Sunitinib Malate
Based on 96 publication(s) in Google Scholar
Sunitinib (SU 11248) Malat is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malat, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
For research use only. We do not sell to patients.
- Purity: 99.74%
- CAS No.: 341031-54-7
- Formula: C26H33FN4O7
- Molecular Weight:532.56
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Sunitinib Malate
More- Cell Metab. 2021 Oct 5;33(10):2021-2039.e8. [Abstract]
- Adv Mater. 2024 May;36(18):e2310421. [Abstract]
- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Blood. 2019 Oct 17;134(16):1323-1336. [Abstract]
- Mol Cell. 2025 Dec 18;85(24):4602-4620.e9. [Abstract]
- Mol Cell. 2025 Jul 17;85(14):2733-2748.e7. [Abstract]
- Cell Death Differ. 2026 Mar 23. [Abstract]
- Trends Biotechnol. 2025 Dec 18:S0167-7799(25)00490-1. [Abstract]
- Acta Pharm Sin B. 2025 Oct;15(10):5458-5473. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Autophagy. 2026 May;22(5):982-1002. [Abstract]
- Autophagy. 2025 Mar;21(3):619-638. [Abstract]
- Adv Sci (Weinh). 2026 Apr;13(23):e11606. [Abstract]
- Adv Sci (Weinh). 2025 Nov 17:e12563. [Abstract]
- Adv Sci (Weinh). 2025 Sep 15:e06367. [Abstract]
- Theranostics. 2021 Mar 12;11(11):5387-5403. [Abstract]
- Theranostics. 2019 Oct 22;9(26):8377-8391. [Abstract]
- Theranostics. 2018 Jul 30;8(15):4262-4278. [Abstract]
- Sci Adv. Sci Adv. 2025 Apr 25;11(17):eadu0847. [Abstract]
- Redox Biol. 2026 May:92:104086. [Abstract]
- EBioMedicine. 2018 Nov:37:344-355. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- Cancer Lett. 2024 Jul 1:593:216963. [Abstract]
- Cancer Lett. 2021 Dec 28:523:121-134. [Abstract]
- Cancer Lett. 2019 Apr 10:447:105-114. [Abstract]
- Cell Death Dis. 2024 Jul 27;15(7):533. [Abstract]
- J Pharm Anal. 2023 May;13(5):514-522. [Abstract]
- Acta Pharmacol Sin. 2021 Jan;42(1):108-114. [Abstract]
- EMBO J. 2021 Jun 1;40(11):e106771. [Abstract]
- ACS Appl Mater Interfaces. 2024 Apr 24;16(16):20202-20211. [Abstract]
- Chemosphere. 2022 Dec;308(Pt 2):136354. [Abstract]
- NPJ Precis Oncol. 2026 Jun 19.
- Biomed Pharmacother. 2025 May 14:188:118137. [Abstract]
- Biomed Pharmacother. 2025 May 8:187:118136. [Abstract]
- J Transl Med. 2023 Jan 9;21(1):9. [Abstract]
- Arch Toxicol. 2019 Jun;93(6):1697-1712. [Abstract]
- Clin Transl Med. 2025 Feb;15(2):e70231. [Abstract]
- Br J Cancer. 2024 Jul;131(2):347-360. [Abstract]
- J Med Chem. 2019 Jul 11;62(13):6083-6101. [Abstract]
- J Med Chem. 2016 Sep 22;59(18):8456-72. [Abstract]
- Biochem Pharmacol. 2025 Jun 3:117023. [Abstract]
- Virulence. 2022 Dec;13(1):1849-1867. [Abstract]
- Biomacromolecules. 2021 Jun 14;22(6):2625-2640. [Abstract]
- Commun Biol. 2026 Feb 3;9(1):355. [Abstract]
- Stem Cell Reports. 2017 Dec 12;9(6):1948-1960. [Abstract]
- Front Pharmacol. 2021 Mar 8;12:644342. [Abstract]
- Front Pharmacol. 2021 Apr 29:12:664181. [Abstract]
- Eur J Pharm Sci. 2026 Mar 1:218:107440. [Abstract]
- Int Immunopharmacol. 2020 Apr;81:106227. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Mol Oncol. 2024 Jan;18(1):136-155. [Abstract]
- Cancers (Basel). 2022 Aug 13;14(16):3917. [Abstract]
- J Cell Mol Med. 2025 Feb;29(4):e70428. [Abstract]
- Ther Adv Med Oncol. 2019 May 17:11:1758835919849757. [Abstract]
- iScience. 2024 Jun 28;27(7):110415. [Abstract]
- J Biol Chem. 2026 Jun;302(6):111461. [Abstract]
- Sci Rep. 2026 Feb 6;16(1):7619. [Abstract]
- Sci Rep. 2025 Aug 17;15(1):30048. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Cell Signal. 2024 Sep 20:111425. [Abstract]
- Heliyon. 2024 Mar 16;10(6):e28295. [Abstract]
- Biotechnol Bioeng. 2021 Dec;118(12):4687-4698. [Abstract]
- Exp Cell Res. 2025 Nov 22;454(2):114839. [Abstract]
- Food Chem Toxicol. 2023 May:175:113743. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Eur J Med Res. 2025 Apr 18;30(1):306. [Abstract]
- Hum Cell. 2025 May 13;38(4):100. [Abstract]
- Med Chem Res. 2017, 26(9), 2007-2014.
