No. : 2259657-48-0

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100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

RET-IN-16 is a potent and selective RET inhibitor with IC50s of 3.98 nM, 8.42 nM, 15.05 nM, 7.86 nM, 5.43 nM and 8.86 nM for RET(WT), RET(M918T), RET(V804L), RET(V804M), RET-CCDC6 and RET-KIF5B, respectively. RET-IN-16 has anticancer effects[1].

IC50 & Target

IC50: 3.98 nM (RET(WT)), 8.42 nM (RET(M918T)), 15.05 nM (RET(V804L)), 7.86 nM (RET(V804M)), 5.43 nM (RET-CCDC6), 8.86 nM (RET-KIF5B)[1]
体外研究
(In Vitro)

RET-IN-16 (compound 9x) (0.005-10 μM; 48 hours) exhibits potent activity against CCDC6-RET-Ba/F3 and KIF5B-RET-Ba/F3 with GI50 of 9 nM and 17 nM, respectively[1].
RET-IN-16 (1 μM; 48 hours) selectively suppresses the proliferation of CCDC6-RET fusion cells[1].
RET-IN-16 (50 and 100 μM; 4 hours) remarkably blocks the autophosphorylation of RET in KIF5B-RET and KIF5B-RETV804M Ba/F3 cells, and the phosphorylation of the adapter protein SHC is also inhibited with 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: LC-2/ad, A549, H3122, MDA-MB-231 and A375, SKGT4, HepG2, KYSE450 and BGC823 cells[1]
Concentration: 1 μM
Incubation Time: 48 hours
Result: Potently suppressed the proliferation of LC-2/ad NSCLC cells harboring the CCDC6-RET fusion, but dramatically decreased potency against other RET-negative cancer cells.

Western Blot Analysis

Cell Line: KIF5B-RET and KIF5B-RETV804M Ba/F3 cells[1]
Concentration: 50 and 100 μM
Incubation Time: 4 hours
Result: Remarkably blocked the autophosphorylation of RET, and the phosphorylation of the adapter protein SHC was also inhibited in a dose-dependent manner.

体内研究
(In Vivo)

RET-IN-16 (1 mg/kg; IV; single) exhibits a good drug exposure (AUC0-t = 6959 ± 762 ng·h/mL) and a moderate half-life (T1/2 = 4.28 ± 0.43 h)[1].
RET-IN-16 (10 mg/kg; PO; single) exhibits a low maximum plasma concentration (Cmax = 194 ± 47 ng·h/mL) and drug exposure (AUC0-t = 2112 ± 117 ng·h/mL)[1].
RET-IN-16 (30 and 50 mg/kg; IV; daily; for 8 days) suppresses tumor growth in a dose-dependent manner, and significantly suppresses p-RET and p-SHC in both KIF5B-RET and KIF5B-RETV804M in tumor tissues, as well as significantly induces apoptosis in vivo[1].
Pharmacokinetic Parameters of RET-IN-16 in male Sprague-Dawley rats[1].

IV (1 mg/kg) PO (10 mg/kg)
T1/2 (h) 4.28 ± 0.43 7.59 ± 1.02
Tmax (h) 0.083 ± 0 0.75 ± 0.43
Cmax (ng/mL) 6097 ± 623 194 ± 47
AUC0-t (ng/mL·h) 6959 ± 762 2112 ± 117
AUC0-∞ (ng/mL·h) 7014 ± 753 2343 ± 157
F (%) 3.0

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

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 1 mg/kg for IV, 10 mg/kg for PO
Administration: IV and PO; single (Pharmacokinetic Analysis)
Result: Exhibited a good drug exposure (AUC0-t = 6959 ± 762 ng·h/mL) and a moderate half-life (T1/2 = 4.28 ± 0.43 h) at 1 mg/kg IV; observed a low maximum plasma concentration (Cmax = 194 ± 47 ng·h/mL) and drug exposure (AUC0-t = 2112 ± 117 ng·h/mL) at 10 mg/kg PO.
Animal Model: Half male and female BALB/c-nu mice (6-8 weeks; injected with KIF5B-RET Ba/F3 and KIF5B-RETV804M Ba/F3)[1]
Dosage: 30 and 50 mg/kg
Administration: IV; daily; for 8 days
Result: Suppressed tumor growth in a dose-dependent manner, and significantly suppressed p-RET and p-SHC in both KIF5B-RET and KIF5B-RETV804M in tumor tissues, as well as significantly induced apoptosis in vivo.

