Sunitinib (SU11248) - Moligand™, 10mM in DMSO , Inhibitor of fibroblast growth factor receptor 1;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of fms related receptor tyrosine kinase 4;Inhibitor of kinase insert domain receptor;Inhibitor o, Inhibitor of fibroblast growth factor receptor 1;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of fms related receptor tyrosine kinase 4;Inhibitor of kinase insert domain receptor;Inhibitor of KIT proto-oncogene; receptor tyrosine kinase;I

CAS: 557795-19-4 Cat. No.: S408232 Molecular Weight: 398.47 EC Number: 111-194-2 PubChem CID: 5329102
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GRADE & PURITY Moligand™ ? Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools. 10mM in DMSO
Synonyms
(Z)-N-(2-(diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
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Size
Status
Price
Qty
1ml
S408232-1ml
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Why this grade

Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.

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Storage & shipping

Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.

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Quality documents

SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.

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Literature proof

Cited in 19 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.

Overview

Information

Sunitinib (SU11248) is a multi-targeted RTK inhibitor targetingVEGFR2(Flk-1) andPDGFRβwithIC50of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity ofIRE1α. Sunitinib inducesautophagya
In vitro

Sunitinib also potently inhibits Kit and FLT-3. Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner.

In vivo

Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model.
Cell Data

cell lines:

Concentrations:Dissolved in DMSO, final concentrations ~10 μM

Incubation Time:24 and 48 hours

Powder Purity:≥99%

Specifications

Synonyms
(Z)-N-(2-(diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2, 4-dimethyl-1H-pyrrole-3-carboxamide
Specifications & Purity
Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms
Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces au
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of fibroblast growth factor receptor 1;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of fms related receptor tyrosine kinase 4;Inhibitor of kinase insert domain receptor;Inhibitor of KIT proto-oncogene; receptor tyrosine kinase;I
Names and Identifiers
Isomeric SMILES CCN(CC)CCNC(=O)C1=C(NC(=C1C)/C=C\2/C3=C(C=CC(=C3)F)NC2=O)C
PubChem CID 5329102
UN Number 2811
Packing Group III
Molecular Weight 398.47

Documentation

📋 Safety Data Sheet (SDS)

Comprehensive hazard, handling, storage, and regulatory compliance document.

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✅ Certificate of Analysis (COA)

Lot-specific quality data. Enter your lot number to retrieve the exact COA.

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📊 Datasheet

Quick-reference summary of product specifications and applications.

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🔬 Specification Sheet

Full quality attributes and acceptance criteria for this grade.

