Description
SU16f is a potent and selective PDGFRβ inhibitor with IC50s of 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively. Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs (gastric cancer-derived mesenchymal stem cells) conditioned medium in gastric cancer cell proliferation and migration.
Product information
CAS Number: 251356-45-3
Molecular Weight: 386.44
Formula: C24H22N2O3
Chemical Name: 3-(2,4-dimethyl-5-{[(3Z)-2-oxo-6-phenyl-2,3-dihydro-1H-indol-3-ylidene]methyl}-1H-pyrrol-3-yl)propanoic acid
Smiles: CC1=C(/C=C2/C3C=CC(=CC=3NC/2=O)C2C=CC=CC=2)NC(C)=C1CCC(O)=O
InChiKey: APYYTEJNOZQZNA-MOSHPQCFSA-N
InChi: InChI=1S/C24H22N2O3/c1-14-18(10-11-23(27)28)15(2)25-21(14)13-20-19-9-8-17(12-22(19)26-24(20)29)16-6-4-3-5-7-16/h3-9,12-13,25H,10-11H2,1-2H3,(H,26,29)(H,27,28)/b20-13-
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
SU16f (20 μM; for 8 hours) pretreatment inhibits the promoting role of GC-MSC-CM in SGC-7901 cell proliferation. SU16f (20 μM; for 8 hours) significantly abolishes PDGFRβ activation in SGC-7901 by GC-MSC-CM. SU16f pretreatment results in the upregulation of E-cadherin and downregulation of N-cadherin, Vimentin, and α-SMA. SU16f pretreatment leads to downregulation of p-AKT, Bcl-xl, and Bcl-2 levels and upregulation of Bax expression in SGC-7901 cells by GC-MSC-CM .
References:
- Sun L, et al. Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases. J Med Chem. 1999 Dec 16;42(25):5120-30.
- Huang F, et al. Gastric cancer-derived MSC-secreted PDGF-DD promotes gastric cancer progression. J Cancer Res Clin Oncol. 2014 Nov;140(11):1835-48.
Products are for research use only. Not for human use.
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