分子量

602.61

Formula

C31H29F3N8O2
CAS 号

2259657-48-0
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]. Li X, Su J, Yang Y, et al. Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant. Eur J Med Chem. 2020;207:112755.

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RET-IN-16

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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。

RET-IN-16 

RET-IN-16 是一种有效且具有选择性的 RET 抑制剂，对 RET(WT)，RET(M918T)，RET(V804L)，RET(V804M)，RET-CCDC6 和 RET-KIF5B 的 IC50 分别为 3.98 nM，8.42 nM，15.05 nM，7.86 nM，5.43 nM 和 8.86 nM。RET-IN-16 具有抗癌作用。

RET-IN-16

RET-IN-16 Chemical Structure

CAS No. : 2259657-48-0

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

RET-IN-16 is a potent and selective RET inhibitor with IC50s of 3.98 nM, 8.42 nM, 15.05 nM, 7.86 nM, 5.43 nM and 8.86 nM for RET(WT), RET(M918T), RET(V804L), RET(V804M), RET-CCDC6 and RET-KIF5B, respectively. RET-IN-16 has anticancer effects[1].

IC50 & Target

IC50: 3.98 nM (RET(WT)), 8.42 nM (RET(M918T)), 15.05 nM (RET(V804L)), 7.86 nM (RET(V804M)), 5.43 nM (RET-CCDC6), 8.86 nM (RET-KIF5B)[1]
体外研究
(In Vitro)

RET-IN-16 (compound 9x) (0.005-10 μM; 48 hours) exhibits potent activity against CCDC6-RET-Ba/F3 and KIF5B-RET-Ba/F3 with GI50 of 9 nM and 17 nM, respectively[1].
RET-IN-16 (1 μM; 48 hours) selectively suppresses the proliferation of CCDC6-RET fusion cells[1].
RET-IN-16 (50 and 100 μM; 4 hours) remarkably blocks the autophosphorylation of RET in KIF5B-RET and KIF5B-RETV804M Ba/F3 cells, and the phosphorylation of the adapter protein SHC is also inhibited with 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: LC-2/ad, A549, H3122, MDA-MB-231 and A375, SKGT4, HepG2, KYSE450 and BGC823 cells[1]
Concentration: 1 μM
Incubation Time: 48 hours
Result: Potently suppressed the proliferation of LC-2/ad NSCLC cells harboring the CCDC6-RET fusion, but dramatically decreased potency against other RET-negative cancer cells.

Western Blot Analysis

Cell Line: KIF5B-RET and KIF5B-RETV804M Ba/F3 cells[1]
Concentration: 50 and 100 μM
Incubation Time: 4 hours
Result: Remarkably blocked the autophosphorylation of RET, and the phosphorylation of the adapter protein SHC was also inhibited in a dose-dependent manner.

体内研究
(In Vivo)

RET-IN-16 (1 mg/kg; IV; single) exhibits a good drug exposure (AUC0-t = 6959 ± 762 ng·h/mL) and a moderate half-life (T1/2 = 4.28 ± 0.43 h)[1].
RET-IN-16 (10 mg/kg; PO; single) exhibits a low maximum plasma concentration (Cmax = 194 ± 47 ng·h/mL) and drug exposure (AUC0-t = 2112 ± 117 ng·h/mL)[1].
RET-IN-16 (30 and 50 mg/kg; IV; daily; for 8 days) suppresses tumor growth in a dose-dependent manner, and significantly suppresses p-RET and p-SHC in both KIF5B-RET and KIF5B-RETV804M in tumor tissues, as well as significantly induces apoptosis in vivo[1].
Pharmacokinetic Parameters of RET-IN-16 in male Sprague-Dawley rats[1].

