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AG-370 (Synonyms: NSC 651712)

Katalog-Nr.GC11712

AG-370, ein Indol-Tyrphostin, ist ein potenter PDGF-induzierter Mitogenese-Inhibitor (IC50 von 20 μM).

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AG-370 Chemische Struktur

Cas No.: 134036-53-6

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5mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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).

Chemical Properties

Cas No. 134036-53-6 SDF
Überlieferungen NSC 651712
Chemical Name 3-amino-4-(1H-indol-5-ylmethylene)-2-pentenetricarbonitrile
Canonical SMILES c12c(ccc(c1)/C=C(\C(=C(\C#N)C#N)N)C#N)[nH]cc2
Formula C15H9N5 M.Wt 259.3
Löslichkeit ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.8565 mL 19.2827 mL 38.5654 mL
5 mM 0.7713 mL 3.8565 mL 7.7131 mL
10 mM 0.3857 mL 1.9283 mL 3.8565 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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