| BMS-817378Potent ATP competitive inhibitor of Met/VEGFR2 |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 1174161-69-3 | SDF | Download SDF |
| Chemical Name | (Z)-N-(4-((3-chloro-2-imino-1,2-dihydropyridin-4-yl)oxy)-3-fluorophenyl)-5-(4-fluorophenyl)-4-oxo-1-((phosphonooxy)methyl)-1,4-dihydropyridine-3-carbimidic acid | ||
| Canonical SMILES | ClC1=C(OC2=C(F)C=C(/N=C(O)/C3=CN(COP(O)(O)=O)C=C(C3=O)C4=CC=C(F)C=C4)C=C2)C=CNC1=N | ||
| Formula | C24H18ClF2N4O7P | M.Wt | 578.85 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Description:
IC50: 1.7 nM/15 nM for Met/VEGFR2
The signaling pathway of the receptor tyrosine kinase MET and its ligand hepatocyte growth factor is important for cell growth, survival, and motility and is functionally linked to the signaling pathway of VEGF, which is widely recognized as a key effector in angiogenesis and cancer progression. BMS-817378 is a potent ATP competitive inhibitor of Met/VEGFR2.
In vitro: BMS-794833, which is the active moiety of BMS-817378, is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nm.="" bms-794833="" also="" inhibits="" met="" receptor="" activated="" gastric="" carcinoma="" cell="" line,="" gtl-16,="" with="" ic50="" of="" 39="" nm="">
In vivo: BMS-798433 shows greater than 50% TGI for at least one tumor doubling time with no toxicity observed during 14 days in GTL-16 human gastric tumor xenografts model. BMS-798433 also shows complete tumor stasis at 25 mg/kg against U87 glioblastoma model [1].
Clinical trial: BMS-817378 is now in its ascending multiple-dose study in subjects with advanced cancers.
Reference:[1]http://worldwide.espacenet.com/publicationDetails/biblio?DB=EPODOC&II=0&adjacent=true&locale=en_EP&FT=D&date=20090730&CC=WO&NR=2009094417A1&KC=A1