IV (1 mg/kg) PO (10 mg/kg)
T1/2 (h) 4.28 ± 0.43 7.59 ± 1.02
Tmax (h) 0.083 ± 0 0.75 ± 0.43
Cmax (ng/mL) 6097 ± 623 194 ± 47
AUC0-t (ng/mL·h) 6959 ± 762 2112 ± 117
AUC0-∞ (ng/mL·h) 7014 ± 753 2343 ± 157
F (%) 3.0

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

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 1 mg/kg for IV, 10 mg/kg for PO
Administration: IV and PO; single (Pharmacokinetic Analysis)
Result: Exhibited a good drug exposure (AUC0-t = 6959 ± 762 ng·h/mL) and a moderate half-life (T1/2 = 4.28 ± 0.43 h) at 1 mg/kg IV; observed a low maximum plasma concentration (Cmax = 194 ± 47 ng·h/mL) and drug exposure (AUC0-t = 2112 ± 117 ng·h/mL) at 10 mg/kg PO.
Animal Model: Half male and female BALB/c-nu mice (6-8 weeks; injected with KIF5B-RET Ba/F3 and KIF5B-RETV804M Ba/F3)[1]
Dosage: 30 and 50 mg/kg
Administration: IV; daily; for 8 days
Result: Suppressed tumor growth in a dose-dependent manner, and significantly suppressed p-RET and p-SHC in both KIF5B-RET and KIF5B-RETV804M in tumor tissues, as well as significantly induced apoptosis in vivo.

分子量

602.61

Formula

C31H29F3N8O2
CAS 号

2259657-48-0
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]. Li X, Su J, Yang Y, et al. Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant. Eur J Med Chem. 2020;207:112755.

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RET-IN-16

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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。

RET-IN-16 

RET-IN-16 是一种有效且具有选择性的 RET 抑制剂，对 RET(WT)，RET(M918T)，RET(V804L)，RET(V804M)，RET-CCDC6 和 RET-KIF5B 的 IC50 分别为 3.98 nM，8.42 nM，15.05 nM，7.86 nM，5.43 nM 和 8.86 nM。RET-IN-16 具有抗癌作用。

RET-IN-16

RET-IN-16 Chemical Structure

CAS No. : 2259657-48-0

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

RET-IN-16 is a potent and selective RET inhibitor with IC50s of 3.98 nM, 8.42 nM, 15.05 nM, 7.86 nM, 5.43 nM and 8.86 nM for RET(WT), RET(M918T), RET(V804L), RET(V804M), RET-CCDC6 and RET-KIF5B, respectively. RET-IN-16 has anticancer effects[1].

IC50 & Target

IC50: 3.98 nM (RET(WT)), 8.42 nM (RET(M918T)), 15.05 nM (RET(V804L)), 7.86 nM (RET(V804M)), 5.43 nM (RET-CCDC6), 8.86 nM (RET-KIF5B)[1]
体外研究
(In Vitro)

RET-IN-16 (compound 9x) (0.005-10 μM; 48 hours) exhibits potent activity against CCDC6-RET-Ba/F3 and KIF5B-RET-Ba/F3 with GI50 of 9 nM and 17 nM, respectively[1].
RET-IN-16 (1 μM; 48 hours) selectively suppresses the proliferation of CCDC6-RET fusion cells[1].
RET-IN-16 (50 and 100 μM; 4 hours) remarkably blocks the autophosphorylation of RET in KIF5B-RET and KIF5B-RETV804M Ba/F3 cells, and the phosphorylation of the adapter protein SHC is also inhibited with 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: LC-2/ad, A549, H3122, MDA-MB-231 and A375, SKGT4, HepG2, KYSE450 and BGC823 cells[1]
Concentration: 1 μM
Incubation Time: 48 hours
Result: Potently suppressed the proliferation of LC-2/ad NSCLC cells harboring the CCDC6-RET fusion, but dramatically decreased potency against other RET-negative cancer cells.

