Regorafenib Hydrochloride
Based on 96 publication(s) in Google Scholar
Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.09%
- CAS No.: 835621-07-3
- Formula: C21H16Cl2F4N4O3
- Molecular Weight:519.28
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) Regorafenib Hydrochloride
More- Cancer Cell. 2026 Mar 9;44(3):658-675.e12. [Abstract]
- Cell Res. 2020 Sep;30(9):779-793. [Abstract]
- Cancer Discov. 2021 Jul;11(7):1716-1735. [Abstract]
- Cancer Discov. 2019 Dec;9(12):1686-1695. [Abstract]
- J Extracell Vesicles. 2024 Jul;13(7):e12468. [Abstract]
- Autophagy. 2025 Jul;21(7):1523-1543. [Abstract]
- Autophagy. 2020 Jan;16(1):106-122. [Abstract]
- Exp Hematol Oncol. 2016 Jul 29:5:22. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Acta Pharm Sin B. 2026 Jun 18.
- Acta Pharm Sin B. 2026 Apr 24.
- J Exp Clin Cancer Res. 2024 Jul 11;43(1):192. [Abstract]
- J Exp Clin Cancer Res. 2018 Jan 22;37(1):11. [Abstract]
- Adv Sci (Weinh). 2026 Feb 3:e16660. [Abstract]
- Adv Sci (Weinh). 2024 Jul 9:e2402327. [Abstract]
- Adv Sci (Weinh). 2023 Aug;10(22):e2206798. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- Biomaterials. 2022 Oct:289:121800. [Abstract]
- Cell Death Dis. 2020 Nov 15;11(11):982. [Abstract]
- Cancer Lett. 2022 Jan 1:524:161-171. [Abstract]
- Adv Healthc Mater. 2023 Jul;12(19):e2203120. [Abstract]
- Acta Pharmacol Sin. 2021 Jan;42(1):108-114. [Abstract]
- NPJ Precis Oncol. 2025 May 27;9(1):156. [Abstract]
- J Transl Med. 2024 Dec 3;22(1):1095. [Abstract]
- J Transl Med. 2024 Aug 28;22(1):792. [Abstract]
- J Transl Med. 2024 May 30;22(1):517. [Abstract]
- Leukemia. 2021 Oct;35(10):2827-2839. [Abstract]
- Int J Biol Macromol. 2025 Sep 7;328(Pt 1):147514. [Abstract]
- Int J Mol Med. 2022 Apr;49(4):51. [Abstract]
- Int J Mol Med. 2020 Feb;45(2):461-474. [Abstract]
- Phytother Res. 2026 Apr 29. [Abstract]
- ACS Appl Mater Interfaces. 2026 Apr 1;18(12):17602-17615. [Abstract]
- Br J Cancer. 2017 Sep 26;117(7):974-983. [Abstract]
- Cell Rep. 2025 May 6;44(5):115681. [Abstract]
- J Med Chem. 2015 Apr 9;58(7):2958-66. [Abstract]
- Biochem Pharmacol. 2025 Jul 18:241:117183. [Abstract]
- Cells. 2026 Feb 23;15(4):383. [Abstract]
- J Clin Transl Hepatol. 2025 Jan 28;13(1):15-24. [Abstract]
- Cancer Nanotechnol. 2023 May 9.
