标签归档：ask

TC ASK 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。

TC ASK 10  纯度: ≥99.0%

TC ASK 10 (Compound 10) 是一种有效的，选择性的，口服活性的细胞凋亡信号调节激酶 1 (ASK1) 抑制剂，IC50 为 14 nM。TC ASK 10 对其他代表性激酶的抑制活性低于 50％，ASK2 除外 (IC50 为 0.51 μM)。

TC ASK 10

TC ASK 10 Chemical Structure

CAS No. : 1005775-56-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3660 In-stock
5 mg ￥3850 In-stock
10 mg ￥6500 询价
25 mg ￥12850 询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

TC ASK 10 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • Anti-Cancer Compound Library
  • Oxygen Sensing Compound Library
  • Orally Active Compound Library

生物活性

TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM)[1].

IC50 & Target[1]

ASK1

14 nM (IC50)

体外研究
(In Vitro)

TC ASK 10 (Compound 10; 0-10 μM; 1 hour; INS-1 cells) treatment inhibits streptozotocin (STZ)-induced JNK in INS-1 pancreatic β cells from 0.3 μM. Phosphorylation of p38 is also inhibited in a dosedependent 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: INS-1 cells
Concentration: 0 μM, 0.3 μM, 1 μM, 3 μM, 10 μM
Incubation Time: 1 hour
Result: Was found to inhibit streptozotocin (STZ)-induced JNK in INS-1 pancreatic β cells from 0.3 μM. Phosphorylation of p38 was also inhibited in a dosedependent manner.

体内研究
(In Vivo)

Pharmacokinetic profiles in rats are tested. TC ASK 10 (Compound 10•HCl; rat cassette doing at 0.1 mg/kg, iv and 1 mg/kg, po.) has a good oral bioavailability. The Cmax, Tmax and AUCpo,0-8h are 285.1 ng/mL, 1.67 h and 275.4 ng.h/mL, respectively for TC ASK 10[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

432.35

Formula

C21H23Cl2N5O
CAS 号

1005775-56-3
运输条件

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

4°C, sealed storage, away from moisture

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

DMSO : 100 mg/mL (231.29 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3129 mL 11.5647 mL 23.1294 mL
5 mM 0.4626 mL 2.3129 mL 4.6259 mL
10 mM 0.2313 mL 1.1565 mL 2.3129 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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: ≥ 2.5 mg/mL (5.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.78 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

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

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.78 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.78 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Terao Y, et al. Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7326-9.

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

ASK1-IN-3

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。

ASK1-IN-3 

ASK1-IN-3 是一种有效且具有选择性的 ASK1 激酶抑制剂，IC50 为 33.8 nM，同时也抑制多种细胞周期调节激酶。ASK1-IN-3 具有较强的 HepG2 癌细胞凋亡 (apoptosis) 诱导活性与有效的细胞周期阻滞活性。

ASK1-IN-3

ASK1-IN-3 Chemical Structure

CAS No. : 2426705-19-1

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

ASK1-IN-3 is a potent and selective ASK1 kinase inhibitor with IC50 of 33.8 nM, as well as inhibits several cell cycle regulating kinases. ASK1-IN-3 has strong HepG2 cancer cells apoptosis induction and potent cell cycle arrest activities[1].

IC50 & Target

IC50: 33.8 nM (ASK1)[1]
体外研究
(In Vitro)

ASK1-IN-3 (compound 14l) (10, 20 and 50 μM; 48 hours) induces PARP cleavage in a dose dependent manner, which indicates the induction of HepG2 cells apoptosis[1].
ASK1-IN-3 (1-16 μM; 24 hours) significantly arrests cycle progression at G1 phase[1].

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

Apoptosis Analysis

Cell Line: HepG2[1]
Concentration: 10, 20 and 50 μM
Incubation Time: 48 hours
Result: Induced PARP cleavage in a dose dependent manner.

Cell Cycle Analysis

Cell Line: HepG2[1]
Concentration: 1, 2, 4, 8, and 16 μM
Incubation Time: 24 hours
Result: Significantly arrested cycle progression at G1 phase.

分子量

378.39

Formula

C18H18N8O2
CAS 号

2426705-19-1
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]. Zhang S, Huang C, Lyu X, et al. Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1). Eur J Med Chem. 2020;195:112277.

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

ASK1-IN-3

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。

ASK1-IN-3 

ASK1-IN-3 是一种有效且具有选择性的 ASK1 激酶抑制剂，IC50 为 33.8 nM，同时也抑制多种细胞周期调节激酶。ASK1-IN-3 具有较强的 HepG2 癌细胞凋亡 (apoptosis) 诱导活性与有效的细胞周期阻滞活性。

ASK1-IN-3

ASK1-IN-3 Chemical Structure

CAS No. : 2426705-19-1

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

ASK1-IN-3 is a potent and selective ASK1 kinase inhibitor with IC50 of 33.8 nM, as well as inhibits several cell cycle regulating kinases. ASK1-IN-3 has strong HepG2 cancer cells apoptosis induction and potent cell cycle arrest activities[1].

IC50 & Target

IC50: 33.8 nM (ASK1)[1]
体外研究
(In Vitro)

ASK1-IN-3 (compound 14l) (10, 20 and 50 μM; 48 hours) induces PARP cleavage in a dose dependent manner, which indicates the induction of HepG2 cells apoptosis[1].
ASK1-IN-3 (1-16 μM; 24 hours) significantly arrests cycle progression at G1 phase[1].

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

Apoptosis Analysis

Cell Line: HepG2[1]
Concentration: 10, 20 and 50 μM
Incubation Time: 48 hours
Result: Induced PARP cleavage in a dose dependent manner.

