[CAS NO. 848318-25-2] SSR128129E
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PRODUCTS SPECIFICATIONS [848318-25-2]
Catalog
SLK-S7167
Brand
Selleck
CAS
848318-25-2
DESCRIPTION [848318-25-2]
Overview
| MDL | MFCD25976751 |
|---|---|
| Molecular Weight | 346.31 |
| Molecular Formula | C18H15N2O4.Na |
| SMILES | O=C([O-])C1=CC(C(C2=C(C)C(OC)=C3C=CC=CN23)=O)=CC=C1N.[Na+] |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8876 mL | 14.4379 mL | 28.8759 mL |
| 5 mM | 0.5775 mL | 2.8876 mL | 5.7752 mL |
| 10 mM | 0.2888 mL | 1.4438 mL | 2.8876 mL |
| 50 mM | 0.0578 mL | 0.2888 mL | 0.5775 mL |
Description
SSR128129E is an orally-active and allosteric inhibitor with of 1.9 μM, while not affecting other related RTKs.
Targets
| FGFR1 [1] |
| 1.9 μM |
In vitro
SSR128129E exhibits more effective activity in cell assay due to its allosteric mechanism. SSR128129E dose-dependently inhibits FGF2-induced EC proliferation and migration with IC50 of 31 nM and 15.2 nM, respectively. As a multi-FGFR inhibitor, SSR128129E inhibits responses mediated by FGFR1-4 and thus results in the blockage of proliferation and/or migration in various cell lines including mPanc02, HEK-hFGFR2WT, PAE-hFGFR1, hB9-myeloma and HUVEC.
In vivo
In Arthritis mice, SSR128129E (30 mg/kg, p.o.) inhibits angiogenesis, inflammation, and bone resorption, and reduces the severity of clinical symptoms. In mice bearing various tumor models, SSR128129E (30 mg/kg, p.o.) inhibits both the growth of primary tumors and metastasis. In addition, SSR128129E inhibits growth of anti-VEGFR2-refractory and -sensitive tumor models, and enhances the antitumor activity of anti-VEGFR2. SSR128129E also inhibits arteriosclerosis in a mouse vein graft model and atherosclerosis in apolipoprotein E-deficient mice.
References
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