- Eur J Pharmacol. 2023 Oct 15:957:175986. [Abstract]
- Int J Mol Sci. 2023 Dec 18;24(24):17610. [Abstract]
- Int J Mol Sci. 2022 Sep 14;23(18):10677. [Abstract]
- Int J Mol Sci. 2018 Sep 25;19(10). pii: E2915. [Abstract]
- ACS Omega. 2025 Oct 29;10(44):52562-52575. [Abstract]
- ACS Omega. 2024 Jul 23;9(31):33574-33593. [Abstract]
- Neoplasia. 2023 May:39:100897. [Abstract]
- J Cell Mol Med. 2026 Apr;30(7):e71101. [Abstract]
- Oncol Rep. 2018 Aug;40(2):635-646. [Abstract]
- iScience. 2026 May 20;29(6):116005. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- BMC Cancer. 2024 Dec 20;24(1):1562. [Abstract]
- Ther Adv Med Oncol. 2019 May 17:11:1758835919849757. [Abstract]
- J Biotechnol. 2025 Nov 12:410:1-9. [Abstract]
- Oral Oncol. 2025 Mar:162:107222. [Abstract]
- J Pharm Sci. 2023 Sep;112(9):2581-2590. [Abstract]
- Viruses. 2019 Apr 25;11(4):385. [Abstract]
- Toxicol Appl Pharmacol. 2024 Jul 25:117042. [Abstract]
- Mol Carcinog. 2025 Jul 24. [Abstract]
- Exp Cell Res. 2024 Mar 1;436(1):113956. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Phytochemistry. 2022 Sep:201:113292. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- PLoS One. 2024 Oct 16;19(10):e0312173. [Abstract]
- Photodiagnosis Photodyn Ther. 2024 Aug 22:104319. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Cancer Manag Res. 2026 Apr 16:18:562346. [Abstract]
- Hereditas. 2025 Jul 31;162(1):148. [Abstract]
- Biochem Biophys Res Commun. 2025 Dec 15:792:152981. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Apr 15:1237:124100. [Abstract]
- Biochem Biophys Res Commun. 2024 May 21:709:149812. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2017 Sep 1:1061-1062:220-224. [Abstract]
- Cell Physiol Biochem. 2016;38(1):160-72. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- Anticancer Drugs. 2025 Oct 16. [Abstract]
- Cancer Biomark. 2025 Oct;42(10):18758592251390145. [Abstract]
- Biol Pharm Bull. 2015;38(4):582-6. [Abstract]
- Xenobiotica. 2018 Oct;48(10):1059-1071. [Abstract]
- The Medical College of Wisconsin. 2026.
- bioRxiv. 2026 Apr 15.
- chemRxiv. 2026 Apr 6.
- bioRxiv. 2025 Dec 5.
- bioRxiv. 2025 Nov 20:2025.11.20.689490. [Abstract]
- University of Otago. 2025 Oct 7.
- Hong Kong Polytechnic University. 2025.
- bioRxiv. 2025 Jul 12:2025.07.08.663754. [Abstract]
- Hong Kong Polytechnic University. 2025.
- Patent. US20230101335A1.
- bioRxiv. 2024 Aug 6:2024.03.21.586169. [Abstract]
- bioRxiv. 2024 June 12.
- Research Square Preprint. 2024 Feb 8.
- Cancer Diagn Progn. 2023 Nov 3;3(6):655-659. [Abstract]
- Biomed Pharmacother. 2022 Sep:153:113540. [Abstract]
- Patent. US20210379032A1.
- University of Sao Paulo school. 2018 Oct.
- Technical University of Munich. 24.01.2018.
- Am J Dig Dis (Madison). 2015;2(2):95-99.
