E7080 (Lenvatinib) Chemical Structure
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 (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) 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) 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 (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 is a VEGFR inhibitor, IC50 of 10, 30 and 47 nM for VEGFR-1, -2, and -3.
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 (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) 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.
Brivanib (BMS-540215) is a VEGFR -2 inhibitor with an IC50 of 25 nM and Ki of 26 nM.
E7080 (Lenvatinib) is the most potent dual inhibitor of VEGF-R3 tyrosine kinase (IC50=5.2 nM) as well as VEGF-R2 tyrosine kinase (IC50=4.0 nM) among those small-molecule inhibitors of VEGF-R kinases, such as sunitinib, sorafenib, and CEP-7055. It has been evaluated in vitro (pre-clinical) for anti-cancer effects. E7080 (Lenvatinib) suppresses lymph node and lung metastases of human mammary breast tumor MDA-MB-231 via inhibition of angiogenesis and lymphangiogenesis. [2,3]
It has had promising results from a phase I clinical trial in 2006 and is being tested in several Phase I and II trials as of October 2009, for example against hepatocellular carcinoma and non-small cell lung carcinoma. [1]
| Molecular Weight (WM): | 426.85 |
|---|---|
| Formula: | C21H19ClN4O4 |
| CAS No.: | 417716-92-8 |
| Synonyms: |
N/A
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| Dissolve in (25°C): | DMSO ≥16mg/mL |
| Water <1mg/mL | |
| Ethanol ≥1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
A collection of 426 FDA approved drugs
A collection of 139 natural products
A collection of 40 chemotherapeutic agents
A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules
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