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Tyrphostin AG 1296

Cat. No. M3097
Tyrphostin AG 1296 Structure
Synonym:

AG 1296

Size Price Availability Quantity
5mg USD 95  USD95 In stock
10mg USD 150  USD150 In stock
25mg USD 285  USD285 In stock
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Quality Control & Documentation
Biological Activity

Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.

Customer Product Validations & Biological Datas
Source Oncol Lett (2015). Figure 2. Tyrphostin AG 1296
Method cell invasion assay
Cell Lines U87MG cells
Concentrations 12.5, 50 or 200 nM
Incubation Time 8 h
Results Statistical analysis demonstrated that the anti.migration effect of tyrphostin AG 1296 in U87MG cells, increased in a dose.dependent manner
Protocol (for reference only)
Cell Experiment
Cell lines Swiss 3T3
Preparation method Seeding cells in 24-well plates (5000 cells/well) in DMEM/10% FCS. A day later, the medium is changed to DMEM/2% FcS with or without growth factors and tyrphostins are added as indicated. Three days later count the cells in a hemocytometer
Concentrations ~50 μM
Incubation time 3 days
Animal Experiment
Animal models
Formulation
Dosages
Administration
Chemical Information
Molecular Weight 266.29
Formula C16H14N2O2
CAS Number 146535-11-7
Solubility (25°C) DMSO 6 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Mingxia Gu, et al. iPSC-endothelial cell phenotypic drug screening and in silico analyses identify tyrphostin-AG1296 for pulmonary arterial hypertension

[2] Min Wang, et al. Platelet-derived growth factor B attenuates lethal sepsis through inhibition of inflammatory responses

[3] Hongwei Li, et al. Tyrphostin AG 1296 induces glioblastoma cell apoptosis in vitro and in vivo

[4] Gabriel M Gordon, et al. A cell-based screening assay to identify pharmaceutical compounds that enhance the regenerative quality of corneal repair

[5] Huan-Yong Che, et al. Additive effect by combination of Akt inhibitor, MK-2206, and PDGFR inhibitor, tyrphostin AG 1296, in suppressing anaplastic thyroid carcinoma cell viability and motility

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Keywords: Tyrphostin AG 1296, AG 1296 supplier, VEGFR/PDGFR, inhibitors, activators


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