- R Soc Open Sci. 2025 Apr 23;12(4):241817. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Apr 15:1237:124100. [Abstract]
- Toxicol In Vitro. 2021 Mar;71:105063. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Acta Oncol. 2025 May 27:64:715-728. [Abstract]
- Biochem Biophys Res Commun. 2025 May 15:771:152027. [Abstract]
- Biochem Biophys Res Commun. 2024 Aug 19:739:150568. [Abstract]
- Biochem Biophys Res Commun. 2024 Feb 26:698:149546. [Abstract]
- Biol Pharm Bull. 2026;49(1):122-129. [Abstract]
- Mol Clin Oncol. 2024 Jan 18;20(3):21. [Abstract]
- Int J Clin Exp Pathol. 2015 Apr 1;8(4):3871-81. [Abstract]
- bioRxiv. 2026 Apr 21.
- Res Sq. 2026 Apr 16.
- bioRxiv. 2026 Feb 20.
- Patent. US20240325538A1.
- Patent. US20240238271A1.
- bioRxiv. 2024 Aug 8:2024.08.08.607189. [Abstract]
- University of Oklahoma. 2024.
- bioRxiv. 2024 Jul 10:2024.07.09.602803. [Abstract]
- Res Sq. 2024 Jun 25.
- Methods Mol Biol. 2024:2777:191-204. [Abstract]
- Patent. US20230226111A1.
- Research Square Preprint. 2022 May.
- Patent. US20220064117A1.
- Research Square Preprint. 2022 Feb.
- University of Michigan. 2021 Jun.
- Oncotarget. 2017 Nov 15;8(67):111110-111118. [Abstract]
- Oncotarget. 2017 Jul 27;8(56):95116-95134. [Abstract]
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Cell Proliferation/Viability Assay
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IF
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WB
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WB
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WB
All VEGFR Isoforms
More
Biological Activity
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VEGFR2 80 nM (IC50) |
PDGFRβ 2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| ACHN | IC50 |
2 μM
Compound: Sun
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Cytotoxicity against human ACHN cells after 72 hrs by MTT assay
Cytotoxicity against human ACHN cells after 72 hrs by MTT assay
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[PMID: 25124114] |
Sunitinib Malate is also a good inhibitor of KIT and FLT-3[1]. In RS4;11 cells (FLT3-WT), treatment with Sunitinib (SU11248) inhibits FLT3-WT phosphorylation in a dose-dependent manner with IC50 of approximately 250 nM. In MV4;11 cells that express FLT3-ITD, Sunitinib inhibits FLT3-ITD phosphorylation in a dose-dependent manner with an IC50 of 50 nM following a 2-hour treatment[3].In biochemical assays, Sunitinib (SU11248) exhibits competitive inhibition (with regard to ATP) against Flk-1 and PDGFRβ with Ki values of 9 nM and 8 nM, respectively. Sunitinib is also a competitive, albeit less potent, inhibitor of FGFR1 tyrosine kinase activity, with a Ki value of 0.83 μM. In addition to these three structurally related split kinase domain RTKs, the activity of Sunitinib has also been evaluated against a broad panel of additional tyrosine and serine/threonine kinases. In these biochemical assays, the IC50 values for Sunitinib are generally at least 10-fold higher than those for Flk-1 and PDGFR (e.g., IC50values of: >10 μM for EGFR and Cdk2; 4 μM for Met; 2.4 μM for IGFR-1; 0.8 μM for Abl; and 0.6 μM for Src)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Sunitinib (80 mg/kg/day) inhibits the growth of established SF763T and Colo205 tumor xenografts in athymic mice. Sunitinib (SU11248) treatment effectively inhibits the growth of established tumor xenografts[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 341031-54-7
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Appearance Solid
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Molecular Weight 532.56
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Formula C26H33FN4O7
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Color Light yellow to orange