Western Blot Analysis

Cell Line: KIF5B-RET and KIF5B-RETV804M Ba/F3 cells[1]
Concentration: 50 and 100 μM
Incubation Time: 4 hours
Result: Remarkably blocked the autophosphorylation of RET, and the phosphorylation of the adapter protein SHC was also inhibited in a dose-dependent manner.

体内研究
(In Vivo)

RET-IN-16 (1 mg/kg; IV; single) exhibits a good drug exposure (AUC0-t = 6959 ± 762 ng·h/mL) and a moderate half-life (T1/2 = 4.28 ± 0.43 h)[1].
RET-IN-16 (10 mg/kg; PO; single) exhibits a low maximum plasma concentration (Cmax = 194 ± 47 ng·h/mL) and drug exposure (AUC0-t = 2112 ± 117 ng·h/mL)[1].
RET-IN-16 (30 and 50 mg/kg; IV; daily; for 8 days) suppresses tumor growth in a dose-dependent manner, and significantly suppresses p-RET and p-SHC in both KIF5B-RET and KIF5B-RETV804M in tumor tissues, as well as significantly induces apoptosis in vivo[1].
Pharmacokinetic Parameters of RET-IN-16 in male Sprague-Dawley rats[1].

IV (1 mg/kg) PO (10 mg/kg)
T1/2 (h) 4.28 ± 0.43 7.59 ± 1.02
Tmax (h) 0.083 ± 0 0.75 ± 0.43
Cmax (ng/mL) 6097 ± 623 194 ± 47
AUC0-t (ng/mL·h) 6959 ± 762 2112 ± 117
AUC0-∞ (ng/mL·h) 7014 ± 753 2343 ± 157
F (%) 3.0

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 Sprague-Dawley rats[1]
Dosage: 1 mg/kg for IV, 10 mg/kg for PO
Administration: IV and PO; single (Pharmacokinetic Analysis)
Result: Exhibited a good drug exposure (AUC0-t = 6959 ± 762 ng·h/mL) and a moderate half-life (T1/2 = 4.28 ± 0.43 h) at 1 mg/kg IV; observed a low maximum plasma concentration (Cmax = 194 ± 47 ng·h/mL) and drug exposure (AUC0-t = 2112 ± 117 ng·h/mL) at 10 mg/kg PO.
Animal Model: Half male and female BALB/c-nu mice (6-8 weeks; injected with KIF5B-RET Ba/F3 and KIF5B-RETV804M Ba/F3)[1]
Dosage: 30 and 50 mg/kg
Administration: IV; daily; for 8 days
Result: Suppressed tumor growth in a dose-dependent manner, and significantly suppressed p-RET and p-SHC in both KIF5B-RET and KIF5B-RETV804M in tumor tissues, as well as significantly induced apoptosis in vivo.

分子量

602.61

Formula

C31H29F3N8O2
CAS 号

2259657-48-0
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]. Li X, Su J, Yang Y, et al. Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant. Eur J Med Chem. 2020;207:112755.

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PI3K-IN-31

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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。

PI3K-IN-31 

PI3K-IN-31 (Compound 6b) 是一种有效的 PI3K 抑制剂，对 PI3Kα、PI3Kβ、PI3Kγ 和 PI3Kδ 的 IC50 分别为 3.7 nM、74 nM、14.6 nM 和 9.9 nM。PI3K-IN-31 具有抗癌作用。

PI3K-IN-31

PI3K-IN-31 Chemical Structure

CAS No. : 1359956-12-9

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

PI3K-IN-31 (Compound 6b) is a potent PI3K inhibitor with IC50s of 3.7 nM, 74 nM, 14.6 nM, and 9.9 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. PI3K-IN-31 has anticancer effects[1].

