Tyrphostin AG1296(Synonyms: AG1296)

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。

Tyrphostin AG1296 (Synonyms: AG1296) 纯度: 99.25%

Tyrphostin AG1296 是一种有效的、选择性血小板衍生生长因子受体 (PDGFR) 抑制剂,IC50 值为 0.8 μM。Tyrphostin AG1296 抑制人 PDGF αβ 受体以及相关干细胞因子受体 (c-Kit) 的信号传导。Tyrphostin AG1296 也是有效的 FLT3 抑制剂,IC50 值在微摩尔范围内。

Tyrphostin AG1296(Synonyms: AG1296)

Tyrphostin AG1296 Chemical Structure

CAS No. : 146535-11-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1100 In-stock
5 mg ¥1000 In-stock
10 mg ¥1700 In-stock
25 mg ¥3500 In-stock
50 mg ¥5500 In-stock
100 mg ¥9500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Tyrphostin AG1296 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
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  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Cardiovascular Disease Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range[1][2][3].

IC50 & Target

PDGFRα

 

PDGFRβ

 

体外研究
(In Vitro)

Tyrphostin AG1296 (0.625-20 μM; 72 h) suppresses viability of PLX4032-resistant melanoma cells[4].
Tyrphostin AG1296 (2.5-20 μM; 48 h) induces apoptosis of A375R cells[4].
Tyrphostin AG1296 (5 and 20 μM; 2 h) inhibits PDGFR phosphorylation in A375R cells[4].
Tyrphostin AG1296 (0.0625-1 μM; 8 h) inhibits migration of A375R cells[4].

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 Viability Assay[4]

Cell Line: PLX4032-resistant cell lines (A375R and SK-MEL-5R)
Concentration: 0.625, 1.25, 5, 20 μM
Incubation Time: 72 h
Result: Reduced the viability of both PLX4032-sensitive and PLX4032-resistant cell lines.

Apoptosis Analysis[4]

Cell Line: A375R cells
Concentration: 2.5, 5, 10, 20 μM
Incubation Time: 48 h
Result: Induced dramatic apoptosis in A375R cells.

Western Blot Analysis[4]

Cell Line: A375R cells
Concentration: 5, 20 μM
Incubation Time: 2 h
Result: Inhibited phosphorylation of both PDGFR-α and PDGFR-β.

体内研究
(In Vivo)

Tyrphostin AG1296 (40 and 80 mg/kg; i.p. daily for two weeks) suppresses A375R tumor growth in vivo[4].
Tyrphostin AG1296 (2 mg/kg; i.p. every other day for 3 weeks) inhibits the atherosclerotic plaque progression and enhances plaque stability by inhibiting inflammatory responses, reducing the expression of matrix metalloproteinases and promoting macrophages from proinflammatory phenotype to anti-inflammatory phenotype[5].

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: Nud/nud mice are injected with A375R cells[4]
Dosage: 40, 80 mg/kg
Administration: I.p. daily for two weeks
Result: Led to an intermediate level of tumor growth suppression at dose of 40 mg/kg, and significant inhibition of A375R tumor growth at dose of 80 mg/kg.
Well tolerated by healthy mice without significant signs of overt toxicity or weight loss.

分子量

266.29

Formula

C16H14N2O2

CAS 号

146535-11-7

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 : 33.33 mg/mL (125.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7553 mL 18.7765 mL 37.5530 mL
5 mM 0.7511 mL 3.7553 mL 7.5106 mL
10 mM 0.3755 mL 1.8777 mL 3.7553 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    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (9.39 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (9.39 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 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
  • 2.

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

    Solubility: ≥ 2.5 mg/mL (9.39 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.39 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]. Gazit A, etm, al. Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins. Comparative Study J Med Chem. 1996 May 24; 39(11): 2170-7.

    [2]. Kovalenko M, et, al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Res. 1994 Dec 1; 54(23): 6106-14.

    [3]. Tse KF, et, al. Inhibition of the transforming activity of FLT3 internal tandem duplication mutants from AML patients by a tyrosine kinase inhibitor. Leukemia. 2002 Oct; 16(10): 2027-36.

    [4]. Li Y, et, al. Tyrphostin AG1296, a platelet-derived growth factor receptor inhibitor, induces apoptosis, and reduces viability and migration of PLX4032-resistant melanoma cells. Onco Targets Ther. 2015 May 14; 8: 1043-51.

    [5]. Dong M, et, al. AG1296 enhances plaque stability via inhibiting inflammatory responses and decreasing MMP-2 and MMP-9 expression in ApoE-/- mice. Biochem Biophys Res Commun. 2017 Aug 5;489(4):426-431.

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SV40 T-Ag-derived NLS peptide

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。

SV40 T-Ag-derived NLS peptide 

SV40 T-Ag-derived NLS peptide 是一种核定位信号肽,标记该肽的 DNA 可有效地转移到细胞核中。

SV40 T-Ag-derived NLS peptide

SV40 T-Ag-derived NLS peptide Chemical Structure

CAS No. : 105425-98-7

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

SV40 T-Ag-derived NLS peptide is a nuclear localization signal DNA tagged to this peptide efficiently translocates into the cell nucleus[1].

分子量

1490.77

Formula

C66H111N19O18S

CAS 号

105425-98-7

Sequence Shortening

PKKKRKVEDPYC

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.

Solvent & Solubility
In Vitro: 

H2O

Peptide Solubility and Storage Guidelines:

1.  Calculate the length of the peptide.

2.  Calculate the overall charge of the entire peptide according to the following table:

  Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.  Recommended solution:

Overall charge of peptide Details
Negative (<0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, add NH4OH (<50 μL).
3.  If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.  If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.  Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.  For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献
  • [1]. Benimetskaya L, et al. Protamine-fragment peptides fused to an SV40 nuclear localization signal deliver oligonucleotides that produce antisense effects in prostate and bladder carcinoma cells. Bioconjug Chem. 2002 Mar-Apr;13(2):177-87.