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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
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Synonyms
SU 11248 Malate
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (96)
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Journal Impact Factor
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Most Recent
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Cell Metab
The thermogenic activity of adjacent adipocytes fuels the progression of ccRCC and compromises anti-tumor therapeutic efficacy. [Abstract]2021 Oct 5;33(10):2021-2039.e8. PMID: 34508696 -
Adv Mater
Ultrasound Imaging of Tumor Vascular CD93 with MMRN2 Modified Microbubbles for Immune Microenvironment Prediction. [Abstract]2024 May;36(18):e2310421. PMID: 38270289 -
Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
Blood
Suz12 inactivation cooperates with JAK3 mutant signaling in the development of T-cell acute lymphoblastic leukemia. [Abstract]2019 Oct 17;134(16):1323-1336. PMID: 31492675 -
Mol Cell
Targeting PRDX6-dependent localization and function of GPX4 enhances ferroptosis-mediated tumor suppression. [Abstract]2025 Dec 18;85(24):4602-4620.e9. PMID: 41418756 -
Mol Cell
YTHDC1 lactylation regulates its phase separation to enhance target mRNA stability and promote RCC progression. [Abstract]2025 Jul 17;85(14):2733-2748.e7. PMID: 40680722 -
Cell Death Differ
2026 Mar 23. PMID: 41872532 -
Trends Biotechnol
Industrialization of 3D hiPSC-cardiac microtissues for high-throughput cardiac safety and drug discovery screening. [Abstract]2025 Dec 18:S0167-7799(25)00490-1. PMID: 41419348 -
Acta Pharm Sin B
Small-sized twin-nanoparticles normalize tumor vasculature to enhance tumor accumulation and penetration for potent eradication of cancer stem-like cells. [Abstract]2025 Oct;15(10):5458-5473. PMID: 41132849 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Autophagy
PRKAB2 as a tumor suppressor in renal cell carcinoma: inhibiting mitophagy via the LRPPRC-PRKN/parkin interaction and cardiolipin biosynthesis. [Abstract]2026 May;22(5):982-1002. PMID: 41612594 -
Autophagy
Atractylenolide I inhibits angiogenesis and reverses sunitinib resistance in clear cell renal cell carcinoma through ATP6V0D2-mediated autophagic degradation of EPAS1/HIF2α. [Abstract]2025 Mar;21(3):619-638. PMID: 39477683 -
Adv Sci (Weinh)
PDZK1-ULK1 Axis Triggers Lipophagy to Inhibit Tumor Progression and Sunitinib Resistance in Clear Cell Renal Cell Carcinoma. [Abstract]2026 Apr;13(23):e11606. PMID: 41698049 -
Adv Sci (Weinh)
Folic Acid-Modified Ginger-Derived Exosome-Like Nanoparticles Co-Delivering Sunitinib Suppress Renal Cell Carcinoma via PI3K-Akt Pathway Inhibition, P-gp Downregulation, and Macrophage Reprogramming. [Abstract]2025 Nov 17:e12563. PMID: 41243691 -
Adv Sci (Weinh)
TWF2 Drives Tumor Progression and Sunitinib Resistance in Renal Cell Carcinoma through Hippo Signaling Suppression. [Abstract]2025 Sep 15:e06367. PMID: 40948085 -
Theranostics
2021 Mar 12;11(11):5387-5403. PMID: 33859753 -
Theranostics
Inhibition of SMYD2 suppresses tumor progression by down-regulating microRNA-125b and attenuates multi-drug resistance in renal cell carcinoma. [Abstract]2019 Oct 22;9(26):8377-8391. PMID: 31754403 -
Theranostics
Jujuboside A promotes Aβ clearance and ameliorates cognitive deficiency in Alzheimer's disease through activating Axl/HSP90/PPARγ pathway. [Abstract]2018 Jul 30;8(15):4262-4278. PMID: 30128052
Sunitinib Malate purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278. [Abstract]
BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of RTKs (Dovitinib at 1 µM, Gefinitib at 2.5 µM, Sunitinib at 2.5 µM and LDC1267 at 1 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.