IC50 & Target[1]

PI3Kα

3.7 nM (IC50)

PI3Kδ

9.9 nM (IC50)

PI3Kγ

14.6 nM (IC50)

PI3Kβ

74 nM (IC50)

分子量

435.43

Formula

C19H23F2N7O3
CAS 号

1359956-12-9
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]. Marcian E Van Dort, et al. Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors. Eur J Med Chem. 2022 Feb 5;229:113996.

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PI3K-IN-31

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。

PI3K-IN-31 

PI3K-IN-31 (Compound 6b) 是一种有效的 PI3K 抑制剂，对 PI3Kα、PI3Kβ、PI3Kγ 和 PI3Kδ 的 IC50 分别为 3.7 nM、74 nM、14.6 nM 和 9.9 nM。PI3K-IN-31 具有抗癌作用。

PI3K-IN-31

PI3K-IN-31 Chemical Structure

CAS No. : 1359956-12-9

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

PI3K-IN-31 (Compound 6b) is a potent PI3K inhibitor with IC50s of 3.7 nM, 74 nM, 14.6 nM, and 9.9 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. PI3K-IN-31 has anticancer effects[1].

IC50 & Target[1]

PI3Kα

3.7 nM (IC50)

PI3Kδ

9.9 nM (IC50)

PI3Kγ

14.6 nM (IC50)

PI3Kβ

74 nM (IC50)

分子量

435.43

Formula

C19H23F2N7O3
CAS 号

1359956-12-9
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]. Marcian E Van Dort, et al. Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors. Eur J Med Chem. 2022 Feb 5;229:113996.

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EGFR-IN-48

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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。

EGFR-IN-48 

EGFR-IN-48 是一种有效的且具有口服活性的 EGFR 抑制剂，对 EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWT 的 IC50 值分别为 0.193 nM, 0.251 nM, 10.4 nM。EGFR-IN-48 抑制 BaF3EGFR del19/T790M/C797S 和 PC-9EGFR del19/T790M/C797S 细胞的增殖，IC50 值分别为 1.526 nM 和 66.7 nM。

EGFR-IN-48

EGFR-IN-48 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

EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively[1].

IC50 & Target

EGFRd19/TM/CS

0.193 nM (IC50)

EGFRLR/TM/CS

0.251 nM (IC50)

EGFRWT

10.4 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-48 (compound 23) (10 nM) shows anti-proliferative activities against BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively[1].
EGFR-IN-48 exhibits potent inhibitory activities against various clinically relevant EGFR mutants with IC50s of 10.4, 3.1, 0.9, 0.1, 0.2, 0.3, 0.2 nM for EGFRWT, EGFRLR, EGFRdel19, EGFRdel19/TM, EGFRLR/TM, EGFRLR/TM/CS, EGFRdrl19/TM/CS, respectively[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: BaF3EGFR del19/T790M/C797S, PC-9EGFR del19/T790M/C797S cells
Concentration: 10 nM
Incubation Time:
Result: Showed anti-proliferative activities against BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively.

体内研究
(In Vivo)

EGFR-IN-48 (2 mg/kg for i.v.; 10 mg/kg for o.p.) shows good oral bioavailability and high plasma exposure in CD-1 mouse[1]. Pharmacokinetic Parameters of EGFR-IN-48 in CD-1 mouse[1].

Route Dose (mg/kg) Vdss (L/kg) T1/2 (h) CL (L/h/kg) AUC0-last (h*ng/mL) Cmax (ng/mL) Tmax (h) F (%)
i.v. 2 0.7 3.3 2.4 13820.0
p.o. 10 33811.0 6600.0 0.5 48.9

CD-1 mouse; 2 mg/kg for i.v.; 10 mg/kg for o.p.[1].

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

Animal Model: CD-1 mouse[1]
Dosage:
Administration: 2 mg/kg for i.v.; 10 mg/kg for o.p.
Result: Showed good oral bioavailability and high plasma exposure.

分子量

800.75

Formula

C35H47BrN9O4PS
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]. Fang H, et al. Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFRdel19/T790M/C797S and EGFRL858R/T790M/C797S). Bioorg Med Chem Lett. 2022; 9:128729.