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AG-825(Synonyms: Tyrphostin AG-825)

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。

AG-825 (Synonyms: Tyrphostin AG-825) 纯度: 98.07%

AG-825 是一种选择性、ATP竞争性,抑制酪氨酸磷酸化的 ErbB2 抑制剂,其 IC50 值为 0.35 μM。AG-825 具有抗癌活性。AG825 能明显加速人中性粒细胞的凋亡。AG-825 是一种潜在的克服锰诱导的神经毒性或阿尔茨海默病发展的药物。

AG-825(Synonyms: Tyrphostin AG-825)

AG-825 Chemical Structure

CAS No. : 149092-50-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥880 In-stock
5 mg ¥800 In-stock
10 mg ¥1400 In-stock
25 mg ¥3000 In-stock
50 mg ¥5000 In-stock
100 mg ¥8000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AG-825 相关产品

相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

AG-825 (Tyrphostin AG-825) is a selective and ATP-competitive ErbB2 inhibitor which suppresses tyrosine phosphorylation, with an IC50 of 0.35 μM. AG-825 displays anti-cancer activity[1][2][3]. AG825 significantly accelerates apoptosis of human neutrophils[4]. AG-825 is a potential agent for overcoming Mn-induced neurotoxicity or AD development[5].

IC50 & Target[2]

ErbB2

0.35 μM (IC50)

EGFR

19 μM (IC50)

分子量

397.47

Formula

C19H15N3O3S2

CAS 号

149092-50-2

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 : 250 mg/mL (628.98 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5159 mL 12.5796 mL 25.1591 mL
5 mM 0.5032 mL 2.5159 mL 5.0318 mL
10 mM 0.2516 mL 1.2580 mL 2.5159 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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.23 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 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
*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]. Wolfson E, et al. Nucleolin and ErbB2 inhibition reduces tumorigenicity of ErbB2-positive breast cancer. Cell Death Dis. 2018 Jan 19;9(2):47.

    [2]. Gazit A, et al. Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins. J Med Chem. 1993 Nov 12;36(23):3556-64.

    [3]. He H, et al. Signal therapy for RAS-induced cancers in combination of AG 879 and PP1, specific inhibitors for ErbB2 and Src family kinases, that block PAK activation. Cancer J. 2001 May-Jun;7(3):191-202.

    [4]. Rahman A, et al. Inhibition of ErbB kinase signalling promotes resolution of neutrophilic inflammation. Elife. 2019 Oct 15;8. pii: e50990.

    [5]. Ling J, et al. Identifying key genes, pathways and screening therapeutic agents for manganese-induced Alzheimer disease using bioinformatics analysis. Medicine (Baltimore). 2018 Jun;97(22):e10775.

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Tyrphostin AG 528(Synonyms: Tyrphostin B66; AG 528)

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。

Tyrphostin AG 528 (Synonyms: Tyrphostin B66; AG 528) 纯度: ≥98.0%

Tyrphostin AG-528 (Tyrphostin B66) 是一种蛋白酪氨酸激酶抑制剂,对表皮生长因子受体 (EGFR) 的 IC50 为 4.9 μM,对 ErbB2IC50 为 2.1 μM。Tyrphostin AG-528 也是一种抗癌剂。

Tyrphostin AG 528(Synonyms: Tyrphostin B66;  AG 528)

Tyrphostin AG 528 Chemical Structure

CAS No. : 133550-49-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550 In-stock
5 mg ¥500 In-stock
10 mg ¥850 In-stock
25 mg ¥1700 In-stock
50 mg ¥2900 In-stock
100 mg ¥5200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Tyrphostin AG 528 相关产品

相关化合物库:

  • Covalent Screening 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
  • Covalent Screening Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Breast Cancer 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

Tyrphostin AG 528 is an inhibitor of EGFR and ErbB2 with IC50s of 4.9 and 2.1 μM, respectively. Tyrphostin AG 528 (Tyrphostin B66) is a protein tyrosine kinase inhibitor, with IC50s of 4.9 μM for epidermal growth factor receptors (EGFR) and 2.1 μM for ErbB2[1]. Tyrphostin AG 528 is also an anticancer agent[2].

IC50 & Target

EGFR

4.9 μM (IC50)

ErbB2

2.1 μM (IC50)

体外研究
(In Vitro)

In the present study, the interaction between drug Tyrphostin AG528 and CNT(6,6-6) nanotube by Density Functional Theory (DFT) calculations in solvent water has been investigated for the first time. According to the calculations, intermolecular hydrogen bonds take place between an active position of the molecule Tyrphostin AG528 and hydrogen atoms of the nanotube which play an important role in the stability of complex CNT(6,6- 6)/Tyrphostin AG528. The non-bonded interaction effects of the molecule Tyrphostin AG528 with CNT(6,6-6) nanotube on the electronic properties, chemical shift tensors and natural charge have also been detected. The natural bond orbital (NBO) analysis suggested that the molecule Tyrphostin AG528 as an electron donor and the CNT(6,6-6) nanotube play the role of an electron acceptor at the complex CNT(6,6-6)/Tyrphostin AG528[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.

分子量

306.32

Formula

C18H14N2O3

CAS 号

133550-49-9

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 : 25 mg/mL (81.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2646 mL 16.3228 mL 32.6456 mL
5 mM 0.6529 mL 3.2646 mL 6.5291 mL
10 mM 0.3265 mL 1.6323 mL 3.2646 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 (8.16 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.16 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 (8.16 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.16 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
*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]. Naijue Zhu, et al. Tyrphostin Tumor Growth Inhibitors of EGFR and ErbB2 Tyrosine Kinase. J Chem Crystallogr. 2007, 37, 679–683.

    [2]. Sheikhi M, et al. Investigation of Adsorption Tyrphostin AG528 Anticancer Drug Upon the CNT(6,6-6) Nanotube: A DFT Study. Curr Mol Med. 2019;19(2):91-104.

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Tyrphostin AG1433(Synonyms: SU1433; AG1433)

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。

Tyrphostin AG1433 (Synonyms: SU1433; AG1433) 纯度: 99.20%

Tyrphostin AG1433 (SU1433) 是酪氨酸激酶抑制剂。Tyrphostin AG1433 还是一种选择性的 PDGFRβVEGFR-2 (Flk-1/KDR) 抑制剂,IC50 分别为 5.0 μM 和 9.3 μM。Tyrphostin AG1433 可防止血管形成。

Tyrphostin AG1433(Synonyms: SU1433;  AG1433)

Tyrphostin AG1433 Chemical Structure

CAS No. : 168835-90-3

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生物活性

Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation[1][2][3][4].

IC50 & Target[2]

Flk-1

9.3 μM (IC50)

PDGFRβ

5 μM (IC50)

体外研究
(In Vitro)

Tyrphostin AG1433 (0.1-100 μM; 72 hours; GB8B cells) treatment induces moderate cytotoxicity in glioblastoma 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 Viability Assay[1]

Cell Line: GB8B cells
Concentration: 0.1 μM, 1 μM, 5 μM, 10 μM, 20 μM, 30 μM, 50 μM, 60 μM, 100 μM
Incubation Time: 72 hours
Result: Induced significant cell death in GB8B cells in a concentration-dependent manner.

