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Tyrphostin AG1433 168835-90-3

Tyrphostin AG1433 168835-90-3

CAS No.: 168835-90-3

Tyrphostin AG1433 (SU1433) is a tyrosine kinase inhibitor (TKI). Tyrphostin AG1433 is also a selective inhibitor of PDGF
Data collection:peptidedb@qq.com

This product is for research use only, not for human use. We do not sell to patients.

Tyrphostin AG1433 (SU1433) is a tyrosine kinase inhibitor (TKI). Tyrphostin AG1433 is also a selective inhibitor of PDGFRβ and VEGFR-2 (Flk-1/KDR) with IC50 of 5.0 μM and 9.3 μM respectively. Tyrphostin AG1433 prevents blood vessel formation.

Physicochemical Properties


Molecular Formula C16H14N2O2
Molecular Weight 266.29456
Exact Mass 266.105
CAS # 168835-90-3
PubChem CID 2050
Appearance Light yellow to khaki solid powder
LogP 2.9
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 4
Rotatable Bond Count 1
Heavy Atom Count 20
Complexity 338
Defined Atom Stereocenter Count 0
SMILES

CC1=CC2=NC=C(N=C2C=C1C)C3=CC(=C(C=C3)O)O

InChi Key SMKFYHOKXJUJOT-UHFFFAOYSA-N
InChi Code

InChI=1S/C16H14N2O2/c1-9-5-12-13(6-10(9)2)18-14(8-17-12)11-3-4-15(19)16(20)7-11/h3-8,19-20H,1-2H3
Chemical Name

4-(6,7-dimethylquinoxalin-2-yl)benzene-1,2-diol
Synonyms

Tyrphostin AG1433; Tyrphostin AG-1433
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vitro Treatment of glioblastoma cells with tyrophostin AG1433 (0.1-100 μM; 72 hours; GB8B cells) causes moderate cytotoxicity [1].
ln Vivo Angiogenesis was examined using the Chorioallantoic membrane (CAM) assay to evaluate the impact of Flk-i inhibitors. Tyrphostin AG1433 (SU1433) is suited for CAM in chicken embryos that are 4-6 days old and is made from methylcellulose particles. Under the particles, tyrosine phosphatase AG1433 inhibits the growth of new fish algae [2].
Cell Assay Cell viability assay [1]
Cell Types: GB8B Cell
Tested Concentrations: 0.1 μM, 1 μM, 5 μM, 10 μM, 20 μM, 30 μM, 50 μM, 60 μM, 100 μM
Incubation Duration: 72 hrs (hours)
Experimental Results: Significant induction Cell death occurred in a concentration-dependent manner in GB8B cells.
References

[1]. Silencing of epidermal growth factor, latrophilin and seven transmembrane domain-containing protein 1 (ELTD1) via siRNA-induced cell death in glioblastoma. J Immunoassay Immunochem. 2017;38(1):21-33.

[2]. Flk-1 as a target for tumor growth inhibition. Cancer Res. 1996 Aug 1;56(15):3540-5.

[3]. The ZFHX3 (ATBF1) transcription factor induces PDGFRB, which activates ATM in the cytoplasm to protect cerebellar neurons from oxidative stress. Dis Model Mech. 2010 Nov-Dec;3(11-12):752-62.

[4]. The vascular endothelial growth factor receptor KDR activates multiple signal transduction pathways in porcine aortic endothelial cells. J Biol Chem. 1997 Dec 19;272(51):32521-7.

Additional Infomation Tyrphostin AG 1433 is a member of the Tyrphostin family of tyrosine kinase inhibitors that selectively inhibits platelet-derived growth factor beta-receptor kinase and angiogenesis. (NCI)

Solubility Data


Solubility (In Vitro) DMSO : ~62.5 mg/mL (~234.71 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.08 mg/mL (7.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.7553 mL 18.7765 mL 37.5530 mL
5 mM 0.7511 mL 3.7553 mL 7.5106 mL
10 mM 0.3755 mL 1.8777 mL 3.7553 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.