Customer Validation & Images
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All VEGFR Isoforms
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Biological Activity
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VEGFR1 13 nM (IC50) |
VEGFR2 4.2 nM (IC50) |
VEGFR3 46 nM (IC50) |
PDGFRβ 22 nM (IC50) |
Braf 28 nM (IC50) |
BRafV600E 19 nM (IC50) |
Raf-1 2.5 nM (IC50) |
Regorafenib potently inhibits VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with an IC50 of 3 nM. In HAoSMCs, regorafenib inhibits PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC50 of 3 nM[1]. Regorafenib causes a concentration-dependent decrease in Hep3B cell growth, having an IC50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 835621-07-3
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Appearance Solid
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Molecular Weight 519.28
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Formula C21H16Cl2F4N4O3
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Color White to off-white
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SMILES
ClC1=C(C(F)(F)F)C=C(NC(NC2=C(F)C=C(OC3=CC=NC(C(NC)=O)=C3)C=C2)=O)C=C1.Cl
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Synonyms
BAY 73-4506 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (96)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Chemotherapy triggers immune evasion by fostering LEPR+ Kupffer cell differentiation in liver metastases. [Abstract]2026 Mar 9;44(3):658-675.e12. PMID: 41687606 -
Cell Res
s-HBEGF/SIRT1 circuit-dictated crosstalk between vascular endothelial cells and keratinocytes mediates sorafenib-induced hand-foot skin reaction that can be reversed by nicotinamide. [Abstract]2020 Sep;30(9):779-793. PMID: 32296111 -
Cancer Discov
Exploiting Allosteric Properties of RAF and MEK Inhibitors to Target Therapy-Resistant Tumors Driven by Oncogenic BRAF Signaling. [Abstract]2021 Jul;11(7):1716-1735. PMID: 33568355 -
Cancer Discov
Acquired On-Target Clinical Resistance Validates FGFR4 as a Driver of Hepatocellular Carcinoma. [Abstract]2019 Dec;9(12):1686-1695. PMID: 31575540 -
J Extracell Vesicles
Oxidative stress induces extracellular vesicle release by upregulation of HEXB to facilitate tumour growth in experimental hepatocellular carcinoma. [Abstract]2024 Jul;13(7):e12468. PMID: 38944674 -
Autophagy
Kit-mediated autophagy suppression driven by a viral oncoprotein emerges as a crucial survival mechanism in Merkel cell carcinoma. [Abstract]2025 Jul;21(7):1523-1543. PMID: 40108758 -
Autophagy
2020 Jan;16(1):106-122. PMID: 30909789 -
Exp Hematol Oncol
Effects of molecularly targeted therapies on murine thymus: highly selective mTOR inhibitors induce reversible thymic involution. [Abstract]2016 Jul 29:5:22. PMID: 27478685 -
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 -
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J Exp Clin Cancer Res
Combination of dual JAK/HDAC inhibitor with regorafenib synergistically reduces tumor growth, metastasis, and regorafenib-induced toxicity in colorectal cancer. [Abstract]2024 Jul 11;43(1):192. PMID: 38992681 -
J Exp Clin Cancer Res
Anti-tumor effects of ONC201 in combination with VEGF-inhibitors significantly impacts colorectal cancer growth and survival in vivo through complementary non-overlapping mechanisms. [Abstract]2018 Jan 22;37(1):11. PMID: 29357916 -
Adv Sci (Weinh)
2026 Feb 3:e16660. PMID: 41632021 -
Adv Sci (Weinh)
Stabilization of TGF-β Receptor 1 by a Receptor-Associated Adaptor Dictates Feedback Activation of the TGF-β Signaling Pathway to Maintain Liver Cancer Stemness and Drug Resistance. [Abstract]2024 Jul 9:e2402327. PMID: 38981014 -