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

PI3K-IN-31

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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。

PI3K-IN-31 

PI3K-IN-31 (Compound 6b) 是一种有效的 PI3K 抑制剂，对 PI3Kα、PI3Kβ、PI3Kγ 和 PI3Kδ 的 IC50 分别为 3.7 nM、74 nM、14.6 nM 和 9.9 nM。PI3K-IN-31 具有抗癌作用。

PI3K-IN-31

PI3K-IN-31 Chemical Structure

CAS No. : 1359956-12-9

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

PI3K-IN-31 (Compound 6b) is a potent PI3K inhibitor with IC50s of 3.7 nM, 74 nM, 14.6 nM, and 9.9 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. PI3K-IN-31 has anticancer effects[1].

IC50 & Target[1]

PI3Kα

3.7 nM (IC50)

PI3Kδ

9.9 nM (IC50)

PI3Kγ

14.6 nM (IC50)

PI3Kβ

74 nM (IC50)

分子量

435.43

Formula

C19H23F2N7O3
CAS 号

1359956-12-9
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]. Marcian E Van Dort, et al. Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors. Eur J Med Chem. 2022 Feb 5;229:113996.

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

EGFR-IN-48

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。

EGFR-IN-48 

EGFR-IN-48 是一种有效的且具有口服活性的 EGFR 抑制剂，对 EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWT 的 IC50 值分别为 0.193 nM, 0.251 nM, 10.4 nM。EGFR-IN-48 抑制 BaF3EGFR del19/T790M/C797S 和 PC-9EGFR del19/T790M/C797S 细胞的增殖，IC50 值分别为 1.526 nM 和 66.7 nM。

EGFR-IN-48

EGFR-IN-48 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

EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively[1].

IC50 & Target

EGFRd19/TM/CS

0.193 nM (IC50)

EGFRLR/TM/CS

0.251 nM (IC50)

EGFRWT

10.4 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-48 (compound 23) (10 nM) shows anti-proliferative activities against BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively[1].
EGFR-IN-48 exhibits potent inhibitory activities against various clinically relevant EGFR mutants with IC50s of 10.4, 3.1, 0.9, 0.1, 0.2, 0.3, 0.2 nM for EGFRWT, EGFRLR, EGFRdel19, EGFRdel19/TM, EGFRLR/TM, EGFRLR/TM/CS, EGFRdrl19/TM/CS, respectively[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: BaF3EGFR del19/T790M/C797S, PC-9EGFR del19/T790M/C797S cells
Concentration: 10 nM
Incubation Time:
Result: Showed anti-proliferative activities against BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively.

体内研究
(In Vivo)

EGFR-IN-48 (2 mg/kg for i.v.; 10 mg/kg for o.p.) shows good oral bioavailability and high plasma exposure in CD-1 mouse[1]. Pharmacokinetic Parameters of EGFR-IN-48 in CD-1 mouse[1].

Route Dose (mg/kg) Vdss (L/kg) T1/2 (h) CL (L/h/kg) AUC0-last (h*ng/mL) Cmax (ng/mL) Tmax (h) F (%)
i.v. 2 0.7 3.3 2.4 13820.0
p.o. 10 33811.0 6600.0 0.5 48.9

CD-1 mouse; 2 mg/kg for i.v.; 10 mg/kg for o.p.[1].

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

Animal Model: CD-1 mouse[1]
Dosage:
Administration: 2 mg/kg for i.v.; 10 mg/kg for o.p.
Result: Showed good oral bioavailability and high plasma exposure.

分子量

800.75

Formula

C35H47BrN9O4PS
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]. Fang H, et al. Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFRdel19/T790M/C797S and EGFRL858R/T790M/C797S). Bioorg Med Chem Lett. 2022; 9:128729.

