Research Area
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United States ( Change Country )
BMS 794833 Chemical Structure
Linifanib (ABT-869)
Linifanib (ABT869) is a structurally novel, potent RTK and VEGF and PDGF receptor families inhibitor for, PDGFR-β, KDR, and CSF-1R, with IC50 of 0.2 nM, 2 nM, 4 nM, and 7 nM, respectively.
Axitinib
Axitinib (AG-013736) is a multiple receptor kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-β and c-KIT with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.
BIBF1120 (Vargatef)
BIBF1120 (Vargatef) is a potent VEGF receptor (VEGFR), PDGFR and FGFR kinase inhibitor for VEGFR1, VEGFR2, VEGFR3 with IC50 of 34 nM, 5 nM and 5 nM, respectively.
Cediranib (AZD2171)
Cediranib (AZD2171) is a highly potent VEGFR2 inhibitor for VEGF-stimulated proliferation and KDR phosphorylation with IC50 of 0.4 nM and 0.5 nM, respectively.
Motesanib Diphosphate (AMG-706)
Motesanib (AMG-706) is a multiple inhibitor of VEGFR1/2/3(IC50: 2 ηM /3 ηM /6 ηM),PDGFR (84ηM), kit (8ηM), and Ret (59ηM)receptors
Pazopanib HCl
Pazopanib HCl is a VEGFR inhibitor, IC50 of 10, 30 and 47 nM for VEGFR-1, -2, and -3.
Sorafenib (Nexavar)
Sorafenib (Nexavar) is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and PDGFR) and RAF/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.
Sunitinib Malate (Sutent)
Sunitinib (Sutent) is a multitargeted FLT3, PDGFRs, VEGFRs, and Kit kinase inhibitor with Ki of 0.009 and 0.008 μM for Flk-1 and PDGFR
Vandetanib (Zactima)
Vandetanib (Zactima) is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50 of 60, 90, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively.
Crizotinib (PF-02341066)
Inhibitor of the c-Met kinase and the NPM-ALK. Crizotinib (PF02341066) inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM).
Biological Activity
BMS-794833,a potent ATPcompetitive Met/VEGFR-2 kinase inhibitor,demonstrates enhanced activity versus both Met-dependent and Met-insensitive tumor lines. BMS-794833 also inhibits Ron (Met family),Axl (phylogenetically related Axl/Tyro3/Mer subfamily) and Flt-3 with IC50 values <3 nM. The compound was selective versus a panel of >200 additional RTKs, non-RTKs and serine/threonine kinases based on biochemical or Ambit binding assays. In cell culture, BMS-794833 inhibited the proliferation of human tumor cell lines containing constitutively activated Met receptor (GTL-16 gastric carcinoma). Tumor cell lines whose growth is stimulated by HGF (U87 glioblastoma) were also effectively inhibited by BMS-794833. In vivo, BMS-794833 demonstrated dose-dependent tumor growth inhibition following oral administration in the GTL-16 and L2987 lung carcinoma (Met-insensitive) xenograft models. Despite the impressive antitumor activity, BMS-794833 showed dissolution rate-limited absorption from solid dosage forms.
Product Information
| Molecular Weight (WM): | 468.84 |
|---|---|
| Formula: | C23H15ClF2N4O3 |
| CAS No.: | 1174046-72-0 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥94mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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