Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
(SU11662; SU 11662; SU-11662)
N-Desethyl Sunitinib Chemical Structure
|Product name: N-Desethyl Sunitinib|
|Cat. No.: HY-10873|
N-desethyl sunitinib(SU-11662) is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively).
Targe: VEGFR; PDGFRβ
N-Desethyl Sunitinib is a major and pharmacologically active metabolite of the tyrosine kinase inhibitor and anticancer drug Sunitinib. Sunitinib also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Sunitinib exhibits antiangiogenic and antitumor activity in multiple xenograft models.
|M.Wt||370.42||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.6996 mL||13.4982 mL||26.9964 mL|
|5 mM||0.5399 mL||2.6996 mL||5.3993 mL|
|10 mM||0.2700 mL||1.3498 mL||2.6996 mL|
. Tang, Seng Chuan; Lankheet, Nienke A. G.; Poller, Birk et al. P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) restrict brain accumulation of the active sunitinib metabolite N-desethyl sunitinib. Journal of Pharmacology and Experimental Therapeutics (2012), 341(1), 164-173.
. Penot P, Bouaziz JD, Battistella M, Kerob D, Pagès C, Vilmer C, Basset-Seguin N, Madjessli N, Comte C, Farges C, Bagot M, le Maignan C, Lebbé C.Multiple metastatic epithelioid sarcoma stabilization under sunitinib malate treatment.Br J Dermatol. 2012 Sep 10.
. Nowak AK, Millward MJ, Creaney J, Francis RJ, Dick IM, Hasani A, van der Schaaf A, Segal A, Musk AW, Byrne MJ.A Phase II Study of Intermittent Sunitinib Malate as Second-Line Therapy in Progressive Malignant Pleural Mesothelioma.J Thorac Oncol. 2012 Sep;7(9):1449-56.
2,4-Pyrimidinediamine with linker is a patent compound in WO2013055780A1, Page 71; multikinase inhibitor and has a -NH2 terminal linker for further synthesis.
Altiratinib(DCC-2701) is a novel c-MET/TIE-2/VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with a HGF antagonist in vitro.
Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFR(alpha) and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively.
Apatinib(YN-968D1) is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.
Axitinib(AG013736) blocked phosphorylation of VEGFR-2 and VEGFR-3 with average IC50s of 0.2 and 0.1 to 0.3 nM.
AZD2932 is a new series of quinazoline ether inhibitor which potently inhibits VEGFR-2 and PDGFR with IC50s of 4 nM/8 nM/ 7 nM for PDGFR(beta)/VEGFR-2/Flt-3.
BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases.
BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7/15 nM; also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378.
CP 673451 is a selective inhibitor of PDGFR(alpha)/(beta) with IC50 of 10 nM/1 nM, exhibits >450-fold selectivity over other angiogenic receptors, has antiangiogenic and antitumor activity.
Crenolanib (CP-868596) is a potent and selective inhibitor of PDGFR(alpha)/(beta) with Kd of 2.1 nM/3.2 nM, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src.