体内研究
(In Vivo)

Chorion allantoic membrane (CAM) assays are used to determine the effects of the Flk-i inhibitors on angiogenesis. Tyrphostin AG1433 (SU1433) is prepared in methylcellulose pellets and applies to the CAMs of 4-6-day-old chicken embryos. Tyrphostin AG1433 prevents the formation of new yessels under the pellets[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.

分子量

266.29

Formula

C16H14N2O2

CAS 号

168835-90-3

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 : 62.5 mg/mL (234.71 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7553 mL 18.7765 mL 37.5530 mL
5 mM 0.7511 mL 3.7553 mL 7.5106 mL
10 mM 0.3755 mL 1.8777 mL 3.7553 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 (7.81 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.81 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

*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]. Serban F, et al. Silencing of epidermal growth factor, latrophilin and seven transmembrane domain-containing protein 1 (ELTD1) via siRNA-induced cell death in glioblastoma. J Immunoassay Immunochem. 2017;38(1):21-33.

    [2]. Strawn LM, et al. Flk-1 as a target for tumor growth inhibition. Cancer Res. 1996 Aug 1;56(15):3540-5.

    [3]. Kim TS, et al. The ZFHX3 (ATBF1) transcription factor induces PDGFRB, which activates ATM in the cytoplasm to protect cerebellar neurons from oxidative stress. Dis Model Mech. 2010 Nov-Dec;3(11-12):752-62.

    [4]. Kroll J, et al. The vascular endothelial growth factor receptor KDR activates multiple signal transduction pathways in porcine aortic endothelial cells. J Biol Chem. 1997 Dec 19;272(51):32521-7.

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I-OMe-Tyrphostin AG 538(Synonyms: I-OMe-AG 538)

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。

I-OMe-Tyrphostin AG 538 (Synonyms: I-OMe-AG 538) 纯度: 99.34%

I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) 是 IGF-1R 激酶的特异性抑制剂。I-OMe-Tyrphostin AG 538 抑制 IGF-1R 介导的信号传导,并优先对营养缺乏的 PANC1 细胞产生细胞毒性。I-OMe-Tyrphostin AG 538 是具有 ATP 竞争性的 PI5P4Kα抑制剂,IC50 为 1 μM。

I-OMe-Tyrphostin AG 538(Synonyms: I-OMe-AG 538)

I-OMe-Tyrphostin AG 538 Chemical Structure

CAS No. : 1094048-77-7

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25 mg ¥5500 In-stock
50 mg ¥8500 In-stock
100 mg ¥13500 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM[1].

IC50 & Target

IC50: 1 µM (PI5P4Kα)[1]

体外研究
(In Vitro)

I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) (0.1-1000 µM; 24 hours) is cytotoxic to PANC-1 cells in nutrient-deprived medium[1].
I-OMe-Tyrphostin AG 538 (0-3 µM; 1 hour) blocks phosphorylation of IGF-1R, Akt and 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 Viability Assay[1]

Cell Line: PANC-1 cells
Concentration: 0.1, 1, 10, 1000 µM
Incubation Time: 24 hours
Result: Cytotoxic to PANC-1 cells in nutrient-deprived medium.

Western Blot Analysis[1]

Cell Line: PANC-1 cells (stimulation with 50 ng/ml IGF-1 for 10 min)
Concentration: 0.03, 0.3, 3 µM
Incubation Time: 1 hour
Result: Blocked phosphorylation of IGF-1R, Akt and Erk.

分子量

437.19

Formula

C17H12INO5

CAS 号

1094048-77-7

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 : 50 mg/mL (114.37 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2873 mL 11.4367 mL 22.8734 mL
5 mM 0.4575 mL 2.2873 mL 4.5747 mL
10 mM 0.2287 mL 1.1437 mL 2.2873 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 (5.72 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.72 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 (5.72 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.72 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
*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]. Davis MI, et al. A homogeneous, high-throughput assay for phosphatidylinositol 5-phosphate 4-kinase with a novel, rapid substrate preparation. PLoS One. 2013;8(1):e54127.

    [2]. Momose I, et al. Inhibitors of insulin-like growth factor-1 receptor tyrosine kinase are preferentially cytotoxic to nutrient-deprived pancreatic cancer cells. Biochem Biophys Res Commun. 2009 Feb 27;380(1):171-6.

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AG-024322

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。

AG-024322  纯度: 98.69%

AG-024322 是一种有效的 ATP 竞争性的 pan-CDK 抑制剂,抑制 CDK1, CDK2, CDK4 的 Ki 值在 1-3 nM 范围内。AG-024322 在体内表现出广谱抗肿瘤活性和清晰的靶标调控。AG-024322 诱导细胞凋亡 (apoptosis)。

AG-024322

AG-024322 Chemical Structure

CAS No. : 837364-57-5

规格 价格 是否有货 数量
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10 mg ¥9800 In-stock
25 mg ¥19500 In-stock
50 mg ¥31000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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生物活性

AG-024322 is a potent ATP-competitive pan-CDK inhibitor against cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range[1]. AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis[3].

IC50 & Target[1]

COX-1

2.3 nM (Ki)

COX-2

3 nM (Ki)

COX-4

2.9 nM (Ki)

体外研究
(In Vitro)

AG-024322 (0.1-30 μM; 24 hours) is less toxic at concentrations below 3 µM, the viability of human PBMCs as measured by ATP content with a TC50 value of 1.4 µM for human PBMCs[2].
AG-024322 (0-120 nM) exhibits growth inhibition effects on HCT-116 cells. It is slightly less potent in the functional cellular assay with an IC50 of 120 nM[2].

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

体内研究
(In Vivo)

AG-024322 (intravenous infusion; 2, 6, and 10 mg/kg; 5 days) exhibits no-adverse-effect at 2 mg/kg with mean plasma AUC (0-24.5) of 2.11 g.h/mL. At 6 mg/kg produces pancytic bone marrow hypocellularity, lymphoid depletion. And vascular injury at the injection site renal tubular degeneration occurs at 10 mg/kg[1].
AG-024322 (20 mg/kg) inhibits the growth of established human tumor xenografts of different origins with tumor growth inhibition (TGI) ranging from 32% to 86.4%.It also exhibits anti-tumor effects as a dose-pdependent manner[3].
AG-024322 (20 mg/kg) causes a 65% TGI in the MV522 tumor model. It results a 52% TGI at 1/2 of the maximum tolerated dose (MTD) and only slight anti-tumor activity at 1/4 of the MTD[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 and female cynomolgus monkeys[1]
Dosage: 2, 6, and 10 mg/kg (Toxicity analysis)
Administration: Intravenous infusion; 5 days
Result: Resulted in dose-dependent pancytic bone marrow hypocellularity and lymphoid depletion in lymph nodes, spleen, and/or thymus at >6 mg/kg.

