Tyrphostin AG1296

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].

Product Specifications

CAS Number

[146535-11-7]

Product Name Alternative

AG1296

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; c-Kit; FLT3; PDGFR

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/tyrphostin-ag1296.html

Concentration

10mM

Purity

99.69

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

Smiles

COC1=C(OC)C=C2N=CC(C3=CC=CC=C3)=NC2=C1

Molecular Formula

C16H14N2O2

Molecular Weight

266.29

Precautions

H302, H315, H319, H335

References & Citations

[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.