sunitinib

Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80 2 nM). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.

Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.

5-(5-Fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic Acid is a sunitinib impurity.

N,N-Didesethyl Sunitinib Hydrochloride is a potent AMPK inhibitor with IC50 of 393 nM and 141 nM for AMPKα1 and AMPK2,respectively.

Sunitinib D10 is a deuterium labeled Sunitinib. Sunitinib is a inhibitor of multi-targeted receptor tyrosine kinase(IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively).

Sunitinib-d4 is a deuterated compound of Sunitinib.

N-Desethyl Sunitinib (SU-12662) (hydrochloride), a metabolite of sunitinib, is a robust ATP-competitive inhibitor of VEGFR, PDGFRβ, and KIT, with inhibition constants (K i values) of 2, 9, 17, 8, and 4 nM for VEGFR-1, -2, -3, PDGFRβ, and KIT, respectively [1].

N-Desethyl Sunitinib (SU-11662) is a sunitinib metabolite.

N-Desethylsunitinib hydrochloride is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ, and KIT inhibitor.

Elacridar (GG918) (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.

SB02024 is a VPS34 inhibitor. SB02024 activates cGAS-STING signaling and sensitizes tumors to STING agonist. SB02024 blocked autophagy in vitro and reduced xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7, in vivo. Vps34 inhibitor significantly potentiated cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro in monolayer cultures and when grown as multicellular spheroids. Our data suggests that inhibition of autophagy significantly improves sensitivity to Sunitinib and Erlotinib and that Vps34 is a promising therapeutic target for combination strategies in breast cancer.

Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate containing a cereblon ligand derived from Thalidomide and a linker used in the synthesis of MI-389 [compound 22], a highly effective phthalimide PROTAC degrader developed from the multi-targeted receptor tyrosine kinase inhibitor sunitinib.