Clinical Trial

分子量

418.44

Formula

C23H20F2N6

CAS 号

837364-57-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [1]. Brown AP, et al. Toxicity and toxicokinetics of the cyclin-dependent kinase inhibitor AG-024322 in cynomolgus monkeys following intravenous infusion.Cancer Chemother Pharmacol. 2008 Nov;62(6):1091-101.

    [2]. Jessen BA,et al. Peripheral white blood cell toxicity induced by broad spectrum cyclin-dependent kinase inhibitors.J Appl Toxicol. 2007 Mar-Apr;27(2):133-42.

    [3]. Cathy C. Zhang, et al. AG-024322 is a multi-targeted CDK inhibitor with potent antitumor activity in vivo. Cellular and Molecular Biology 53: Cell Cycle Control and Cancer 1

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AG-494(Synonyms: Tyrphostin AG 494)

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。

AG-494 (Synonyms: Tyrphostin AG 494) 纯度: 99.06%

AG-494 (Tyrphostin AG 494) 是一种高效、选择性的 EGFR 酪氨酸激酶抑制剂 (IC50=0.7 μM)。AG-494 抑制EGFR、ErbB2、HER1-2 和 PDGF-R 的自磷酸化,IC50 为 1.1,39,45 和 6 μM。AG-494 阻断 Cdk2 的激活并抑制 EGF 依赖的 DNA 合成。

AG-494(Synonyms: Tyrphostin AG 494)

AG-494 Chemical Structure

CAS No. : 133550-35-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1100 In-stock
10 mg ¥1000 In-stock
25 mg ¥1800 In-stock
50 mg ¥2800 In-stock
100 mg ¥4500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AG-494 相关产品

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生物活性

AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis[1][2][3].

IC50 & Target

EGFR

0.7 μM (IC50)

体外研究
(In Vitro)

In DHER-14 cells, AG 494 inhibits Cdk2 activation and EGF-dependent DNA synthesis[2].
AG-494 significantly prevents NF-kB activation in silica-stimulated cells, and also reduces NF-kB activation in H2O2-treated cells[4].
AG-494 (3-9 μM; 5-7 days) inhibits BMP9-induced ALP activity in a dose-dependent manner[5].

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

280.28

Formula

C16H12N2O3

CAS 号

133550-35-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (356.79 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5679 mL 17.8393 mL 35.6786 mL
5 mM 0.7136 mL 3.5679 mL 7.1357 mL
10 mM 0.3568 mL 1.7839 mL 3.5679 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 (protect from light)。-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 (8.92 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.92 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

*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]. Gazit A, et al. Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J Med Chem. 1991;34(6):1896-1907.

    [2]. Osherov N, et al. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett. 1997;410(2-3):187-190.

    [3]. Osherov N, et al. Selective inhibition of the epidermal growth factor and HER2/neu receptors by tyrphostins. J Biol Chem. 1993 May 25;268(15):11134-42.

    [4]. Liu X, Qin J, et al. Cross-talk between EGF and BMP9 signalling pathways regulates the osteogenic differentiation of mesenchymal stem cells. J Cell Mol Med. 2013;17(9):1160-1172.

    [5]. Jihee Lee Kang, et al. SILICA-INDUCED NUCLEAR FACTOR- k B ACTIVATION: INVOLVEMENT OF REACTIVE OXYGEN SPECIES AND PROTEIN TYROSINE KINASE ACTIVATION. Journal of Toxicology and Environmental Health, Part A.

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DMEM/F12培养基ADVANCED D-MEM/F-12

DMEM/F12培养基ADVANCED D-MEM/F-12

规格

  • 500ML
  • 产品详情
  • 产品参数

DMEM/F12培养基ADVANCED D-MEM/F-12Advanced DMEM/F-12(Dulbecco 改良 Eagle 培养基/Ham's F-12)是一种广泛使用的基础培养基,可在减少胎牛血清 (FBS) 添加量的情况下培养哺乳动物细胞

参数

别名
品牌 gibco产品订购
货号 12634010
货期 7
单位
保存条件 0

Tyrphostin AG 112

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。

Tyrphostin AG 112 

Tyrphostin AG 112 是 EGFR 磷酸化的抑制剂。

Tyrphostin AG 112

Tyrphostin AG 112 Chemical Structure

CAS No. : 144978-82-5

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

Tyrphostin AG 112 is an EGFR phosphorylation inhibitor[1].

分子量

236.23

Formula

C13H8N4O

CAS 号

144978-82-5

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]. Rodrigo Franco, et al. Epidermal Growth Factor Receptor Is Activated by Hyposmolarity and Is an Early Signal Modulating Osmolyte Efflux Pathways in Swiss 3T3 Fibroblasts. Pflugers Arch. 2004 Mar;447(6):830-9.

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

Tyrphostin AG 112

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。

Tyrphostin AG 112 

Tyrphostin AG 112 是 EGFR 磷酸化的抑制剂。

Tyrphostin AG 112

Tyrphostin AG 112 Chemical Structure

CAS No. : 144978-82-5

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

Tyrphostin AG 112 is an EGFR phosphorylation inhibitor[1].

分子量

236.23

Formula

C13H8N4O

CAS 号

144978-82-5

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]. Rodrigo Franco, et al. Epidermal Growth Factor Receptor Is Activated by Hyposmolarity and Is an Early Signal Modulating Osmolyte Efflux Pathways in Swiss 3T3 Fibroblasts. Pflugers Arch. 2004 Mar;447(6):830-9.

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

Tyrphostin AG 112

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。

Tyrphostin AG 112 

Tyrphostin AG 112 是 EGFR 磷酸化的抑制剂。

Tyrphostin AG 112

Tyrphostin AG 112 Chemical Structure

CAS No. : 144978-82-5

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

Tyrphostin AG 112 is an EGFR phosphorylation inhibitor[1].