Adv Sci (Weinh)
Donafenib and GSK-J4 Synergistically Induce Ferroptosis in Liver Cancer by Upregulating HMOX1 Expression. [Abstract]2023 Aug;10(22):e2206798. PMID: 37330650 -
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 -
Biomaterials
2022 Oct:289:121800. PMID: 36166893 -
Cell Death Dis
A small natural molecule CADPE kills residual colorectal cancer cells by inhibiting key transcription factors and translation initiation factors. [Abstract]2020 Nov 15;11(11):982. PMID: 33191401 -
Cancer Lett
Induction of IL-6Rα by ATF3 enhances IL-6 mediated sorafenib and regorafenib resistance in hepatocellular carcinoma. [Abstract]2022 Jan 1:524:161-171. PMID: 34687791 -
Adv Healthc Mater
A Novel Patient-Personalized Nanovector Based on Homotypic Recognition and Magnetic Hyperthermia for an Efficient Treatment of Glioblastoma Multiforme. [Abstract]2023 Jul;12(19):e2203120. PMID: 37058273 -
Acta Pharmacol Sin
Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]2021 Jan;42(1):108-114. PMID: 32398685 -
NPJ Precis Oncol
Optimized culturing yields high success rates and preserves molecular heterogeneity, enabling personalized screening for high-grade gliomas. [Abstract]2025 May 27;9(1):156. PMID: 40425813 -
J Transl Med
Doxorubicin synergizes bortezomib-induced multiple myeloma cell death by inhibiting aggresome formation and augmenting endoplasmic reticulum/Golgi stress and apoptosis. [Abstract]2024 Dec 3;22(1):1095. PMID: 39623468 -
J Transl Med
Mito-LND and (E)-Akt inhibitor-IV: novel compounds inducing endoplasmic reticulum stress and ROS accumulation against hepatocellular carcinoma. [Abstract]2024 Aug 28;22(1):792. PMID: 39198815 -
J Transl Med
CircDCAF8 promotes the progression of hepatocellular carcinoma through miR-217/NAP1L1 Axis, and induces angiogenesis and regorafenib resistance via exosome-mediated transfer. [Abstract]2024 May 30;22(1):517. PMID: 38816735 -
Leukemia
Downregulation of MTSS1 in acute myeloid leukemia is associated with a poor prognosis, chemotherapy resistance, and disease aggressiveness. [Abstract]2021 Oct;35(10):2827-2839. PMID: 33782537 -
Int J Biol Macromol
vtRNA1-1 drives regorafenib resistance by sustaining cancer stemness via impaired autophagy and altered svRNA biogenesis. [Abstract]2025 Sep 7;328(Pt 1):147514. PMID: 40925433 -
Int J Mol Med
A pre‑clinical model combining cryopreservation technique with precision‑cut slice culture method to assess the in vitro drug response of hepatocellular carcinoma. [Abstract]2022 Apr;49(4):51. PMID: 35179217 -
Int J Mol Med
MicroRNA‑15a‑5p induces pulmonary artery smooth muscle cell apoptosis in a pulmonary arterial hypertension model via the VEGF/p38/MMP‑2 signaling pathway. [Abstract]2020 Feb;45(2):461-474. PMID: 31894295 -
Phytother Res
Flavokawain A Targets CXCR4-Mediated Vasculogenic Mimicry to Reverse Hepatocellular Carcinoma Resistance to Tyrosine Kinase Inhibitors. [Abstract]2026 Apr 29. PMID: 42052746 -
ACS Appl Mater Interfaces
Chlorin e6 and Regorafenib Assemblies to Boost Photodynamic Immunotherapy through PD-L1 Downregulation and Tumor-Associated Macrophage Reprogramming. [Abstract]2026 Apr 1;18(12):17602-17615. PMID: 41855525 -
Br J Cancer
Activation of an AKT/FOXM1/STMN1 pathway drives resistance to tyrosine kinase inhibitors in lung cancer. [Abstract]2017 Sep 26;117(7):974-983. PMID: 28850563
Regorafenib Hydrochloride purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2017 Sep 26;117(7):974-983. [Abstract]
The effect of the AKT inhibitor MK2206 (10 μM) on the expression levels of phosphor-AKT, AKT, and STMN1 in TKI-pretreated NCI-H460 cells. β-actin is used as a loading control.