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Sci Adv
Acute BRCAness induction and AR pathway blockage through CDK12/7/9 degradation enhances PARP inhibitor sensitivity in prostate cancer. [Abstract]Sci Adv. 2025 Apr 25;11(17):eadu0847. PMID: 40267193 -
Redox Biol
USP20 governs tyrosine kinase inhibitors resistance through ferroptosis evasion by targeting GPX4 in cancers. [Abstract]2026 May:92:104086. PMID: 41844497 -
EBioMedicine
Screening of FDA-approved drugs identifies sutent as a modulator of UCP1 expression in brown adipose tissue. [Abstract]2018 Nov:37:344-355. PMID: 30348622
Sunitinib Malate purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2018 Nov:37:344-355. [Abstract]
Sutent (Sunitinib Malate) treatment decreases lipid accumulation in adipose and liver tissues and increases UCP1 expression in brown adipose tissue. Western blot analysis of UCP1 protein expression level in mouse brown adipose.
Sunitinib Malate purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2018 Nov:37:344-355. [Abstract]
Sutent (Sunitinib Malate) treatment decreases lipid accumulation in adipose and liver tissues and increases UCP1 expression in brown adipose tissue. Representative images of immunohistochemistry stainining of UCP1 in BAT.
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Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
Cancer Lett
Preoperative neoadjuvant targeted therapy remodels intra-tumoral heterogeneity of clear-cell renal cell carcinoma and ferroptosis inhibition induces resistance progression. [Abstract]2024 Jul 1:593:216963. PMID: 38768682 -
Cancer Lett
Circular RNA circSNX6 promotes sunitinib resistance in renal cell carcinoma through the miR-1184/GPCPD1/ lysophosphatidic acid axis. [Abstract]2021 Dec 28:523:121-134. PMID: 34626691 -
Cancer Lett
Repurposing cabozantinib to GISTs: Overcoming multiple imatinib-resistant cKIT mutations including gatekeeper and activation loop mutants in GISTs preclinical models. [Abstract]2019 Apr 10:447:105-114. PMID: 30684595 -
Cell Death Dis
DEPDC1 as a metabolic target regulates glycolysis in renal cell carcinoma through AKT/mTOR/HIF1α pathway. [Abstract]2024 Jul 27;15(7):533. PMID: 39068164 -
J Pharm Anal
A robust luminescent assay for screening alkyladenine DNA glycosylase inhibitors to overcome DNA repair and temozolomide drug resistance. [Abstract]2023 May;13(5):514-522. PMID: 37305785
Sunitinib Malate purchased from MedChemExpress. Usage Cited in: J Pharm Anal. 2023 May;13(5):514-522. [Abstract]
Sunitinib (0-100 μM; 72 h) induces significant cell death in T98G cells.
Sunitinib Malate purchased from MedChemExpress. Usage Cited in: J Pharm Anal. 2023 May;13(5):514-522. [Abstract]
Sunitinib (3 μM; 24 h) increases the expression of γ-H2Ax and Temozolomide (TMZ; 10 μM; 24 h) increases the induction of Sunitinib, in T98G cells.
Sunitinib Malate purchased from MedChemExpress. Usage Cited in: J Pharm Anal. 2023 May;13(5):514-522. [Abstract]
Sunitinib (3 μM; 24 h) increases the expression of γ-H2Ax and Temozolomide (TMZ; 10 μM; 24 h) increases the induction of Sunitinib, in T98G cells.