分子量

236.23

Formula

C13H8N4O

CAS 号

144978-82-5

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]. Rodrigo Franco, et al. Epidermal Growth Factor Receptor Is Activated by Hyposmolarity and Is an Early Signal Modulating Osmolyte Efflux Pathways in Swiss 3T3 Fibroblasts. Pflugers Arch. 2004 Mar;447(6):830-9.

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

AG-1478 hydrochloride(Synonyms: Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride)

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。

AG-1478 hydrochloride (Synonyms: Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride)

AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) 是一种选择性的 EGFR 酪氨酸激酶抑制剂,IC50 为 3 nM。AG-1478 hydrochloride 对 HCV 和脑心肌炎病毒 (EMCV) 具有抗病毒作用。

AG-1478 hydrochloride(Synonyms: Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride)

AG-1478 hydrochloride Chemical Structure

CAS No. : 170449-18-0

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

* Please select Quantity before adding items.

AG-1478 hydrochloride 的其他形式现货产品:

AG-1478

生物活性

AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV)[1][2][3][4].

IC50 & Target

EGFR

3 nM (IC50)

HCV

 

EMCV

 

体外研究
(In Vitro)

AG-1478 (AG1478) is irreversible for growth regulation of human lung (A549) and prostate (DU145) cancer cell lines, cultured in chemically defined DMEM/F12 medium. AG-1478 seems to be more effective at lower concentrations, but is unable to completely inhibit growth of A549 cells[1]. Inhibition of EGFR by specific tyrosine kinase inhibitor AG-1478 (AG1478) significantly decreases the angiotensin II-mediated synthesis of TGF-β and fibronectin by cardiac fibroblasts. EGFR is pharmacologically inhibited by small-molecule inhibitor AG-1478 with IC50 of 4 nM[2]. Both Polyfect (PF) and Superfect (SF) treatment lead to increased apoptosis in HEK 293 cells to a similar extent as assessed by flow cytometry. The antioxidant, tempol, significantly reduced dendrimer-mediated apoptosis for both PF and SF. AG-1478 (AG1478), at a 10-fold higher dose (100 μM) than used in signaling studies, is used as a positive control and significantly induced apoptosis in HEK 293 cells[3].

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

体内研究
(In Vivo)

Administration of AG-1478 (AG1478) significantly reduces myocardial inflammation, fibrosis, apoptosis, and dysfunction in both two obese mouse models. ApoE-/- mice are first fed with HFD for 8 weeks (ApoE-HFD), and then administrated with AG-1478 (10 mg/kg/day) or 542 (10 mg/kg/day) for another 8 weeks by oral gavage. AG-1478 or 542 treatment blocks HFD induced cardiac EGFR phosphorylation in vivo, without affecting the plasma level of low density lipoprotein (LDL) and total triglyceride (TG)[2]. Administration of EGF (10 nM) leads to a robust and reproducible elevation in EGFR phosphorylation that can be blocked by AG-1478 (AG1478), a known inhibitor of EGFR phosphorylation. Increasing doses of Polyfect (PF) result in a significant reduction in EGF-induced EGFR phosphorylation (p<0.05) but this is to a lesser extent than observed with AG1478[3].

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

分子量

352.22

Formula

C16H15Cl2N3O2

CAS 号

170449-18-0

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]. Bojko A, et al. The effect of tyrphostins AG494 and AG1478 on the autocrine growth regulation of A549 and DU145 cells. Folia Histochem Cytobiol. 2012 Jul 5;50(2):186-95.

    [2]. Li W, et al. EGFR Inhibition Blocks Palmitic Acid-induced inflammation in cardiomyocytes and Prevents Hyperlipidemia-induced Cardiac Injury in Mice. Sci Rep. 2016 Apr 18;6:24580.

    [3]. Akhtar S, et al. Cationic Polyamidoamine Dendrimers as Modulators of EGFR Signaling In Vitro and In Vivo. PLoS One. 2015 Jul 13;10(7):e0132215.

    [4]. Dorobantu CM, et al. Tyrphostin AG1478 Inhibits Encephalomyocarditis Virus and Hepatitis C Virus by Targeting Phosphatidylinositol 4-Kinase IIIα. Antimicrob Agents Chemother. 2016 Sep 23;60(10):6402-6.

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

AG-1478 hydrochloride(Synonyms: Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride)

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。

AG-1478 hydrochloride (Synonyms: Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride)

AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) 是一种选择性的 EGFR 酪氨酸激酶抑制剂,IC50 为 3 nM。AG-1478 hydrochloride 对 HCV 和脑心肌炎病毒 (EMCV) 具有抗病毒作用。

AG-1478 hydrochloride(Synonyms: Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride)

AG-1478 hydrochloride Chemical Structure

CAS No. : 170449-18-0

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

* Please select Quantity before adding items.

AG-1478 hydrochloride 的其他形式现货产品:

AG-1478

生物活性

AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV)[1][2][3][4].

IC50 & Target

EGFR

3 nM (IC50)

HCV

 

EMCV

 

体外研究
(In Vitro)

AG-1478 (AG1478) is irreversible for growth regulation of human lung (A549) and prostate (DU145) cancer cell lines, cultured in chemically defined DMEM/F12 medium. AG-1478 seems to be more effective at lower concentrations, but is unable to completely inhibit growth of A549 cells[1]. Inhibition of EGFR by specific tyrosine kinase inhibitor AG-1478 (AG1478) significantly decreases the angiotensin II-mediated synthesis of TGF-β and fibronectin by cardiac fibroblasts. EGFR is pharmacologically inhibited by small-molecule inhibitor AG-1478 with IC50 of 4 nM[2]. Both Polyfect (PF) and Superfect (SF) treatment lead to increased apoptosis in HEK 293 cells to a similar extent as assessed by flow cytometry. The antioxidant, tempol, significantly reduced dendrimer-mediated apoptosis for both PF and SF. AG-1478 (AG1478), at a 10-fold higher dose (100 μM) than used in signaling studies, is used as a positive control and significantly induced apoptosis in HEK 293 cells[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.

体内研究
(In Vivo)

Administration of AG-1478 (AG1478) significantly reduces myocardial inflammation, fibrosis, apoptosis, and dysfunction in both two obese mouse models. ApoE-/- mice are first fed with HFD for 8 weeks (ApoE-HFD), and then administrated with AG-1478 (10 mg/kg/day) or 542 (10 mg/kg/day) for another 8 weeks by oral gavage. AG-1478 or 542 treatment blocks HFD induced cardiac EGFR phosphorylation in vivo, without affecting the plasma level of low density lipoprotein (LDL) and total triglyceride (TG)[2]. Administration of EGF (10 nM) leads to a robust and reproducible elevation in EGFR phosphorylation that can be blocked by AG-1478 (AG1478), a known inhibitor of EGFR phosphorylation. Increasing doses of Polyfect (PF) result in a significant reduction in EGF-induced EGFR phosphorylation (p<0.05) but this is to a lesser extent than observed with AG1478[3].