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

SHP2-IN-8

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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。

SHP2-IN-8 

SHP2-IN-8 是一种高效、具有选择性和细胞活性的变构 SHP2 抑制剂，IC50 为 23 nM，Ki 为 22 nM。SHP2-IN-8 可逆的、非竞争性的。SHP2-IN-8 能引起显著的热位移，ΔTm 为 7.01 ℃。SHP2-IN-8 可诱导 Hela 细胞凋亡 (apoptosis)，抑制 AKT 的磷酸化。

SHP2-IN-8

SHP2-IN-8 Chemical Structure

CAS No. : 1801692-60-3

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

SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells[1].

IC50 & Target

IC50: 23 nM (SHP2)[1]
Ki: 22 nM (SHP2)[1]
体外研究
(In Vitro)

SHP2-IN-8 (compound TK-453) (0-100 μM; 48 hours) has moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells[1].
SHP2-IN-8 (0-30 μM; 24 hours) induces the apoptosis of Hela cells in a concentration-dependent manner[1].
SHP2-IN-8 (0-30 μM; 0-2 hour）concentration- and time-dependently inhibits the phosphorylation of AKT in Hela and KYSE-70 cell lines[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: Hela, KYSE-70, THP-1[1]
Concentration: 0, 1, 3, 10, 30 and 100 μM
Incubation Time: 48 hours
Result: Showed moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells at the concentrations of 30 and 100 μM.

Apoptosis Analysis

Cell Line: Hela[1]
Concentration: 0, 10 and 30 μM
Incubation Time: 24 hours
Result: Induced the apoptosis of Hela cells in a concentration-dependent manner.

Western Blot Analysis

Cell Line: Hela and KYSE-70[1]
Concentration: 0, 0.3, 1, 3, 10 and 30 μM; or 10 μM
Incubation Time: 2 hours; or 0, 5, 10, 15, 30, 60, 120 min
Result: Concentration- and time-dependently inhibited the phosphorylation of AKT in Hela and KYSE-70 cell lines.

分子量

398.35

Formula

C17H21Cl2N5S
CAS 号

1801692-60-3
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]. Tang K, Zhao M, Wu YH, et al. Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors. Eur J Med Chem. 2022;230:114106.

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SHP2-IN-8

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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。

SHP2-IN-8 

SHP2-IN-8 是一种高效、具有选择性和细胞活性的变构 SHP2 抑制剂，IC50 为 23 nM，Ki 为 22 nM。SHP2-IN-8 可逆的、非竞争性的。SHP2-IN-8 能引起显著的热位移，ΔTm 为 7.01 ℃。SHP2-IN-8 可诱导 Hela 细胞凋亡 (apoptosis)，抑制 AKT 的磷酸化。

SHP2-IN-8

SHP2-IN-8 Chemical Structure

CAS No. : 1801692-60-3

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

SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells[1].

IC50 & Target

IC50: 23 nM (SHP2)[1]
Ki: 22 nM (SHP2)[1]
体外研究
(In Vitro)

SHP2-IN-8 (compound TK-453) (0-100 μM; 48 hours) has moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells[1].
SHP2-IN-8 (0-30 μM; 24 hours) induces the apoptosis of Hela cells in a concentration-dependent manner[1].
SHP2-IN-8 (0-30 μM; 0-2 hour）concentration- and time-dependently inhibits the phosphorylation of AKT in Hela and KYSE-70 cell lines[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: Hela, KYSE-70, THP-1[1]
Concentration: 0, 1, 3, 10, 30 and 100 μM
Incubation Time: 48 hours
Result: Showed moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells at the concentrations of 30 and 100 μM.

Apoptosis Analysis

Cell Line: Hela[1]
Concentration: 0, 10 and 30 μM
Incubation Time: 24 hours
Result: Induced the apoptosis of Hela cells in a concentration-dependent manner.

Western Blot Analysis

Cell Line: Hela and KYSE-70[1]
Concentration: 0, 0.3, 1, 3, 10 and 30 μM; or 10 μM
Incubation Time: 2 hours; or 0, 5, 10, 15, 30, 60, 120 min
Result: Concentration- and time-dependently inhibited the phosphorylation of AKT in Hela and KYSE-70 cell lines.

