Regorafenib
Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity[1].
Product Specifications
CAS Number
[755037-03-7]
Product Name Alternative
BAY 73-4506
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Autophagy; c-Kit; FGFR; PDGFR; Raf; RET; Tie; VEGFR
Type
Reference compound
Related Pathways
Autophagy; MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/Regorafenib.html
Purity
99.93
Solubility
DMSO : 125 mg/mL (ultrasonic)
Smiles
O=C(NC1=CC=C(C(C(F)(F)F)=C1)Cl)NC2=CC=C(OC3=CC(C(NC)=O)=NC=C3)C=C2F
Molecular Formula
C21H15ClF4N4O3
Molecular Weight
482.82
Precautions
H302, H315, H319, H335
References & Citations
[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.|[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.|[3]Carr BI, et al. Fluoro-Bay 43-9006 (Regorafenib) effects on hepatoma cells: growth inhibition, quiescence, and recovery. J Cell Physiol, 2013, 228 (2), 292-297.|[4]Wagner J, et al. Anti-tumor effects of ONC201 in combination with VEGF-inhibitors significantly impacts colorectal cancer growth and survival in vivo through complementary non-overlapping mechanisms. J Exp Clin Cancer Res. 2018 Jan 22;37 (1) :11.|[5]Matsuoka K, et al. Effective Sequential Combined Chemotherapy with Tipiracil and Regorafenib in Human Colorectal Cancer Cells. Int J Mol Sci. 2018 Sep 25;19 (10) . pii: E2915.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
B-Raf; C-Raf; PDGFRβ; Tie2; VEGFR1/Flt-1; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4
Citation 01
ACS Omega. 2024 Jul 23;9 (31) :33574-33593.|ACS Omega. 2025 Oct 29;10 (44) :52562–52575.|Acta Pharmacol Sin. 2021 Jan;42 (1) :108-114.|Adv Healthc Mater. 2023 Jul;12 (19) :e2203120.|Adv Sci (Weinh) . 2023 Aug;10 (22) :e2206798.|Adv Sci (Weinh) . 2024 Jul 9:e2402327.|Am J Dig Dis (Madison) . 2015;2 (2) :95-99.|Anticancer Drugs. 2025 Oct 16.|Autophagy. 2020 Jan;16 (1) :106-122. |Autophagy. 2025 Jul;21 (7) :1523-1543.|Biochem Biophys Res Commun. 2024 May 21:709:149812.|Biochem Biophys Res Commun. 2025 Dec 15:792:152981.|Biochem Pharmacol. 2025 Jul 18:241:117183.|Bioengineering (Basel) . 2025 Oct 19;12 (10) :1121.|Biol Pharm Bull. 2015;38 (4) :582-6. |Biomaterials. 2022 Oct:289:121800.|Biomed Pharmacother. 2022 Sep:153:113540.|bioRxiv. 2024 Aug 6:2024.03.21.586169.|bioRxiv. 2024 June 12.|bioRxiv. 2025 Jul 12:2025.07.08.663754.|BMC Cancer. 2024 Dec 20;24 (1) :1562.|Br J Cancer. 2017 Sep 26;117 (7) :974-983.|Cancer Biomark. 2025 Oct;42 (10) :18758592251390145.|Cancer Diagn Progn. 2023 Nov 3;3 (6) :655-659.|Cancer Discov. 2019 Dec;9 (12) :1686-1695.|Cancer Discov. 2021 Jul;11 (7) :1716-1735.|Cancer Lett. 2022 Jan 1:524:161-171.|Cancer Nanotechnol. 2023 May 9.|Cell Death Dis. 2020 Nov 15;11 (11) :982.|Cell Physiol Biochem. 2016;38 (1) :160-72. |Cell Rep Med. 2025 Apr 2:102053.|Cell Rep. 2025 May 6;44 (5) :115681.|Cell Res. 2020 Sep;30 (9) :779-793. |Eur J Drug Metab Pharmacokinet. 2021 Sep;46 (5) :625-635.|Eur J Pharmacol. 2023 Oct 15:957:175986.|Exp Cell Res. 2020 Aug 1;393 (1) :112054.|Exp Cell Res. 2024 Mar 1;436 (1) :113956.|Exp Hematol Oncol. 2016 Jul 29:5:22.|Fundam Clin Pharmacol. 2021 Oct;35 (5) :919-929.|Harvard Medical School LINCS LIBRARY|Hereditas. 2025 Jul 31;162 (1) :148.|Hong Kong Polytechnic University. 2025.|Int J Biol Macromol. 2025 Sep 7;328 (Pt 1) :147514.|Int J Mol Med. 2020 Feb;45 (2) :461-474.|Int J Mol Med. 2022 Apr;49 (4) :51.|Int J Mol Sci. 2018 Sep 25;19 (10) . pii: E2915. |Int J Mol Sci. 2022 Sep 14;23 (18) :10677.|Int J Mol Sci. 2023 Dec 18;24 (24) :17610.|J Biotechnol. 2025 Nov 12:410:1-9.|J Chromatogr B Analyt Technol Biomed Life Sci. 2017 Sep 1:1061-1062:220-224.|J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Apr 15:1237:124100.|J Clin Transl Hepatol. 2025 Jan 28;13 (1) :15-24.|J Exp Clin Cancer Res. 2018 Jan 22;37 (1) :11. |J Exp Clin Cancer Res. 2024 Jul 11;43 (1) :192.|J Extracell Vesicles. 2024 Jul;13 (7) :e12468.|J Med Chem. 2015 Apr 9;58 (7) :2958-66. |J Pharm Sci. 2023 Sep;112 (9) :2581-2590.|J Transl Med. 2024 Aug 28;22 (1) :792.|J Transl Med. 2024 Dec 3;22 (1) :1095.|J Transl Med. 2024 May 30;22 (1) :517.|Leukemia. 2021 Oct;35 (10) :2827-2839.|Mol Carcinog. 2025 Jul 24.|Neoplasia. 2023 May:39:100897.|NPJ Precis Oncol. 2025 May 27;9 (1) :156.|Oncol Rep. 2018 Aug;40 (2) :635-646. |Oral Oncol. 2025 Mar:162:107222.|Patent. US20210379032A1.|Patent. US20230101335A1.|Photodiagnosis Photodyn Ther. 2024 Aug 22:104319.|Phytochemistry. 2022 Sep:201:113292.|PLoS One. 2024 Nov 1;19 (11) :e0308647.|PLoS One. 2024 Oct 16;19 (10) :e0312173.|Research Square Preprint. 2024 Feb 8.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Technical University of Munich. 24.01.2018.|Ther Adv Med Oncol. 2019 May 17:11:1758835919849757.|Toxicol Appl Pharmacol. 2024 Jul 25:117042.|University of Otago. 2025 Oct 7.|University of Sao Paulo school of medicine, 2018 Oct.|Viruses. 2019 Apr 25;11 (4) :385.|Xenobiotica. 2018 Oct;48 (10) :1059-1071. |bioRxiv. 2025 Nov 20:2025.11.20.689490.|Hong Kong Polytechnic University. 2025.
Available Sizes
Curated Selection
Explore Other Products
Discover premium biology products from our extensive collection of 20M+ items
H1000-50B-ML550 100 µL
HA-1 (HLA-HA1, HMHA1, KIAA0223, Minor Histocompatibility Antigen HA-1, mHag HA-1, Minor Histocompatibility Protein HA-1) (MaxLight 550) discontinued
Ask
View Details 