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Cell Rep
OTUD4 inhibits ferroptosis by stabilizing GPX4 and suppressing autophagic degradation to promote tumor progression. [Abstract]2025 May 6;44(5):115681. PMID: 40338740 -
J Med Chem
Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain. [Abstract]2015 Apr 9;58(7):2958-66. PMID: 25790278 -
Biochem Pharmacol
Pitavastatin overcomes multi-drug resistance in CRC and NSCLC by targeting the NRP1-ZFX axis. [Abstract]2025 Jul 18:241:117183. PMID: 40684995 -
Cells
A Comprehensive Adenoid Cystic Carcinoma-Derived Organoid Platform for Disease Modeling and Drug Screening Captures Interpatient Heterogeneity. [Abstract]2026 Feb 23;15(4):383. PMID: 41744826 -
J Clin Transl Hepatol
HBx Facilitates Drug Resistance in Hepatocellular Carcinoma via CD133-regulated Self-renewal of Liver Cancer Stem Cells. [Abstract]2025 Jan 28;13(1):15-24. PMID: 39801781 -
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Eur J Pharmacol
Regorafenib activates oxidative stress by inhibiting SELENOS and potentiates oxaliplatin-induced cell death in colon cancer cells. [Abstract]2023 Oct 15:957:175986. PMID: 37598924 -
Int J Mol Sci
Therapeutic Potential of Regorafenib in Cisplatin-Resistant Bladder Cancer with High Epithelial-Mesenchymal Transition and Stemness Properties. [Abstract]2023 Dec 18;24(24):17610. PMID: 38139437 -
Int J Mol Sci
Chidamide plus Tyrosine Kinase Inhibitor Remodel the Tumor Immune Microenvironment and Reduce Tumor Progression When Combined with Immune Checkpoint Inhibitor in Naïve and Anti-PD-1 Resistant CT26-Bearing Mice. [Abstract]2022 Sep 14;23(18):10677. PMID: 36142591 -
Int J Mol Sci
Effective Sequential Combined Chemotherapy with Trifluridine/Tipiracil and Regorafenib in Human Colorectal Cancer Cells. [Abstract]2018 Sep 25;19(10). pii: E2915. PMID: 30257515
Regorafenib Hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2018 Sep 25;19(10). pii: E2915. [Abstract]
Effects on the expression of phosphorylated extracellular signal-related kinase (p-ERK), ERK, thymidylate synthase (TS), and markers of cell death in SW620, HCT 116, and HT-29 cells using various Regorafenib treatment schedules.
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ACS Omega
Association Study of OATP1B3 Polymorphisms on Hepatic Uptake and Drug-Drug Interaction In Vitro. [Abstract]2025 Oct 29;10(44):52562-52575. PMID: 41244417 -
ACS Omega
Regorafenib Attenuates Osteoclasts Differentiation by Inhibiting the NF-κB, NFAT, ERK, and p38 Signaling Pathways. [Abstract]2024 Jul 23;9(31):33574-33593. PMID: 39130575 -
Neoplasia
Regorafenib induces NOX5-mediated endoplasmic reticulum stress and potentiates the anti-tumor activity of cisplatin in non-small cell lung cancer cells. [Abstract]2023 May:39:100897. PMID: 36940556
Regorafenib Hydrochloride purchased from MedChemExpress. Usage Cited in: Neoplasia. 2023 May:39:100897. [Abstract]
Regorafenib (0-40 µM; 36 h) markedly increases the expression of cleaved caspase-3, while decreases the expression of anti-apoptotic protein Bcl-2, in both H1299 and PC-9 cells.
