AG-370
Catalogue Number: C4539-APE
| Manufacturer: | Apexbio |
| Molecular Formula: | C15H9N5 |
| Physical state: | A crystalline solid |
| Type: | Kinase Inhibitors |
| Alias: | NSC 651712 |
| Shipping Condition: | Blue Ice |
| Unit(s): | 1 mg, 10 mg, 25 mg, 5 mg |
Description
Description: IC50: 20 µM for PDGF receptor kinase in human bone marrow fibroblastsAG-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).
Additional Text
Storage Note
Store at -20°C
Solubility
≤30mg/ml in DMSO;30mg/ml in dimethyl formamide
Smile String
c12c(ccc(c1)/C=C(C(=C(C#N)C#N)N)C#N)[nH]cc2
C4539 CofA
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