View spec sheet →

Advanced Data

Associated Targets(Human)
GJD4 Tdark Gap junction delta-4 protein (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DLK1 Tchem Protein delta homolog 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CSF1R Tclin Macrophage colony-stimulating factor 1 receptor (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DAPK3 Tchem Death-associated protein kinase 3 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RET Tclin Proto-oncogene tyrosine-protein kinase receptor Ret (11 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
STK17A Tchem Serine/threonine-protein kinase 17A (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
STK10 Tchem Serine/threonine-protein kinase 10 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
STK33 Tchem Serine/threonine-protein kinase 33 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
STK4 Tchem Serine/threonine-protein kinase 4 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FLT4 Tclin Vascular endothelial growth factor receptor 3 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
IRAK1 Tchem Interleukin-1 receptor-associated kinase 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 (38 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GAK Tchem Cyclin-G-associated kinase (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FGFR1 Tclin Fibroblast growth factor receptor 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CSNK1D Tchem Casein kinase I isoform delta (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ITK Tclin Tyrosine-protein kinase ITK/TSK (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MERTK Tchem Tyrosine-protein kinase Mer (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TNIK Tchem TRAF2 and NCK-interacting protein kinase (6 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PDGFRA Tclin Platelet-derived growth factor receptor alpha (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PHKG1 Tchem Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PDGFRB Tclin Platelet-derived growth factor receptor beta (15 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MINK1 Tchem Misshapen-like kinase 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RPS6KA2 Tchem Ribosomal protein S6 kinase alpha-2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP3K19 Tchem Mitogen-activated protein kinase kinase kinase 19 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
LCK Tclin Tyrosine-protein kinase Lck (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP4K1 Tchem Mitogen-activated protein kinase kinase kinase kinase 1 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
LRRK2 Tchem Leucine-rich repeat serine/threonine-protein kinase 2 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK1 Tclin Tyrosine-protein kinase JAK1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BMP2K Tchem BMP-2-inducible protein kinase (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
Tchem Uncharacterized protein FLJ45252 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FLT1 Tclin Vascular endothelial growth factor receptor 1 (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KDR Tclin Vascular endothelial growth factor receptor 2 (33 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
AAK1 Tchem AP2-associated protein kinase 1 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PRKAA1 Tclin 5'-AMP-activated protein kinase catalytic subunit alpha-1 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CHEK2 Tchem Serine/threonine-protein kinase Chk2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
AXL Tchem Tyrosine-protein kinase receptor UFO (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ULK1 Tchem Serine/threonine-protein kinase ULK1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ULK2 Tchem Serine/threonine-protein kinase ULK2 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CLK1 Tchem Dual specificity protein kinase CLK1 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CLK2 Tchem Dual specificity protein kinase CLK2 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CLK4 Tchem Dual specificity protein kinase CLK4 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KIT Tclin Mast/stem cell growth factor receptor Kit (27 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PAK3 Tchem Serine/threonine-protein kinase PAK 3 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MYLK3 Tchem Myosin light chain kinase 3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MYLK Tchem Myosin light chain kinase, smooth muscle (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
Certificates(CoA,COO,BSE/TSE and Analysis Chart)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Chemical and Physical Properties
SolubilitySolubility (25°C) In vitro Ethanol: 49 mg/mL (196.98 mM); Water: 21 mg/mL (84.42 mM); DMSO: 12 mg/mL (48.24 mM);
Citations of This Product
References
1. Huimin Xie, Lin Ma, Xiaoli He, Songsong Zhao, Jin Wang, Ao Zhu, Changming Liu, Olga Piskareva, Chao Deng, Fenghua Meng, Mi Liu.  (2025)  Elevating MHC I expression on tumor cells by nanovesicles loading tyrosine kinase inhibitors can improve the efficacy of cancer vaccines.  Frontiers in Immunology,      [PMID:41019037] [10.3389/fimmu.2025.1653533]
2. Xiaofei Zhang, Mengyuan Lv, Yuyang Wang, Nan Zhang, Di Chen.  (2025)  Inner-wall biochar-coated pipette tip microextraction for rapid and sustainable determination of tyrosine kinase inhibitors in plasma.  RSC Advances,  15  (40): (33536-33548).  [PMID:40959299] [10.1039/D5RA05405B]