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J Cell Mol Med
2026 Apr;30(7):e71101. PMID: 41896195 -
Oncol Rep
Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues. [Abstract]2018 Aug;40(2):635-646. PMID: 29917168 -
iScience
Phospho-JNK agonists show promising effects for the treatment of hepatocellular carcinoma. [Abstract]2026 May 20;29(6):116005. PMID: 42211113 -
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 -
BMC Cancer
Regorafenib induces DNA damage and enhances PARP inhibitor efficacy in pancreatic ductal carcinoma. [Abstract]2024 Dec 20;24(1):1562. PMID: 39707244 -
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 -
J Biotechnol
2025 Nov 12:410:1-9. PMID: 41238124 -
Oral Oncol
Application of patient derived xenograft model in personalized drug screening for chondrosarcoma of head and neck: A preclinical study. [Abstract]2025 Mar:162:107222. PMID: 39999643 -
J Pharm Sci
Monoacylglycerol lipase inhibitor JJKK048 ameliorates ABCG2 transporter-mediated regorafenib resistance induced by hypoxia in triple negative breast cancer cells. [Abstract]2023 Sep;112(9):2581-2590. PMID: 37220829 -
Viruses
Screening of an FDA-Approved Drug Library with a Two-Tier System Identifies an Entry Inhibitor of Severe Fever with Thrombocytopenia Syndrome Virus. [Abstract]2019 Apr 25;11(4):385. PMID: 31027241 -
Toxicol Appl Pharmacol
Liquidambaric acid inhibits the proliferation of hepatocellular carcinoma cells by targeting PPARα-RXRα to down-regulate fatty acid metabolism. [Abstract]2024 Jul 25:117042. PMID: 39067772 -
Mol Carcinog
2025 Jul 24. PMID: 40705959 -
Exp Cell Res
Inhibition of RhoGEF/RhoA alleviates regorafenib resistance and cancer stemness via Hippo signaling pathway in hepatocellular carcinoma. [Abstract]2024 Mar 1;436(1):113956. PMID: 38341081 -
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 -
Phytochemistry
2022 Sep:201:113292. PMID: 35780923 -
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 -
PLoS One
The correlation between cellular O-GlcNAcylation and sensitivity to O-GlcNAc inhibitor in colorectal cancer cells. [Abstract]2024 Oct 16;19(10):e0312173. PMID: 39413067 -
Photodiagnosis Photodyn Ther
Regorafenib enhances the efficacy of photodynamic therapy in hepatocellular carcinoma through MAPK signaling pathway suppression. [Abstract]2024 Aug 22:104319. PMID: 39181490 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
Cancer Manag Res
Regorafenib-Induced Stress Response Alters the Bioenergetic Profile of Osteosarcoma Cells and Modulates Gene Expression Associated with Metabolic regulation-a Potential Mechanism of Osteosarcoma Treatment-Related Adaptation. [Abstract]2026 Apr 16:18:562346. PMID: 42016157 -
Hereditas
EPHX1 enhances drug resistance to regorafenib by activating the JAK/STAT signaling pathway in hepatocellular carcinoma cell lines. [Abstract]2025 Jul 31;162(1):148. PMID: 40745342 -
Biochem Biophys Res Commun
2025 Dec 15:792:152981. PMID: 41242297 -
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 -
Biochem Biophys Res Commun
Allosteric SHP2 inhibition enhances regorafenib's effectiveness in colorectal cancer treatment. [Abstract]2024 May 21:709:149812. PMID: 38564942 -
J Chromatogr B Analyt Technol Biomed Life Sci
Investigation of the effect of plasma albumin levels on regorafenib-induced hepatotoxicity using a validated liquid chromatography-tandem mass spectrometry method. [Abstract]2017 Sep 1:1061-1062:220-224. PMID: 28750235 -
Cell Physiol Biochem
2016;38(1):160-72. PMID: 26765545 -
Eur J Drug Metab Pharmacokinet
Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
Anticancer Drugs
A genome-wide screen identified ARHGAP35 as a regulator of regorafenib resistance in liver cancer. [Abstract]2025 Oct 16. PMID: 41176659 -
Cancer Biomark
TUBB3 (βIII-tubulin) drives gastric cancer progression and poor prognosis by regulating cell cycle and invadopodia formation. [Abstract]2025 Oct;42(10):18758592251390145. PMID: 41129675 -
Biol Pharm Bull
Regorafenib is transported by the organic anion transporter 1B1 and the multidrug resistance protein 2. [Abstract]2015;38(4):582-6. PMID: 25739790 -
