Tyrphostin AG 1296
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In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
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Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Tyrphostin AG 1296是一种血小板生长因子受体(PDGFR)的选择性抑制剂,IC50值为0.3 μM-0.5 μM[1]。
Tyrphostin AG 1296是一种ATP竞争性的PDGFR抑制剂。Tyrphostin AG 1296结合PDGFR可导致ATP结合位点构象变化。在体外实验中,Tyrphostin AG 1296可有效抑制Swiss 3T3细胞膜上配体诱导的PDGF受体自磷酸化。Tyrphostin AG 1296在浓度高达100 μM的情况下仍不影响EGF受体。Tyrphostin AG 1296也可抑制PDGF而非EGF或胰岛素诱导的有丝分裂。Tyrphostin AG 1296可逆地抑制PDGF诱导的DNA合成,平均IC50值为1.5 μM。除此之外,tyrphostin AG 1296可抑制PDGF诱导的细胞生长,在Swiss 3T3细胞中IC50值为3.2 μM[1,2]。
参考文献:
[1] Kovalenko M, Gazit A, Bhmer A, et al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Research, 1994, 54(23): 6106-6114.
[2] Kovalenko M, Rnnstrand L, Heldin C H, et al. Phosphorylation site-specific inhibition of platelet-derived growth factor β-receptor autophosphorylation by the receptor blocking tyrphostin AG1296. Biochemistry, 1997, 36(21): 6260-6269.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 266.29 |
Cas No. | 146535-11-7 |
Formula | C16H14N2O2 |
Solubility | insoluble in H2O; ≥2.8 mg/mL in EtOH with ultrasonic; ≥6.65 mg/mL in DMSO |
Chemical Name | 6,7-dimethoxy-2-phenylquinoxaline |
SDF | Download SDF |
Canonical SMILES | COC1=C(C=C2C(=C1)N=CC(=N2)C3=CC=CC=C3)OC |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
Swiss 3T3细胞,猪主动脉内皮细胞,sis转化细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于6.7 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
6-8 h |
应用 |
AG1296(0.1-5 μM)以剂量依赖性方式抑制Swiss 3T3细胞膜中PDGF受体激酶的活性。AG1296抑制PDGF受体自磷酸化,IC50为0.3-0.5 μM。AG1296强烈抑制PDGF诱导的有丝分裂发生。在Swiss 3T3细胞中,AG1296抑制基础FGF的促有丝分裂作用,IC50为12.3 ± 3.1 μM。AG1296有效抑制PDGF诱导的细胞生长,IC50为3.2 μM。在猪主动脉内皮细胞中,AG1296抑制人PDGFα-和PDGFβ-受体的自磷酸化,并且在受体转染的细胞中抑制PDGFα和PDGFβ受体依赖性的DNA合成。AG1296(5-50 μM)有效抑制sis转化的NIH 3T3细胞的生长。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Kovalenko M, Gazit A, Bhmer A, et al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation[J]. Cancer Research, 1994, 54(23): 6106-6114. |
Description | Tyrphostin AG 1296是一种血小板生长因子受体(PDGFR)的选择性抑制剂,IC50值为0.3 μM-0.5 μM。 | |||||
靶点 | PDGFR | |||||
IC50 | 0.3 μM-0.5 μM |
质量控制和MSDS
- 批次:
相关生物数据
![Tyrphostin AG 1296 Tyrphostin AG 1296](http://www.apexbt.com/media/diy/images/wb/A2477_1.jpg)
相关生物数据
![Tyrphostin AG 1296 Tyrphostin AG 1296](https://www.apexbt.com/media/diy/images/wb/A2477_2.jpg)