Sunitinib (Malate)

Sunitinib (Malate)

• CAS Number: 341031-54-7
• UNSPSC Description: Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
• Target Antigen: Apoptosis; Autophagy; IRE1; Mitophagy; PDGFR; VEGFR
• Type: Reference compound
• Related Pathways: Apoptosis;Autophagy;Cell Cycle/DNA Damage;Protein Tyrosine Kinase/RTK
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/Sunitinib-Malate.html
• Purity: 99.91
• Solubility: DMSO : ≥ 15 mg/mL|H2O : 12.5 mg/mL (ultrasonic;adjust pH to 3 with HCl)|H2O : 3.33 mg/mL (ultrasonic;warming;heat to 60°C)
• Smiles: O=C(NCCN(CC)CC)C1=C(NC(/C=C2C(NC3=C\2C=C(C=C3)F)=O)=C1C)C.O=C([C@H](CC(O)=O)O)O
• Molecular Weight: 532.56
• References & Citations: [1]Sun L, et al. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor r|[2]Ali MM, et al. Structure of the Ire1 autophosphorylation complex and implications for the unfolded protein response. EMBO J. 2011 Mar 2;30(5):894-905.|[3]O'Farrell AM, et al. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood. 2003 May 1;101(9):3597-605.|[4]Mendel DB, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin CanAdv Mater. 2024 Jan 25:e2310421.|Biochem Biophys Res Commun. 2024 Jan 18:698:149546.|EBioMedicine. 2018 Nov;37:344-355.|Food Chem Toxicol. 2023 Mar 25;113743.|Harvard Medical School LINCS LIBRARY|Methods Mol Biol. 2024:2777:191-204.|Oncotarget. 2017 Jul 27;8(56):95116-95134. |University of Michigan. 2021 Jun.|ACS Appl Mater Interfaces. 2024 Apr 16|Acta Pharmacol Sin. 2021 Jan;42(1):108-114.|Arch Toxicol. 2019 Jun;93(6):1697-1712. |Autophagy. 2024 Oct 30.|Biochem Biophys Res Commun. 2024 Aug 19:739:150568.|Biomacromolecules. 2021 Jun 2.|bioRxiv. 2024 Aug 8:2024.08.08.607189.|bioRxiv. 2024 Jul 10:2024.07.09.602803.|Biotechnol Bioeng. 2021 Sep 3.|Blood. 2019 Oct 17;134(16):1323-1336. |Br J Cancer. 2024 May 31.|Cancer Lett. 2019 Apr 10;447:105-114.|Cancer Lett. 2021 Oct 6;S0304-3835(21)00513-9.|Cancer Lett. 2024 Jul 1:593:216963.|Cancers (Basel). 2022, 14(16), 3917.|Cell Death Dis. 2024 Jul 27;15(7):533.|Cell Metab. 2021 Sep 8;S1550-4131(21)00375-2.|Cell Rep Methods. 2023 Oct 23;3(10):100599.|Cell Signal. 2024 Sep 20:111425.|Chemosphere. 2022 Sep 7;136354.|EMBO J. 2021 Apr 28;e106771.|Exp Cell Res. 2020 Aug 1;393(1):112054.|Front Pharmacol. 2021 Mar 8;12:644342.|Front Pharmacol. 29 April 2021.|Heliyon. 2024 Mar 30, e28295.|Int Immunopharmacol. 2020 Apr;81:106227.|Int J Clin Exp Pathol. 2015 Apr 1;8(4):3871-81.|iScience. 2024 June 28.|J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Mar 26:1237:124100.|J Med Chem. 2016 Sep 22;59(18):8456-72. |J Med Chem. 2019 Jul 11;62(13):6083-6101.|J Pharm Anal. 2023 Apr 19.|J Transl Med. 2023 Jan 9;21(1):9.|Med Chem Res. 2017, 26(9), 2007-2014.|Mol Clin Oncol. 2024 Jan 18.|Mol Oncol. 2023 Nov 27.|Nat Biomed Eng. 2018 Aug;2(8):578-588.|Oncotarget. 2017 Nov 15;8(67):111110-111118. |Patent. US20220064117A1.|Patent. US20230226111A1.|Patent. US20240238271A1.|Patent. US20240325538A1.|Res Sq. 2024 Jun 25.|Research Square Preprint. 2022 Feb.|Research Square Preprint. 2022 May.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Stem Cell Reports. 2017 Dec 12;9(6):1948-1960.|Ther Adv Med Oncol. 2019 May 17;11:1758835919849757. |Theranostics. 2018 Jul 30;8(15):4262-4278.|Theranostics. 2021 Mar 12;11(11):5387-5403.|Theranostics. 2019 Oct 22;9(26):8377-8391. |Toxicol In Vitro. 2021 Mar;71:105063.|Virulence. 2022 Dec;13(1):1849-1867.
• Shipping Conditions: Room Temperature
• Storage Conditions: 4°C (Powder, sealed storage, away from moisture)
• Clinical Information: Launched