Tyrphostin AG 1296

Catalog No.S8024 Batch:S802401

Print

Technical Data

Formula

C16H14N2O2
Molecular Weight 266.29 CAS No. 146535-11-7
Solubility (25°C)* In vitro DMSO 6 mg/mL (22.53 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells.
Targets
PDGFR [1] c-Kit (Swiss 3T3) [1] FGFR (Swiss 3T3) [1]
0.3 μM-0.5 μM 1.8 μM 12.3 μM
In vitro AG 1296 inhibits selectively the PDGF receptor kinase and the PDGF dependent DNA synthesis in Swiss 3T3 cells and in porcine aorta endothellal cells with 50% inhibitory concentrations below 5 and 1μM, respectively. AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. AG1296 potently inhibits signaling of human PDGF -α and -β receptors but has no effect on autophosphorylation of the VEGFR KDR or on DNA synthesis induced by VEGF in porcine aortlc endothelial cells. Treatment by AG1296 reverses the transformed phenotype of sis-transfected NIH 3T3 cells but has no effect on src-transformed NIH3T3 cells. [1] AG1296 is an ATP-competitive inhibitor. AG1296 interferes neither with PDGF binding nor with PDGF receptor dimerization while it abolishes PDGF receptor autophosphorylation. Thus, AG1296 is a pure inhibitor of the catalytic activity of the receptor tyrosine kinase. [2]

Protocol (from reference)

Kinase Assay:[1]
  • Membrane Autophosphorylation Assays

    Membranes are prepared from confluent cultures of Swiss 3T3 cells as described. For measuring receptor autophosphorylation, 10μg membrane protein per assay are incubated for 20 min on ice in the presence of 1.2μg/mL EGF or 2μg/mL PDGF, or both; 50 mM Hepes (pH 7.5); and 3 mM MnCl2 in a volume of 45μl. In order to test the effects of tyrphostins, these are added in a volume of 0.5 μl (in DMSO; final concentration, 0.5%) 15 min before addition of the growth factors. Phosphorylation is initiated by addition of [γ-32P]ATP and terminated after 2 min by addition of 10μL of a solution containing 6% SDS, 30%β-mercatoethanol, 40% glycerol, and 0.5 mg/mL bromophenol blue. The samples are heated for 5 min at 95 ℃ and subjected to SDS-PAGE using 10% acrylamide gels. The gels are stained and dried and subjected to autoradiographic analysis.
Cell Assay:[1]
  • Cell lines

    Swiss 3T3

  • Concentrations

    ~50 μM

  • Incubation Time

    3 days

  • Method

    Cells are seeded in 24-well plates (5000 cells/well) in DMEM/10% FCS. On the next day the medium is changed to DMEM/2% FcS with or without growth factors and tyrphostins are added as indicated. Three days later the cells are counted in a hemocytometer

Customer Product Validation

Data from [Onco Targets Ther, 2014, 7, 425-32]

Selleck's Tyrphostin AG 1296 has been cited by 14 publications

PDGF signaling inhibits mitophagy in glioblastoma stem cells through N6-methyladenosine [ Dev Cell, 2022, 57(12):1466-1481.e6] PubMed: 35659339
PIM1 is a Poor Prognostic Factor for and Potential Therapeutic Target in Serous Carcinoma of the Endometrium [ Front Pharmacol, 2021, 12:804327] PubMed: 35069215
Inhibition of PDGF-BB reduces alkali-induced corneal neovascularization in mice [ Mol Med Rep, 2021, 23(4):1] PubMed: 33537811
PDGFRα: Expression and Function during Mitral Valve Morphogenesis [ J Cardiovasc Dev Dis, 2021, 8(3)28] PubMed: 33805717
Small-molecule inhibitor - tyrphostin AG1296 regulates proliferation, survival and migration of rhabdomyosarcoma cells [ J Physiol Pharmacol, 2021, 72(6)] PubMed: 35377340
PDGF Signaling Promotes Mitophagy in Glioblastoma Stem Cells Through N 6-Methyladenosine [ CellPress, 2021, None] PubMed: None
Low-Dose Sorafenib Acts as a Mitochondrial Uncoupler and Ameliorates Nonalcoholic Steatohepatitis. [ Cell Metab, 2020, 5;31(5):892-908 e11] PubMed: 32375062
Discovering the anti-cancer potential of non-oncology drugs by systematic viability profiling [ Nat Cancer, 2020, 1(2):235-248] PubMed: 32613204
A Pygopus 2-histone interaction is critical for cancer cell de-differentiation and progression in malignant breast cancer [ Cancer Res, 2020, canres.2910.2019] PubMed: 32586983
Blocking fibrotic signaling in fibroblasts from patients with carpal tunnel syndrome. [ J Cell Physiol, 2018, 233(3):2067-2074] PubMed: 28294324

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.