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Acta Pharmacol Sin
Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]2021 Jan;42(1):108-114. PMID: 32398685 -
EMBO J
Inhibition of Syk promotes chemical reprogramming of fibroblasts via metabolic rewiring and H2 S production. [Abstract]2021 Jun 1;40(11):e106771. PMID: 33909912 -
ACS Appl Mater Interfaces
Tumor Supplying Artery Injection of Liposome@Sunitinib Could Effectively Inhibit the Progression of Kidney Tumor. [Abstract]2024 Apr 24;16(16):20202-20211. PMID: 38624141 -
Chemosphere
The influence of sunitinib and sorafenib, two tyrosine kinase inhibitors, on development and thyroid system in zebrafish larvae. [Abstract]2022 Dec;308(Pt 2):136354. PMID: 36087734 -
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Biomed Pharmacother
Unravelling the cardioprotective effects of calcitriol in Sunitinib-induced toxicity: A comprehensive in silico and in vitro study. [Abstract]2025 May 14:188:118137. PMID: 40373630 -
Biomed Pharmacother
Inhibition of the PI3K/AKT signaling pathway contributes to the anti-renal cell carcinoma effects of deoxyelephantopin. [Abstract]2025 May 8:187:118136. PMID: 40344699 -
J Transl Med
Papillary thyroid cancer organoids harboring BRAFV600E mutation reveal potentially beneficial effects of BRAF inhibitor-based combination therapies. [Abstract]2023 Jan 9;21(1):9. PMID: 36624452 -
Arch Toxicol
Upregulation of phosphoinositide 3-kinase prevents sunitinib-induced cardiotoxicity in vitro and in vivo. [Abstract]2019 Jun;93(6):1697-1712. PMID: 31025080 -
Clin Transl Med
SHP2 inhibition and adjuvant therapy synergistically target KIT-mutant GISTs via ERK1/2-regulated GSK3β/cyclin D1 pathway. [Abstract]2025 Feb;15(2):e70231. PMID: 39981588 -
Br J Cancer
PDZK1 confers sensitivity to sunitinib in clear cell renal cell carcinoma by suppressing the PDGFR-β pathway. [Abstract]2024 Jul;131(2):347-360. PMID: 38822145 -
J Med Chem
Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)- N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors. [Abstract]2019 Jul 11;62(13):6083-6101. PMID: 31250638 -
J Med Chem
Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kinase. [Abstract]2016 Sep 22;59(18):8456-72. PMID: 27545040
Sunitinib Malate purchased from MedChemExpress. Usage Cited in: J Med Chem. 2016 Sep 22;59(18):8456-72. [Abstract]
Effect of compounds 1 (Imatinib), 2 (Sunitinib), and 35 on cKIT mediated signaling pathways in GIST-T1 and GIST-5R cancer cell lines.
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Biochem Pharmacol
Protective effects of artesunate on the neurovascular unit by regulating PDGFRβ signaling in experimental cerebral malaria. [Abstract]2025 Jun 3:117023. PMID: 40473225 -
Virulence
Adaptor complex-mediated trafficking of Newcastle disease virus fusion protein is regulated by the YLMY motif of its cytoplasmic tail. [Abstract]2022 Dec;13(1):1849-1867. PMID: 36258290 -
Biomacromolecules
Toolbox of Biodegradable Dendritic (Poly glycerol sulfate)-SS-poly(ester) Micelles for Cancer Treatment: Stability, Drug Release, and Tumor Targeting. [Abstract]2021 Jun 14;22(6):2625-2640. PMID: 34076415 -
Commun Biol
TGFBI promotes liver fibrosis through remodeling the profibrotic microenvironment by a positive feedback regulatory loop. [Abstract]2026 Feb 3;9(1):355. PMID: 41634371 -
Stem Cell Reports
Inhibition of Farnesyltransferase Potentiates NOTCH-Targeted Therapy against Glioblastoma Stem Cells. [Abstract]2017 Dec 12;9(6):1948-1960. PMID: 29198824 -
Front Pharmacol
2021 Mar 8;12:644342. PMID: 33790797 -
Front Pharmacol