Xenobiotica
Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1. [Abstract]2018 Oct;48(10):1059-1071. PMID: 29034773 -
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bioRxiv
Hidden-driver inference reveals synergistic brain-penetrant therapies for medulloblastoma. [Abstract]2025 Nov 20:2025.11.20.689490. PMID: 41332625 -
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bioRxiv
2025 Jul 12:2025.07.08.663754. PMID: 40672312 -
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bioRxiv
2024 Aug 6:2024.03.21.586169. PMID: 38586030 -
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Cancer Diagn Progn
Recombinant Methioninase Lowers the Effective Dose of Regorafenib Against Colon-Cancer Cells: A Strategy for Widespread Clinical Use of a Toxic Drug. [Abstract]2023 Nov 3;3(6):655-659. PMID: 37927805 -
Biomed Pharmacother
Advantage of clinical colchicine concentration to promote sorafenib or regorafenib anti-cancer effects on hepatocellular carcinoma. [Abstract]2022 Sep:153:113540. PMID: 36076618 -
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Solvent & Solubility
DMSO : 100 mg/mL (192.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 2 mg/mL (3.85 mM); Suspended solution; Need ultrasonic
Protocol
For proliferation assays, GIST 882 and TT cells are grown in RPMI medium containing L-glutamine, and MDA-MB-231, HepG2 and A375 cells in DMEM always containing 10% hiFBS. Cells are trypsinized, plated at 5×104 cells/well in 96-well plates in complete media containing 10% FBS and grown overnight at 37°C. The next day, vehicle or regorafenib serially diluted in complete growth media to between 10 μM and 5 nM final concentrations, and 0.2% DMSO, is added and incubation is continued for 96 hr. Cell proliferation is quantified using CellTitre-GloTM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Female athymic NCr nu/nu mice, kept in accordance with Federal guidelines, are subcutaneously inoculated with 5×106 Colo-205 or MDA-MB-231 cells or implanted with 1 mm3 786-O tumor fragments. When tumors reach a volume of 100 mm3, regorafenib or vehicle control is administered orally qd×21 in the 786-O model, and qd×9 in the Colo-205 and MDA-MB-231 models, respectively, at doses of 100, 30, 10, and 3 mg/kg. Paclitaxel is administered intravenously at 10 mg/kg in ethanol/Cremophor EL®/saline (12.5%/12.5%/75%) every 2 days×5. Tumor size (volume) is estimated twice weekly (l×w2)/2, and the percentage of tumor growth inhibition (TGI) is obtained from terminal tumor weights (1-T/C×100). Mice are weighed every other day starting from the first day of treatment. The general health status of the mice is monitored daily.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Wilhelm SM, et al. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer, 2011, 129(1), 245-255. [Content Brief]
[2]. Heng DY, et al. Targeted therapy for metastatic renal cell carcinoma: current treatment and future directions. Ther Adv Med Oncol, 2010, 2(1), 39-49. [Content Brief]
[3]. Carr BI, et al. Fluoro-Sorafenib (Regorafenib) effects on hepatoma cells: growth inhibition, quiescence, and recovery. J Cell Physiol, 2013, 228(2), 292-297. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9257 mL | 9.6287 mL | 19.2574 mL | 48.1436 mL |
| 5 mM | 0.3851 mL | 1.9257 mL | 3.8515 mL | 9.6287 mL | |
| 10 mM | 0.1926 mL | 0.9629 mL | 1.9257 mL | 4.8144 mL | |
| 15 mM | 0.1284 mL | 0.6419 mL | 1.2838 mL | 3.2096 mL | |
| 20 mM | 0.0963 mL | 0.4814 mL | 0.9629 mL | 2.4072 mL | |
| 25 mM | 0.0770 mL | 0.3851 mL | 0.7703 mL | 1.9257 mL | |
| 30 mM | 0.0642 mL | 0.3210 mL | 0.6419 mL | 1.6048 mL | |
| 40 mM | 0.0481 mL | 0.2407 mL | 0.4814 mL | 1.2036 mL | |
| 50 mM | 0.0385 mL | 0.1926 mL | 0.3851 mL | 0.9629 mL | |
| 60 mM | 0.0321 mL | 0.1605 mL | 0.3210 mL | 0.8024 mL | |
| 80 mM | 0.0241 mL | 0.1204 mL | 0.2407 mL | 0.6018 mL | |
| 100 mM | 0.0193 mL | 0.0963 mL | 0.1926 mL | 0.4814 mL |
Regorafenib Hydrochloride Related Classifications
HY-13308 Related Classifications
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