AG-370
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 20 μM for PDGF receptor kinase in human bone marrow fibroblasts
AG-370 is a tyrphostin PDGFR inhibitor.
Protein tyrosine kinase inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of protein tyrosine kinases. Tyrphostins are a class of antiproliferative agents selectively inhibiting protein tyrosine kinases of key growth factors including epidermal growth factor or platelet-derived growth factor (PDGF) via blocking the phosphorylation of tyrosine residues.
In vitro: Previous study found that AG-370 inhibited PDGF receptor autophosphorylation and the tyrosine phosphorylation of intracellular protein substrates that coprecipitated with the PDGF receptor in digitonin-permeabilized fibroblasts and in intact fibroblasts. When compared with AG18, a potent EGF receptor blocker, AG370 was more efficient in inhibiting PDGF-induced proliferation of fibroblasts and phosphorylation of the intracellular protein substrates. Under the conditions in which AG370 could inhibit PDGF-induced mitogenesis and phosphorylation, AG18 did not alter [125I]PDGF internalization and enhance [125I]PDGF binding. These findings suggested that AG370 might have a therapeutic potential for treatment of diseases involving abnormal cellular proliferation induced by PDGF [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Bryckaert, M. C.,Eldor, A.,Fontenay, M., et al. Inhibition of platelet-derived growth factor-induced mitogenesis and tyrosine kinase activity in cultured bone marrow fibroblasts by tyrphostins. Experimental Cell Research 199, 255-261 (1992).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 259.3 |
Cas No. | 134036-53-6 |
Formula | C15H9N5 |
Synonyms | NSC 651712 |
Solubility | ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide |
Chemical Name | 3-amino-4-(1H-indol-5-ylmethylene)-2-pentenetricarbonitrile |
SDF | Download SDF |
Canonical SMILES | c12c(ccc(c1)/C=C(\C(=C(\C#N)C#N)N)C#N)[nH]cc2 |
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。 |
质量控制和MSDS
- 批次:
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纯度 ≥ 95.00% (cis/trans mixture)
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)