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

分子量

352.22

Formula

C16H15Cl2N3O2

CAS 号

170449-18-0

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]. Bojko A, et al. The effect of tyrphostins AG494 and AG1478 on the autocrine growth regulation of A549 and DU145 cells. Folia Histochem Cytobiol. 2012 Jul 5;50(2):186-95.

    [2]. Li W, et al. EGFR Inhibition Blocks Palmitic Acid-induced inflammation in cardiomyocytes and Prevents Hyperlipidemia-induced Cardiac Injury in Mice. Sci Rep. 2016 Apr 18;6:24580.

    [3]. Akhtar S, et al. Cationic Polyamidoamine Dendrimers as Modulators of EGFR Signaling In Vitro and In Vivo. PLoS One. 2015 Jul 13;10(7):e0132215.

    [4]. Dorobantu CM, et al. Tyrphostin AG1478 Inhibits Encephalomyocarditis Virus and Hepatitis C Virus by Targeting Phosphatidylinositol 4-Kinase IIIα. Antimicrob Agents Chemother. 2016 Sep 23;60(10):6402-6.

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

AG-1478 hydrochloride(Synonyms: Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride)

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。

AG-1478 hydrochloride (Synonyms: Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride)

AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) 是一种选择性的 EGFR 酪氨酸激酶抑制剂,IC50 为 3 nM。AG-1478 hydrochloride 对 HCV 和脑心肌炎病毒 (EMCV) 具有抗病毒作用。

AG-1478 hydrochloride(Synonyms: Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride)

AG-1478 hydrochloride Chemical Structure

CAS No. : 170449-18-0

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

* Please select Quantity before adding items.

AG-1478 hydrochloride 的其他形式现货产品:

AG-1478

生物活性

AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV)[1][2][3][4].

IC50 & Target

EGFR

3 nM (IC50)

HCV

 

EMCV

 

体外研究
(In Vitro)

AG-1478 (AG1478) is irreversible for growth regulation of human lung (A549) and prostate (DU145) cancer cell lines, cultured in chemically defined DMEM/F12 medium. AG-1478 seems to be more effective at lower concentrations, but is unable to completely inhibit growth of A549 cells[1]. Inhibition of EGFR by specific tyrosine kinase inhibitor AG-1478 (AG1478) significantly decreases the angiotensin II-mediated synthesis of TGF-β and fibronectin by cardiac fibroblasts. EGFR is pharmacologically inhibited by small-molecule inhibitor AG-1478 with IC50 of 4 nM[2]. Both Polyfect (PF) and Superfect (SF) treatment lead to increased apoptosis in HEK 293 cells to a similar extent as assessed by flow cytometry. The antioxidant, tempol, significantly reduced dendrimer-mediated apoptosis for both PF and SF. AG-1478 (AG1478), at a 10-fold higher dose (100 μM) than used in signaling studies, is used as a positive control and significantly induced apoptosis in HEK 293 cells[3].

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

体内研究
(In Vivo)

Administration of AG-1478 (AG1478) significantly reduces myocardial inflammation, fibrosis, apoptosis, and dysfunction in both two obese mouse models. ApoE-/- mice are first fed with HFD for 8 weeks (ApoE-HFD), and then administrated with AG-1478 (10 mg/kg/day) or 542 (10 mg/kg/day) for another 8 weeks by oral gavage. AG-1478 or 542 treatment blocks HFD induced cardiac EGFR phosphorylation in vivo, without affecting the plasma level of low density lipoprotein (LDL) and total triglyceride (TG)[2]. Administration of EGF (10 nM) leads to a robust and reproducible elevation in EGFR phosphorylation that can be blocked by AG-1478 (AG1478), a known inhibitor of EGFR phosphorylation. Increasing doses of Polyfect (PF) result in a significant reduction in EGF-induced EGFR phosphorylation (p<0.05) but this is to a lesser extent than observed with AG1478[3].

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

分子量

352.22

Formula

C16H15Cl2N3O2

CAS 号

170449-18-0

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]. Bojko A, et al. The effect of tyrphostins AG494 and AG1478 on the autocrine growth regulation of A549 and DU145 cells. Folia Histochem Cytobiol. 2012 Jul 5;50(2):186-95.

    [2]. Li W, et al. EGFR Inhibition Blocks Palmitic Acid-induced inflammation in cardiomyocytes and Prevents Hyperlipidemia-induced Cardiac Injury in Mice. Sci Rep. 2016 Apr 18;6:24580.

    [3]. Akhtar S, et al. Cationic Polyamidoamine Dendrimers as Modulators of EGFR Signaling In Vitro and In Vivo. PLoS One. 2015 Jul 13;10(7):e0132215.

    [4]. Dorobantu CM, et al. Tyrphostin AG1478 Inhibits Encephalomyocarditis Virus and Hepatitis C Virus by Targeting Phosphatidylinositol 4-Kinase IIIα. Antimicrob Agents Chemother. 2016 Sep 23;60(10):6402-6.

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

AG957(Synonyms: Tyrphostin AG957; NSC 654705)

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。

AG957 (Synonyms: Tyrphostin AG957; NSC 654705)

AG957 (Tyrphostin AG957;NSC 654705) 是一种酪氨酸激酶抑制剂,具有抗 BCR/ABL 酪氨酸激酶活性。AG957抑制 p210bcr/abl 酶活性,IC50 为 2.9 μM。

AG957(Synonyms: Tyrphostin AG957;  NSC 654705)

AG957 Chemical Structure

CAS No. : 140674-76-6

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

* Please select Quantity before adding items.

生物活性

AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity[1][2]. AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210bcr/abl autokinase activity[3].

体外研究
(In Vitro)

AG957 inhibit p210bcr-abl tyrosine kinase activity. AG957 inhibits DNA synthesis as early as 2 h (60% inhibition at 20 microM). AG957 inhibits p210bcr-abl tyrosine phosphorylation in living cells by 1 h without an inhibition of total protein phosphorylation[1]. Tyrphostin AG957, a protein tyrosine kinase (PTK) inhibitor which has activity against the p210BCR/ABL kinase, on beta1 integrin function in CML progenitors[2].
AG957 (0.1-100 μM ) pretreatment results in significant inhibition of proliferation of chronic myelogenous leukemia (CML) colony-forming cells (CFC) CML CFC[2].
AG957 (25 μM) partially inhibits phosphorylation of several proteins that are BCR/ABL PTK substrates and are involved in normal integrin signaling in BCR/ABL expressing cells[2].