Sodium-Glucose CoTransporter-2 Inhibitor Empagliflozin Ameliorates Sunitinib-Induced Cardiac Dysfunction via Regulation of AMPK-mTOR Signaling Pathway-Mediated Autophagy. [Abstract]2021 Apr 29:12:664181. PMID: 33995090 -
Eur J Pharm Sci
Design, synthesis, formulation, and bioevaluation of ZZP-2, a FLT3-ITD inhibitor for the treatment of acute myeloid leukemia. [Abstract]2026 Mar 1:218:107440. PMID: 41520929 -
Int Immunopharmacol
Modulating the tumor immune microenvironment with sunitinib malate supports the rationale for combined treatment with immunotherapy. [Abstract]2020 Apr;81:106227. PMID: 32078941 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Mol Oncol
Ovarian cancer relies on the PDGFRβ-fibronectin axis for tumorsphere formation and metastatic spread. [Abstract]2024 Jan;18(1):136-155. PMID: 38010623 -
Cancers (Basel)
Physiological Cell Culture Media Tune Mitochondrial Bioenergetics and Drug Sensitivity in Cancer Cell Models. [Abstract]2022 Aug 13;14(16):3917. PMID: 36010911 -
J Cell Mol Med
MATN1-AS1 Promotes Tumour Metastasis and Sunitinib Resistance via E2F2 in Clear Cell Renal Cell Carcinoma. [Abstract]2025 Feb;29(4):e70428. PMID: 39999286 -
Ther Adv Med Oncol
Axitinib overcomes multiple imatinib resistant cKIT mutations including the gatekeeper mutation T670I in gastrointestinal stromal tumors. [Abstract]2019 May 17:11:1758835919849757. PMID: 31205508 -
iScience
Decoding sunitinib resistance in ccRCC: Metabolic-reprogramming-induced ABAT and GABAergic system shifts. [Abstract]2024 Jun 28;27(7):110415. PMID: 39100925 -
J Biol Chem
2026 Jun;302(6):111461. PMID: 41999888 -
Sci Rep
2026 Feb 6;16(1):7619. PMID: 41651965 -
Sci Rep
Dendrobium officinale Kimura & Migo polysaccharide ameliorates skin photoaging by promoting angiogenesis. [Abstract]2025 Aug 17;15(1):30048. PMID: 40820014 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Cell Signal
TAF1D promotes tumorigenesis and metastasis by activating PI3K/AKT/mTOR signaling in clear cell renal cell carcinoma. [Abstract]2024 Sep 20:111425. PMID: 39307376 -
Heliyon
Integrated genomic and proteomic analyses identify PYGL as a novel experimental therapeutic target for clear cell renal cell carcinoma. [Abstract]2024 Mar 16;10(6):e28295. PMID: 38545181 -
Biotechnol Bioeng
An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]2021 Dec;118(12):4687-4698. PMID: 34478150 -
Exp Cell Res
Fbxo45 promotes cell viability, invasion and sunitinib resistance of clear cell renal cell carcinoma by targeting Erbin. [Abstract]2025 Nov 22;454(2):114839. PMID: 41285235 -
Food Chem Toxicol
Berberine attenuates sunitinib-induced cardiac dysfunction by normalizing calcium regulation disorder via SGK1 activation. [Abstract]2023 May:175:113743. PMID: 36972840 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
Eur J Med Res
SAP30 promotes clear cell renal cell carcinoma proliferation and inhibits apoptosis through the MT1G axis. [Abstract]2025 Apr 18;30(1):306. PMID: 40247376 -
Hum Cell
Sunitinib-resistant renal cell carcinoma cell-derived exosomes promote facilitation of tumor progression via secretion of the lncRNA SNHG16. [Abstract]2025 May 13;38(4):100. PMID: 40358820 -
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R Soc Open Sci
Synergistic anticancer activity of resveratrol-loaded polymeric nanoparticles and sunitinib in colorectal cancer treatment. [Abstract]2025 Apr 23;12(4):241817. PMID: 40271141 -
J Chromatogr B Analyt Technol Biomed Life Sci
Simultaneous determination of 11 oral targeted antineoplastic drugs and 2 active metabolites by LC-MS/MS in human plasma and its application to therapeutic drug monitoring in cancer patients. [Abstract]2024 Apr 15:1237:124100. PMID: 38547701 -