Cell Cycle Analysis

Cell Line: HepG2[1]
Concentration: 1, 2, 4, 8, and 16 μM
Incubation Time: 24 hours
Result: Significantly arrested cycle progression at G1 phase.

分子量

378.39

Formula

C18H18N8O2
CAS 号

2426705-19-1
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]. Zhang S, Huang C, Lyu X, et al. Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1). Eur J Med Chem. 2020;195:112277.

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

ASK1-IN-3

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。

ASK1-IN-3 

ASK1-IN-3 是一种有效且具有选择性的 ASK1 激酶抑制剂，IC50 为 33.8 nM，同时也抑制多种细胞周期调节激酶。ASK1-IN-3 具有较强的 HepG2 癌细胞凋亡 (apoptosis) 诱导活性与有效的细胞周期阻滞活性。

ASK1-IN-3

ASK1-IN-3 Chemical Structure

CAS No. : 2426705-19-1

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

ASK1-IN-3 is a potent and selective ASK1 kinase inhibitor with IC50 of 33.8 nM, as well as inhibits several cell cycle regulating kinases. ASK1-IN-3 has strong HepG2 cancer cells apoptosis induction and potent cell cycle arrest activities[1].

IC50 & Target

IC50: 33.8 nM (ASK1)[1]
体外研究
(In Vitro)

ASK1-IN-3 (compound 14l) (10, 20 and 50 μM; 48 hours) induces PARP cleavage in a dose dependent manner, which indicates the induction of HepG2 cells apoptosis[1].
ASK1-IN-3 (1-16 μM; 24 hours) significantly arrests cycle progression at G1 phase[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.

Apoptosis Analysis

Cell Line: HepG2[1]
Concentration: 10, 20 and 50 μM
Incubation Time: 48 hours
Result: Induced PARP cleavage in a dose dependent manner.

Cell Cycle Analysis

Cell Line: HepG2[1]
Concentration: 1, 2, 4, 8, and 16 μM
Incubation Time: 24 hours
Result: Significantly arrested cycle progression at G1 phase.

分子量

378.39

Formula

C18H18N8O2
CAS 号

2426705-19-1
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]. Zhang S, Huang C, Lyu X, et al. Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1). Eur J Med Chem. 2020;195:112277.

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

ASK120067

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。

ASK120067  纯度: 98.01%

ASK120067 是一种有效的口服活性 EGFRT790M 抑制剂 (IC50:0.3 nM)，对 EGFRWT(IC50:6.0 nM) 具有选择性。ASK120067 是用于非小细胞肺癌 (NSCLC) 研究的第三代 EGFR-TKI。

ASK120067

ASK120067 Chemical Structure

CAS No. : 1934259-00-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3600 In-stock
5 mg ￥3000 In-stock
10 mg ￥4800 In-stock
25 mg ￥9500 In-stock
50 mg ￥14500 In-stock
100 mg ￥22500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

ASK120067 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Drug Repurposing Compound Library
  • Covalent Screening Library
  • Differentiation Inducing Compound Library
  • Orally Active Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1].

IC50 & Target[1]

EGFRT790M

0.5 nM (IC50)

EGFRL858R/T790M

0.3 nM (IC50)

EGFR (WT)

6 nM (IC50)

EGFRExon 19 deletion

0.5 nM (IC50)

体外研究
(In Vitro)

In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT) is 6 nM[1].
ASK120067 selectively inhibits the growth of EGFR-mutant cell lines and exhibits potent antiproliferative activity in the mutant EGFR NSCLC cells, with IC50 values of 12 nM, 6 nM and 2 nM against NCI-H1975 (T790M mutation), PC-9, and HCC827 cells (sensitizing mutations), respectively. However, it shows moderate or weak anti-growth activities in A431, LoVo and A549 cells (EGFRWT), with IC50 values ranging from 338 nM to 1541 nM[1].
ASK120067 (0.1-100 nM) inhibits the phosphorylation of EGFR at Tyrosine residue 1068 and its downstream signaling proteins AKT and ERK in NCI-H1975 cells (EGFRL858R/T790M) even at low dosage (0.1-1 nM). Additionally, ASK120067 inhibits p-EGFR and p-Akt and p-erk in EGFR WT A431 cell until the concentration reaches 10 to 100 nM[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.
体内研究
(In Vivo)

ASK120067 (oral gavage; 5-20 mg/kg; once daily; 21 days) results in significantly regressed tumor growth, with a tumor growth inhibition (TGI) rate of 85.7%, and administration of 10 mg/kg ASK120067 causes dramatic tumor shrinkage with a TGI rate of 99.3%, exhibiting a similar potency with Osimertinib[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/cA nude mice[1]
Dosage: 5-20 mg/kg
Administration: Oral gavage; 5-20 mg/kg; once daily; 21 days
Result: Were well tolerated in animals without observed body weight loss
Demonstrated profound and selective antitumor efficacy and decreased TGI rate.
Significantly inhibited the phosphorylation of EGFR L858R/T790M and AKT in tumor tissue.

Clinical Trial

分子量

546.06

Formula

C29H32ClN7O2
CAS 号

1934259-00-3
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 : 41.67 mg/mL (76.31 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8313 mL 9.1565 mL 18.3130 mL
5 mM 0.3663 mL 1.8313 mL 3.6626 mL
10 mM 0.1831 mL 0.9157 mL 1.8313 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: ≥ 2.5 mg/mL (4.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.58 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

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

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.81 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]. Tao Zhang, et al. Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol Cancer. 2020 May 13;19(1):90.

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