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

Cell Proliferation Assay[2]

Cell Line: CML and CFC
Concentration: 0, 0.1, 1, 10, 100 μM
Incubation Time: Pretreatment for 1 hour
Result: A significant dose-dependent inhibition of CML CFC growth was seen following preincubation with AG957.

Western Blot Analysis[2]

Cell Line: K562 and BCR/ABL-tranfected M07e cells (MBA-4)
Concentration: 25 μM
Incubation Time: 24 hours
Result: Partially inhibited tyrosine phosphorylation of p210BCR/ABL, the focal adhesion protein paxillin, the p85 regulatory subunit of the PI3K and the adapter protein cbl in K562 cells.
Inhibited phosphorylation of these proteins as well as the adapter protein crkl in MBA4 cells.

体内研究
(In Vivo)

AG957 (10 mg/kg; intratracheally 1 h before intratracheal LPS challenge) blocks c-Abl activity in the lung of mice[4].

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

Animal Model: C57BL/6J mice[4]
Dosage: 10 mg/kg
Administration: Intratracheally 1 h before intratracheal LPS challenge
Result: LPS induced significant phosphorylation of paxillin at Y31 and Y118. Inhibition of c-Abl by AG957 attenuated LPS-induced phosphorylation of paxillin at both sites.
LPS induced significant phosphorylation of VE-cadherin in DMSO-treated mice, which was attenuated in AG957-treated mice.

分子量

273.28

Formula

C15H15NO4

CAS 号

140674-76-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. G Kaur, et al. Tyrphostin induced growth inhibition: correlation with effect on p210bcr-abl autokinase activity in K562 chronic myelogenous leukemia. Anticancer Drugs. 1994 Apr;5(2):213-22.

    [2]. R Bhatia, et al. Tyrphostin AG957, a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity restores beta1 integrin-mediated adhesion and inhibitory signaling in chronic myelogenous leukemia hematopoietic progenitors. Leukemia. 1998 Nov;12(11):1708-17.

    [3]. P A Svingen, et al. Effects of the bcr/abl kinase inhibitors AG957 and NSC 680410 on chronic myelogenous leukemia cells in vitro. Clin Cancer Res. 2000 Jan;6(1):237-49.

    [4]. Panfeng Fu, et al. c-Abl mediated tyrosine phosphorylation of paxillin regulates LPS-induced endothelial dysfunction and lung injury. Am J Physiol Lung Cell Mol Physiol. 2015 May 15;308(10):L1025-38.

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

AG957(Synonyms: Tyrphostin AG957; NSC 654705)

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。

AG957 (Synonyms: Tyrphostin AG957; NSC 654705)

AG957 (Tyrphostin AG957;NSC 654705) 是一种酪氨酸激酶抑制剂,具有抗 BCR/ABL 酪氨酸激酶活性。AG957抑制 p210bcr/abl 酶活性,IC50 为 2.9 μM。

AG957(Synonyms: Tyrphostin AG957;  NSC 654705)

AG957 Chemical Structure

CAS No. : 140674-76-6

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

* Please select Quantity before adding items.

生物活性

AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity[1][2]. AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210bcr/abl autokinase activity[3].

体外研究
(In Vitro)

AG957 inhibit p210bcr-abl tyrosine kinase activity. AG957 inhibits DNA synthesis as early as 2 h (60% inhibition at 20 microM). AG957 inhibits p210bcr-abl tyrosine phosphorylation in living cells by 1 h without an inhibition of total protein phosphorylation[1]. Tyrphostin AG957, a protein tyrosine kinase (PTK) inhibitor which has activity against the p210BCR/ABL kinase, on beta1 integrin function in CML progenitors[2].
AG957 (0.1-100 μM ) pretreatment results in significant inhibition of proliferation of chronic myelogenous leukemia (CML) colony-forming cells (CFC) CML CFC[2].
AG957 (25 μM) partially inhibits phosphorylation of several proteins that are BCR/ABL PTK substrates and are involved in normal integrin signaling in BCR/ABL expressing cells[2].

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

Cell Proliferation Assay[2]

Cell Line: CML and CFC
Concentration: 0, 0.1, 1, 10, 100 μM
Incubation Time: Pretreatment for 1 hour
Result: A significant dose-dependent inhibition of CML CFC growth was seen following preincubation with AG957.

Western Blot Analysis[2]

Cell Line: K562 and BCR/ABL-tranfected M07e cells (MBA-4)
Concentration: 25 μM
Incubation Time: 24 hours
Result: Partially inhibited tyrosine phosphorylation of p210BCR/ABL, the focal adhesion protein paxillin, the p85 regulatory subunit of the PI3K and the adapter protein cbl in K562 cells.
Inhibited phosphorylation of these proteins as well as the adapter protein crkl in MBA4 cells.

体内研究
(In Vivo)

AG957 (10 mg/kg; intratracheally 1 h before intratracheal LPS challenge) blocks c-Abl activity in the lung of mice[4].

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

Animal Model: C57BL/6J mice[4]
Dosage: 10 mg/kg
Administration: Intratracheally 1 h before intratracheal LPS challenge
Result: LPS induced significant phosphorylation of paxillin at Y31 and Y118. Inhibition of c-Abl by AG957 attenuated LPS-induced phosphorylation of paxillin at both sites.
LPS induced significant phosphorylation of VE-cadherin in DMSO-treated mice, which was attenuated in AG957-treated mice.

分子量

273.28

Formula

C15H15NO4

CAS 号

140674-76-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. G Kaur, et al. Tyrphostin induced growth inhibition: correlation with effect on p210bcr-abl autokinase activity in K562 chronic myelogenous leukemia. Anticancer Drugs. 1994 Apr;5(2):213-22.

    [2]. R Bhatia, et al. Tyrphostin AG957, a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity restores beta1 integrin-mediated adhesion and inhibitory signaling in chronic myelogenous leukemia hematopoietic progenitors. Leukemia. 1998 Nov;12(11):1708-17.

    [3]. P A Svingen, et al. Effects of the bcr/abl kinase inhibitors AG957 and NSC 680410 on chronic myelogenous leukemia cells in vitro. Clin Cancer Res. 2000 Jan;6(1):237-49.

