Sunitinib
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
Product Specifications
CAS Number
[557795-19-4]
Product Name Alternative
SU 11248
UNSPSC
12352005
Hazard Statement
H360, H372
Target
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.html
Purity
99.69
Solubility
DMSO : 20.83 mg/mL (ultrasonic)
Smiles
O=C(NCCN(CC)CC)C1=C(NC(/C=C2C(NC3=C\2C=C(C=C3)F)=O)=C1C)C
Molecular Formula
C22H27FN4O2
Molecular Weight
398.47
Precautions
H360, H372
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 receptor tyrosine kinase. J Med Chem. 2003 Mar 27;46 (7) :1116-9.|[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 Can
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, protect from light)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
PDGFRβ; VEGFR2/KDR/Flk-1
Citation 01
ACS Appl Mater Interfaces. 2024 Apr 16|Acta Pharm Sin B. 2025 Aug 7.|Acta Pharmacol Sin. 2021 Jan;42 (1) :108-114.|Adv Sci (Weinh) . 2025 Nov 17:e12563.|Adv Sci (Weinh) . 2025 Sep 15:e06367.|Arch Toxicol. 2019 Jun;93 (6) :1697-1712. |Autophagy. 2025 Mar;21 (3) :619-638.|Biochem Biophys Res Commun. 2024 Aug 19:739:150568.|Biochem Biophys Res Commun. 2025 May 15:771:152027.|Bioengineering (Basel) . 2025 Oct 19;12 (10) :1121.|Biomacromolecules. 2021 Jun 14;22 (6) :2625-2640.|Biomed Pharmacother. 2025 May 14:188:118137.|Biomed Pharmacother. 2025 May 8:187:118136.|bioRxiv. 2024 Aug 8:2024.08.08.607189.|bioRxiv. 2024 Jul 10:2024.07.09.602803.|Biotechnol Bioeng. 2021 Dec;118 (12) :4687-4698.|Blood. 2019 Oct 17;134 (16) :1323-1336. |Br J Cancer. 2024 Jul;131 (2) :347-360.|Cancer Lett. 2019 Apr 10:447:105-114.|Cancer Lett. 2021 Dec 28:523:121-134.|Cancer Lett. 2024 Jul 1:593:216963.|Cancers (Basel) . 2022 Aug 13;14 (16) :3917.|Cell Death Dis. 2024 Jul 27;15 (7) :533.|Cell Metab. 2021 Oct 5;33 (10) :2021-2039.e8.|Cell Rep Med. 2025 Apr 2:102053.|Cell Rep Methods. 2023 Oct 23;3 (10) :100599.|Cell Signal. 2024 Sep 20:111425.|Chemosphere. 2022 Dec;308 (Pt 2) :136354.|Clin Transl Med. 2025 Feb;15 (2) :e70231.|EMBO J. 2021 Jun 1;40 (11) :e106771.|Eur J Med Res. 2025 Apr 18;30 (1) :306.|Exp Cell Res. 2020 Aug 1;393 (1) :112054.|Exp Cell Res. 2025 Nov 22;454 (2) :114839.|Front Pharmacol. 2021 Apr 29:12:664181.|Front Pharmacol. 2021 Mar 8;12:644342.|Heliyon. 2024 Mar 16;10 (6) :e28295.|Hum Cell. 2025 May 13;38 (4) :100.|Int Immunopharmacol. 2020 Apr;81:106227.|Int J Clin Exp Pathol. 2015 Apr 1;8 (4) :3871-81.|iScience. 2024 Jun 28;27 (7) :110415.|J Cell Mol Med. 2025 Feb;29 (4) :e70428.|J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Apr 15:1237:124100.|J Med Chem. 2016 Sep 22;59 (18) :8456-72. |J Med Chem. 2019 Jul 11;62 (13) :6083-6101.|J Pharm Anal. 2023 May;13 (5) :514-522.|J Transl Med. 2023 Jan 9;21 (1) :9.|Med Chem Res. 2017, 26 (9), 2007-2014.|Mol Clin Oncol. 2024 Jan 18;20 (3) :21.|Mol Oncol. 2024 Jan;18 (1) :136-155.|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.|PLoS One. 2024 Nov 1;19 (11) :e0308647.|Res Sq. 2024 Jun 25.|Research Square Preprint. 2022 Feb.|Research Square Preprint. 2022 May.|Sci Adv. Sci Adv. 2025 Apr 25;11 (17) :eadu0847.|Sci Rep. 2025 Aug 17;15 (1) :30048.|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.|University of Oklahoma. 2024.|Virulence. 2022 Dec;13 (1) :1849-1867.|Acta Oncol. 2025 May 27:64:715-728.|Adv Mater. 2024 May;36 (18) :e2310421.|Biochem Biophys Res Commun. 2024 Feb 26:698:149546.|Biochem Pharmacol. 2025 Jun 3:117023.|EBioMedicine. 2018 Nov:37:344-355.|Food Chem Toxicol. 2023 May:175:113743.|Harvard Medical School LINCS LIBRARY|Methods Mol Biol. 2024:2777:191-204.|Mol Cell. 2025 Jul 17;85 (14) :2733-2748.e7.|Oncotarget. 2017 Jul 27;8 (56) :95116-95134. |R Soc Open Sci. 2025 Apr 23;12 (4) :241817.|University of Michigan. 2021 Jun.
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