SU10994|SU-10994|VEGFR inhibitor

Cas No.:
Chemical Name:	SU-10994
Synonyms:	SU10994;SU 10994
SMILES:	CC1=CC(CCC(=O)O)=C(/C=C2\C(=O)NC3=CC=CC=C23)N1
Formula:	C₁₇H₁₆O₃N₂
M.Wt:	296.33
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

AMG-232 is a novel inhibitor of p53-MDM2 with IC50 value of 9.2 nM. Tumor protein p53 (p53) is a very unstable protein with a half-life ranging from 5 to 30 min and participates in a variety of anticancer processes, such as inducing cell apoptosis and inhibiting angiogenesis. Mouse double minute 2 homolog (MDM2), also named as E3 ubiquitin-protein ligase Mdm2, involves in mediating p53 tumor suppressor. It has been conclusively demonstrated p53 is under-expressed in tumor cells. AMG-232 is a potent p53-MDM2 interaction inhibitor and is regarded as a promising drug in clinic. When tested with SJSA-1 tumor cell line, AMG-232 treatment resulted in cell-cycle arrest and inhibition of tumor cell proliferation via binding to MDM2 protein and robustly inducing p53 activity. It was shown that p53-MDM2 bond rang from a Kd of 60 to 700 nM Depending on the length of p53 peptide. In mouse model with SJSA-1 tumor cells subcutaneous xenograft, co-administration of AMG-232 and chemotherapies induced DNA damage and p53 activity which resulted in significantly superior antitumor efficacy and regression through arresting cell growth and inducting apoptosis.

Cat. No.	Product name	Field of application
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DC71628	WAY-340935	WAY-340935 (VEGFR2-IN-2) can inhibit the function of VEGFR2 and the anti-proliferative activity against the H460 cell line is produced partly by interaction of VEGFR protein.
DC71627	Ansornitinib	Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases.
DC71625	Tivozanib hydrochloride hydrate	Tivozanib hydrochloride hydrate is a potent and selective and orally active VEGFR tyrosine kinase inhibitor with IC50是of 0.21, 0.16, 0.24 nM for VEGFR-1, VEGFR-2, VEGFR-3, respectively. Tivozanib hydrochloride hydrate inhibits angiogenesis and vascular permeability in tumor tissues and shows antitumor activity. Tivozanib hydrochloride hydrate has the potential for the research of metastatic renal cell carcinoma (RCC) .
DC7607	Vatalanib	Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 1/2.
DC5078	Tivozanib(AV-951)	Tivozanib (AV-951, KRN-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 0.21 nM/0.16 nM/0.24 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met EGFR and IGF-1R.
DC10065	Takeda-6d	Takeda-6d has potent inhibitory activity in both B-RAF with an IC50 of 7.0 nM and VEGFR2 with an IC50 of 2.2 nM.
DC7302	SU14813	SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), Kit, and fms-like tyrosine kinase 3 (FLT-3).
DC9794	SU-10994	SU-10994 is a novel VEGFR inhibitor.
DC10284	Motesanib	Motesanib is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.