    [4]. Panfeng Fu, et al. c-Abl mediated tyrosine phosphorylation of paxillin regulates LPS-induced endothelial dysfunction and lung injury. Am J Physiol Lung Cell Mol Physiol. 2015 May 15;308(10):L1025-38.

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AG957(Synonyms: Tyrphostin AG957; NSC 654705)

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。

AG957 (Synonyms: Tyrphostin AG957; NSC 654705)

AG957 (Tyrphostin AG957;NSC 654705) 是一种酪氨酸激酶抑制剂,具有抗 BCR/ABL 酪氨酸激酶活性。AG957抑制 p210bcr/abl 酶活性,IC50 为 2.9 μM。

AG957(Synonyms: Tyrphostin AG957;  NSC 654705)

AG957 Chemical Structure

CAS No. : 140674-76-6

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

* Please select Quantity before adding items.

生物活性

AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity[1][2]. AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210bcr/abl autokinase activity[3].

体外研究
(In Vitro)

AG957 inhibit p210bcr-abl tyrosine kinase activity. AG957 inhibits DNA synthesis as early as 2 h (60% inhibition at 20 microM). AG957 inhibits p210bcr-abl tyrosine phosphorylation in living cells by 1 h without an inhibition of total protein phosphorylation[1]. Tyrphostin AG957, a protein tyrosine kinase (PTK) inhibitor which has activity against the p210BCR/ABL kinase, on beta1 integrin function in CML progenitors[2].
AG957 (0.1-100 μM ) pretreatment results in significant inhibition of proliferation of chronic myelogenous leukemia (CML) colony-forming cells (CFC) CML CFC[2].
AG957 (25 μM) partially inhibits phosphorylation of several proteins that are BCR/ABL PTK substrates and are involved in normal integrin signaling in BCR/ABL expressing cells[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.

Cell Proliferation Assay[2]

Cell Line: CML and CFC
Concentration: 0, 0.1, 1, 10, 100 μM
Incubation Time: Pretreatment for 1 hour
Result: A significant dose-dependent inhibition of CML CFC growth was seen following preincubation with AG957.

Western Blot Analysis[2]

Cell Line: K562 and BCR/ABL-tranfected M07e cells (MBA-4)
Concentration: 25 μM
Incubation Time: 24 hours
Result: Partially inhibited tyrosine phosphorylation of p210BCR/ABL, the focal adhesion protein paxillin, the p85 regulatory subunit of the PI3K and the adapter protein cbl in K562 cells.
Inhibited phosphorylation of these proteins as well as the adapter protein crkl in MBA4 cells.

体内研究
(In Vivo)

AG957 (10 mg/kg; intratracheally 1 h before intratracheal LPS challenge) blocks c-Abl activity in the lung of mice[4].

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: C57BL/6J mice[4]
Dosage: 10 mg/kg
Administration: Intratracheally 1 h before intratracheal LPS challenge
Result: LPS induced significant phosphorylation of paxillin at Y31 and Y118. Inhibition of c-Abl by AG957 attenuated LPS-induced phosphorylation of paxillin at both sites.
LPS induced significant phosphorylation of VE-cadherin in DMSO-treated mice, which was attenuated in AG957-treated mice.

分子量

273.28

Formula

C15H15NO4

CAS 号

140674-76-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. G Kaur, et al. Tyrphostin induced growth inhibition: correlation with effect on p210bcr-abl autokinase activity in K562 chronic myelogenous leukemia. Anticancer Drugs. 1994 Apr;5(2):213-22.

    [2]. R Bhatia, et al. Tyrphostin AG957, a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity restores beta1 integrin-mediated adhesion and inhibitory signaling in chronic myelogenous leukemia hematopoietic progenitors. Leukemia. 1998 Nov;12(11):1708-17.

    [3]. P A Svingen, et al. Effects of the bcr/abl kinase inhibitors AG957 and NSC 680410 on chronic myelogenous leukemia cells in vitro. Clin Cancer Res. 2000 Jan;6(1):237-49.

    [4]. Panfeng Fu, et al. c-Abl mediated tyrosine phosphorylation of paxillin regulates LPS-induced endothelial dysfunction and lung injury. Am J Physiol Lung Cell Mol Physiol. 2015 May 15;308(10):L1025-38.

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

多肽定制pTH (44-68) (human) 编码 [64421-69-8]

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 pTH (44-68) (human)
编码 [64421-69-8]
别名 pTH (44-68) (human)
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) RDAGSQRPRKKEDNVLVESHEKSLG-OH
序列(三字母缩写) Arg-Asp-Ala-Gly-Ser-Gln-Arg-Pro-Arg-Lys-Lys-Glu-Asp-Asn-Val-Leu-Val-Glu-Ser-His-Glu-Lys-Ser-Leu-Gly
基本描述
溶解度
分子量 0
化学式
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents pTH (44-68) (human)          编码     [64421-69-8]
Figures pTH (44-68) (human)          编码     [64421-69-8]
Reference
C端
N端
化学桥

Tyrphostin 25(Synonyms: AG82; Tyrphostin A 25; Tyrphostin AG 82; RG-50875)

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。

Tyrphostin 25 (Synonyms: AG82; Tyrphostin A 25; Tyrphostin AG 82; RG-50875)

Tyrphostin 25 (AG82) 是一种 EGFR 酪氨酸激酶的特异性抑制剂。Tyrphostin 25 也是一种 GPR35 激动剂,IC50 值为 0.94 µM,EC50 值为 5.3 µM。

Tyrphostin 25(Synonyms: AG82;  Tyrphostin A 25;  Tyrphostin AG 82;  RG-50875)

Tyrphostin 25 Chemical Structure

CAS No. : 118409-58-8

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

Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase. Tyrphostin 25 is also a GPR35 agonist with an IC50 of 0.94 µM and an EC50 of 5.3 µM[1][2].

IC50 & Target

EGFR tyrosine kinase[1]
IC50: 0.94 µM (GPR35)[2]
EC50: 5.3 µM (GPR35)[2]

分子量

202.17

Formula

C10H6N2O3

CAS 号

118409-58-8

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]. Klemke RL, et al. Receptor tyrosine kinase signaling required for integrin alpha v beta 5-directed cell motility but not adhesion on vitronectin. J Cell Biol. 1994 Nov;127(3):859-66.

    [2]. Deng H, et al. Tyrphostin analogs are GPR35 agonists. FEBS Lett. 2011 Jun 23;585(12):1957-62.

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