Toxicol In Vitro
Activation of inflammasomes by tyrosine kinase inhibitors of vascular endothelial growth factor receptor: Implications for VEGFR TKIs-induced immune related adverse events. [Abstract]2021 Mar;71:105063. PMID: 33271325 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
Acta Oncol
Hedgehog inhibitors exert anti-proliferation effects and synergistically interact with trastuzumab in HER2-positive gastric cancer models. [Abstract]2025 May 27:64:715-728. PMID: 40426308 -
Biochem Biophys Res Commun
Tyrosine kinase inhibitors induce cardiotoxicity by causing Ca2+ overload through the inhibition of phosphoinositide 3-kinase activity. [Abstract]2025 May 15:771:152027. PMID: 40403685 -
Biochem Biophys Res Commun
Swimming training attenuates doxorubicin induced cardiomyopathy by targeting the mir-17-3p/KEAP1/NRF2 axis. [Abstract]2024 Aug 19:739:150568. PMID: 39178797 -
Biochem Biophys Res Commun
2024 Feb 26:698:149546. PMID: 38266314 -
Biol Pharm Bull
Evaluation of Drug-Induced Kidney Injury by Primary Culture of Rat Kidney Tissue Slices Using Oxygen-Permeable Polyolefin Plate with Low Drug Adsorption. [Abstract]2026;49(1):122-129. PMID: 41565252 -
Mol Clin Oncol
Exploring the anticancer potential of hydrogen sulfide and BAY‑876 on clear cell renal cell carcinoma cells: Uncovering novel mutations in VHL and KDR genes among ccRCC patients. [Abstract]2024 Jan 18;20(3):21. PMID: 38332991 -
Int J Clin Exp Pathol
SOX9 was involved in TKIs resistance in renal cell carcinoma via Raf/MEK/ERK signaling pathway. [Abstract]2015 Apr 1;8(4):3871-81. PMID: 26097571
Sunitinib Malate purchased from MedChemExpress. Usage Cited in: Int J Clin Exp Pathol. 2015 Apr 1;8(4):3871-81. [Abstract]
The relationship between SOX9 and Raf/MEK/ERK signaling pathway. Co-treatment of si-SOX9-1 and Sorafenib (10uM, 15uM)/Sunitinib (2 uM, 3 uM) significantly decreases expression of MEK1 and its phosphorylated protein (p-MEK1/2, p-ERK1/2) as assayed by Western blot (with GAPDH as internal control).
Sunitinib Malate purchased from MedChemExpress. Usage Cited in: Int J Clin Exp Pathol. 2015 Apr 1;8(4):3871-81. [Abstract]
The relationship between SOX9 and Raf/MEK/ERK signaling pathway. Co-treatment of si-SOX9-1 and Sorafenib (10uM, 15uM)/Sunitinib (2 uM, 3 uM) significantly decreases expression of MEK1 and its phosphorylated protein (p-MEK1/2, p-ERK1/2) as assayed by RT-PCR (with β-actin as internal control).
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bioRxiv
The mammalian Ire1 inhibitor, 4μ8C, exhibits broad anti- Aspergillus activity in vitro and in a treatment model of fungal keratitis. [Abstract]2024 Aug 8:2024.08.08.607189. PMID: 39149375 -
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bioRxiv
Acute BRCAness Induction and AR Signaling Blockage through CDK12/7/9 Degradation Enhances PARP Inhibitor Sensitivity in Prostate Cancer. [Abstract]2024 Jul 10:2024.07.09.602803. PMID: 39026842 -
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Methods Mol Biol
Co-Delivery Polymeric Poly(Lactic-Co-Glycolic Acid) (PLGA) Nanoparticles to Target Cancer Stem-Like Cells. [Abstract]2024:2777:191-204. PMID: 38478345 -
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Oncotarget
Discovery of a highly selective KIT kinase primary V559D mutant inhibitor for gastrointestinal stromal tumors (GISTs). [Abstract]2017 Nov 15;8(67):111110-111118. PMID: 29340041
Sunitinib Malate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Nov 15;8(67):111110-111118. [Abstract]
In cell EC50 determination of CHMFL-KIT-031 with parental Colo320DM (KIT wt) and KIT V559D overexpressed Colo320DM cells.