分子量

398.35

Formula

C17H21Cl2N5S
CAS 号

1801692-60-3
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]. Tang K, Zhao M, Wu YH, et al. Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors. Eur J Med Chem. 2022;230:114106.

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

SHP2-IN-8

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。

SHP2-IN-8 

SHP2-IN-8 是一种高效、具有选择性和细胞活性的变构 SHP2 抑制剂，IC50 为 23 nM，Ki 为 22 nM。SHP2-IN-8 可逆的、非竞争性的。SHP2-IN-8 能引起显著的热位移，ΔTm 为 7.01 ℃。SHP2-IN-8 可诱导 Hela 细胞凋亡 (apoptosis)，抑制 AKT 的磷酸化。

SHP2-IN-8

SHP2-IN-8 Chemical Structure

CAS No. : 1801692-60-3

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

SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells[1].

IC50 & Target

IC50: 23 nM (SHP2)[1]
Ki: 22 nM (SHP2)[1]
体外研究
(In Vitro)

SHP2-IN-8 (compound TK-453) (0-100 μM; 48 hours) has moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells[1].
SHP2-IN-8 (0-30 μM; 24 hours) induces the apoptosis of Hela cells in a concentration-dependent manner[1].
SHP2-IN-8 (0-30 μM; 0-2 hour）concentration- and time-dependently inhibits the phosphorylation of AKT in Hela and KYSE-70 cell lines[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: Hela, KYSE-70, THP-1[1]
Concentration: 0, 1, 3, 10, 30 and 100 μM
Incubation Time: 48 hours
Result: Showed moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells at the concentrations of 30 and 100 μM.

Apoptosis Analysis

Cell Line: Hela[1]
Concentration: 0, 10 and 30 μM
Incubation Time: 24 hours
Result: Induced the apoptosis of Hela cells in a concentration-dependent manner.

Western Blot Analysis

Cell Line: Hela and KYSE-70[1]
Concentration: 0, 0.3, 1, 3, 10 and 30 μM; or 10 μM
Incubation Time: 2 hours; or 0, 5, 10, 15, 30, 60, 120 min
Result: Concentration- and time-dependently inhibited the phosphorylation of AKT in Hela and KYSE-70 cell lines.

分子量

398.35

Formula

C17H21Cl2N5S
CAS 号

1801692-60-3
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]. Tang K, Zhao M, Wu YH, et al. Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors. Eur J Med Chem. 2022;230:114106.

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

Tutuilamide A

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。

Tutuilamide A 

Tutuilamide A 是一种有效的猪胰弹性蛋白酶 (PPE) 抑制剂，IC50 值为 1.2 nM。Tutuilamide A 还抑制人中性粒细胞弹性蛋白酶 (HNE; IC50=0.73 nM) 和激肽释放酶 7 (KLK7; IC50=5.0 nM)。

Tutuilamide A

Tutuilamide A Chemical Structure

CAS No. : 2756129-42-5

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

Tutuilamide A is a potent porcine pancreatic elastase (PPE) inhibitor, with an IC50 of 1.2 nM. Tutuilamide A also inhibits human neutrophil elastase (HNE; IC50=0.73 nM) and kallikrein 7 (KLK7; IC50=5.0 nM)[1].

IC50 & Target

IC50: 1.2 nM (porcine pancreatic elastase), 0.73 nM (human neutrophil elastase), 5.0 nM (kallikrein 7)[1]
分子量

1021.59

Formula

C51H69ClN8O12
CAS 号

2756129-42-5
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]. Chen QY, et, al. Ahp-Cyclodepsipeptides as tunable inhibitors of human neutrophil elastase and kallikrein 7: Total synthesis of tutuilamide A, serine protease selectivity profile and comparison with lyngbyastatin 7. Bioorg Med Chem. 2020 Dec 1;28(23):115756.

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