3. Xianzhou Huang, Lu Li, Chunqing Ou, Meiling Shen, Xinchao Li, Miaomiao Zhang, Rui Wu, Xiaorong Kou, Ling Gao, Furong Liu, Rui Luo, Qinjie Wu, Changyang Gong.  (2023)  Tumor Environment Regression Therapy Implemented by Switchable Prune-to-Essence Nanoplatform Unleashed Systemic Immune Responses.  Advanced Science,      [PMID:37875395] [10.1002/advs.202303715]
4. Yingping Zeng, Shufen Zhang, Sufen Li, Guangtao Song, Tingting Meng, Hong Yuan, Fuqiang Hu.  (2023)  Normalizing Tumor Blood Vessels to Improve Chemotherapy and Inhibit Breast Cancer Metastasis by Multifunctional Nanoparticles.  MOLECULAR PHARMACEUTICS,      [PMID:37728215] [10.1021/acs.molpharmaceut.3c00381]
5. Dongjie Li, Chengzhu Song, Chunpu Song, Xinrui Tian, Huaibo Zhang, Jie Zhang, Xiaoyan Zhao.  (2023)  Sunitinib induces cardiotoxicity through modulating oxidative stress and Nrf2-dependent ferroptosis in vitro and in vivo.  CHEMICO-BIOLOGICAL INTERACTIONS,      [PMID:38101598] [10.1016/j.cbi.2023.110829]
6. Fangjun Chen, Wenda Chen, Zhenxin Wang, Yingfei Peng, Beili Wang, Baishen Pan, Wei Guo.  (2023)  Development and clinical application of a liquid chromatography-tandem mass spectrometry-based assay to quantify eight tyrosine kinase inhibitors in human plasma.  Journal of Mass Spectrometry and Advances in the Clinical Lab,      [PMID:37234251] [10.1016/j.jmsacl.2023.05.001]
7. Yingping Zeng, Tong Yu, Shufen Zhang, Guangtao Song, Tingting Meng, Hong Yuan, Fuqiang Hu.  (2022)  Combination of tumor vessel normalization and immune checkpoint blockade for breast cancer treatment via multifunctional nanocomplexes.  Biomaterials Science,  10  (15): (4140-4155).  [PMID:35726757] [10.1039/D2BM00600F]
8. Zhiguang Fu, Hongqi Li, Peng Xue, Hanying Yu, Shuo Yang, Cheng Tao, Wei Li, Yingjie Wang, Jianjun Zhang, Yu Wang.  (2022)  Implantable Bioresponsive Hydrogel Prevents Local Recurrence of Breast Cancer by Enhancing Radiosensitivity.  Frontiers in Bioengineering and Biotechnology,      [PMID:35497337] [10.3389/fbioe.2022.881544]
9. Hou Bolin, Wang Gang, Gao Quan, Wei Yanjie, Zhang Caining, Wang Yange, Huo Yuqing, Yang Huaiyi, Jiang Xuejun, Xi Zhijun.  (2019)  SQSTM1/p62 loss reverses the inhibitory effect of sunitinib on autophagy independent of AMPK signaling.  Scientific Reports,  (1): (1-13).  [PMID:31366950] [10.1038/s41598-019-47597-4]
10. Gao Ningning, Zhong Jingjing, Wang Xiaodong, Jin Zhenchao, Li Wang, Liu Yu, Diao Yuwen, Wang Zhulin, Jiang Wenqi, Jin Guangyi.  (2016)  Immunomodulatory and Antitumor Effects of a Novel TLR7 Agonist Combined with Lapatinib.  Scientific Reports,  (1): (1-9).  [PMID:28000738] [10.1038/srep39598]
11. Wei Li, Yan Wang, Hongkun Miao, Maohui Yan, Chen Liu, Yu Wang, Jianjun Zhang, Zhiguang Fu.  (2025)  Application of MMP-2-responsive in situ forming injectable hydrogel in preventing the recurrence of oral squamous cell carcinoma.  RSC Advances,  15  (3): (1507-1513).  [PMID:39831041] [10.1039/D4RA06120A]
12. Qianqian Wang, Yuanyuan Zheng, Bowen Deng, Di Chen, Liuqun Jia, Nian Shi.  (2024)  Automated kapok fiber-based pipette-tip solid-phase extraction coupled with liquid chromatography-tandem mass spectrometry for rapid and sensitive analysis of tyrosine kinase inhibitors in plasma.  JOURNAL OF CHROMATOGRAPHY A,      [PMID:39378625] [10.1016/j.chroma.2024.465420]
13. Jing Ye, Yuanyuan Zheng, Xiangyu Li, Xingyi Jiang, Di Chen.  (2024)  Melt-blown polypropylene nonwoven as an efficient and eco-economic sorbent for pipette tip micro-solid phase extraction for the determination of tyrosine kinase inhibitors.  ANALYTICA CHIMICA ACTA,      [PMID:39396303] [10.1016/j.aca.2024.343240]
14. Qianqian Wang, Yuwei Liu, Yuanyuan Zheng, Di Chen, Ya Xie, Nian Shi.  (2024)  MonoTip C18 pipette tip solid-phase extraction coupled with liquid chromatography-tandem mass spectrometry enables rapid and automated therapeutic drug monitoring of tyrosine kinase inhibitors.  Arabian Journal of Chemistry,      [PMID:] [10.1016/j.arabjc.2024.105976]
15. Ruyi Lin, Jia Yan, Bokai Gong, Fan Tong, Yujun Song, Xue Xia, Haili Hu, Yufan Wang, Yang Zhou, Tao Gong, Maxim Shevtsov, Huile Gao.  (2024)  Self-Delivered Transformable Nanosystem Capable of Enhancing Photodynamic Effectiveness and Multi-Target Ameliorating Immunosuppression for Treatment of Breast Cancer and Lung Metastasis.  ADVANCED FUNCTIONAL MATERIALS,      [PMID:] [10.1002/adfm.202405051]
16. Guang-rong Lu, Rui-zhen Wang, Xin-yu Zhao, Jun-er Xu, Cheng-ke Huang, Wei Sun, Rui-jie Chen, Zhe Wang.  (2024)  The CYP3A inducer dexamethasone affects the pharmacokinetics of sunitinib by accelerating its metabolism in rats.  CHEMICO-BIOLOGICAL INTERACTIONS,      [PMID:39244184] [10.1016/j.cbi.2024.111228]
17. Dong Wang, Mengrong Li, Tingting Dai, Xiangyu Zhang, Di Chen.  (2025)  Sensitive analysis of tyrosine kinase inhibitors in plasma using polypropylene fabric-solid phase extraction combined with liquid chromatography-tandem mass spectrometry.  JOURNAL OF CHROMATOGRAPHY A,      [PMID:40865307] [10.1016/j.chroma.2025.466315]
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19. Dong Wang, Mengrong Li, Xiangyu Zhang, Xu Miao, Lifeng Han, Di Chen.  (2026)  Standardized ready-to-use natural deep eutectic solvent-impregnated polypropylene fiber units for robust and high-throughput determination of tyrosine kinase inhibitors in biological fluids.  ANALYTICA CHIMICA ACTA,      [PMID:] [10.1016/j.aca.2026.345394]
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