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Oncotarget
The addition of abemaciclib to sunitinib induces regression of renal cell carcinoma xenograft tumors. [Abstract]2017 Jul 27;8(56):95116-95134. PMID: 29221116
Sunitinib Malate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134. [Abstract]
Abemaciclib causes increased PARP cleavage in RCC. In 786-O cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with Sunitinib.
Sunitinib Malate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134. [Abstract]
Abemaciclib causes increased PARP cleavage in RCC. In Caki-1 cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with Sunitinib.
Solvent & Solubility
DMSO : ≥ 15 mg/mL (28.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 12.5 mg/mL (23.47 mM; ultrasonic and adjust pH to 3 with HCl)
H2O : 12.5 mg/mL (23.47 mM; ultrasonic and adjust pH to 3 with HCl)
H2O : 3.33 mg/mL (6.25 mM; ultrasonic and warming and heat to 60°C)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: The maximum solubility in 100 mM Citrate buffer
Solubility: 10 mg/mL (18.78 mM); Suspended solution; Need ultrasonic and adjust pH to 5 with HCl
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Biochemical assays to determine the activity of Sunitinib against different protein kinases are performed. Ki values for SU11248 against Flk-1, PDGFRβ, and FGFR1 are determined using glutathione S-transferase-fusion proteins containing the complete cytoplasmic domain of the RTK. Cellular assays to directly determine the ability of SU11248 to inhibit ligand-dependent RTK phosphorylation or cell proliferation and mitogenic responses are performed using serum-starved cells stimulated with 40 ng/mL VEGF165 (Flk-1/KDR), 0.5 μg/mL basic FGF (FGFR), or 50 ng/mL PDGF-AA (PDGFRα) or PDGF-BB (PDGFRβ)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
RS4;11 and MV4;11 cell lines are starved overnight in medium containing 0.1% FBS prior to addition of SU11248 (1 nM, 5 nM, 10 nM, 25 nM, 75 nM, 100 nM, 250 nM, 500 nM) and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay in triplicate for each condition, as described by the manufacturer. Trypan blue cell viability assays are performed in parallel and yielded similar results[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Female nu/nu mice (8-12 weeks old, 25 g) are used. Briefly, 3-5×106 tumor cells are implanted s.c. into the hind flank region of mice on day 0. Daily treatment of tumor-bearing mice with oral administration of SU11248 as a carboxymethyl cellulose suspension or as a citrate buffered (pH 3.5) solution is initiated once the tumors reached the indicated average size. Tumor growth is evaluated based on twice-weekly measurement of tumor volume. Typically, studies are terminated when tumors in vehicle-treated animals reach an average size of 1000 mm3 or when the tumors are judged to adversely effect the well being of the animals.
Rats[4]
Forty female Sprague-Dawley rats (200-230 g) are used. Each group consists of 5-10 animals fed ad libitum. 1×104 Walker 256 cells are injected into the left abdominal mammary fat pad, under gas anesthesia (2% isoflurane). Rats are weighed daily and given Sunitinib malate (30 mg/kg) and/or Fingolimod (5 mg/kg) in olive oil by gavage. The tumors are measured with calipers. The animals are anesthetized and killed by an intracardiac injection of ketamine (50 mg/mL) before tumor ulceration. Rats are dissected to detect pulmonary, liver, kidney, or intestinal metastasis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[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 [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / H2O / H2O / DMSO | 1 mM | 1.8777 mL | 9.3886 mL | 18.7772 mL | 46.9431 mL |
| 5 mM | 0.3755 mL | 1.8777 mL | 3.7554 mL | 9.3886 mL | |
| H2O / H2O / DMSO | 10 mM | 0.1878 mL | 0.9389 mL | 1.8777 mL | 4.6943 mL |
| 15 mM | 0.1252 mL | 0.6259 mL | 1.2518 mL | 3.1295 mL | |
| 20 mM | 0.0939 mL | 0.4694 mL | 0.9389 mL | 2.3472 mL | |
| DMSO | 25 mM | 0.0751 mL | 0.3755 mL | 0.7511 mL | 1.8777 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.