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Regorafenib

Catalog No. T1792 CAS 755037-03-7

Synonyms: BAY 73-4506, Fluoro-Sorafenib

Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.

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Regorafenib, CAS 755037-03-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 30.00
10 mg	In stock	$ 47.00
25 mg	In stock	$ 73.00
50 mg	In stock	$ 97.00
100 mg	In stock	$ 147.00
200 mg	In stock	$ 195.00
500 mg	In stock	$ 326.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 99.95%

Purity: 99.87%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.
Targets&IC50	B-Raf (V600E):19 nM (cell free), c-Kit:7 nM (cell free), Raf-1:2.5 nM (cell free), VEGFR1:13 nM (cell free), RET:1.5 nM (cell free), VEGFR2:4.2 nM (cell free)
In vitro	METHODS: Human hepatocellular carcinoma cells Hep3B, PLC/PRF/5 and HepG2 were treated with Regorafenib (0-10 μM) for 72 h. Cell viability was measured by MTT. RESULTS: Regorafenib concentration-dependently decreased the viability of Hep3B cells with an IC50 of about 5 μM. PLC/PRF/5 cells were similarly sensitized to Hep3B cells. However, HepG2 cells were more sensitive, with an IC50 of approximately 1 μM. [1] METHODS: Tumor cells NIH-3T3/VEGFR2, CHO/TIE2, HAoSMC/PDGFR-β and MCF-7/FGFR were treated with Regorafenib (10-3000 nM) for 1 h. The expression levels of the target proteins were detected by Western Blot. RESULTS: Regorafenib inhibited p-VEGFR2, p-TIE2, p-PDGFR-β and p-FGFR. [2]
In vivo	METHODS: To test the antitumor activity in vivo, Regorafenib (3-100 mg/kg) was orally administered to NCr nu/nu mice bearing tumors Colo-205 or MDA-MB-231 once daily for nine days. RESULTS: Regorafenib inhibited tumor growth. In the Colo-205 model, Regorafenib at a dose of 10 mg/kg resulted in a TGI of 75% on day 14. In the MDA-MB-231 model, Regorafenib was highly effective at doses as low as 3 mg/kg, resulting in a significant TGI of 81%. [2] METHODS: To assay antitumor activity in vivo, Regorafenib (3-10 mg/kg) was administered orally to NMRI nu/nu mice harboring tumors HT-29 or MDA-MB-231 once daily for twenty-seven days. RESULTS: Regorafenib dose-dependently inhibited HT-29 and MDA-MB-231 tumor growth. [3]
Kinase Assay	In vitro assays using recombinant VEGFR2 (murine aa785–aa1367), VEGFR3 (murine aa818–aa1363), PDGFR-b (aa561–aa1106), RAF-1 (aa305–aa648) and BRAFV600E (aa409–aa765) kinase domains were performed as previously described. Initial in vitro kinase inhibition profiling was performed at a fixed 1 μM compound concentration under Millipore standard conditions [10 μM adenosine-50'- triphosphate (ATP) concentration]. Inhibitory concentration of 50% (IC50) values were determined from selected responding kinases, e.g., VEGFR1 and RET. TIE2 kinase inhibition was measured with a homogeneous time-resolved fluorescence (HTRF) assay using a recombinant fusion protein of glutathione-S-transferase, the intracellular domain of TIE2 and the peptide biotin-Ahx-EPKDDAYPLYSDFG as substrate.
Cell Research	Each cell line was seeded at 0.3×10^5 cells/2ml of DMEM containing 10% FBS in 35 mm tissue culture dishes. The cells were incubated for 24 h to allow attachment, and then the medium was replaced by fresh culture medium containing Regorafenib at increasing concentrations (1 μM, 2.5 μM, 5 μM, 7.5 μM and 10 μM). In these experimental conditions, the cells were allowed to grow for 72 or 96 h. Time-course experiments on Hep3B cells were performed with 7.5 μM of Regorafenib at short (15, 60, 180 min.), middle (24, 48, 72 and 96 h) or long times (up to seven days). When the cells were treated for long times the drug was replaced with a fresh one. Each experiment included a control with the equivalent concentration of DMSO (solvent control) as the one used for adding Regorafenib. Each experiment was performed in triplicate and repeated 3 times. Subsequent analyses were performed at specific Regorafenib concentrations and incubation times [2].
Animal Research	Female athymic NCr nu/nu mice, kept in accordance with Federal guidelines, were subcutaneously inoculated with 5×10^6 Colo-205 or MDAMB-231 cells or implanted with 1 mm^3 786-O tumor fragments. When tumors reached a volume of ~100 mm^3, regorafenib or vehicle control was administered orally qd×21 in the 786-O model, and qd×9 in the Colo-205 and MDA-MB231 models, respectively, at doses of 100, 30, 10, and 3 mg/kg. Paclitaxel was administered intravenously at 10 mg/kg in ethanol/Cremophor ELV/saline (12.5%/12.5%/75%) every 2 days×5. Tumor size (volume) was estimated twice weekly (l×w^2)/2, and the percentage of tumor growth inhibition (TGI) was obtained from terminal tumor weights (1-T/C100). Mice were weighed every other day starting from the first day of treatment. The general health status of the mice was monitored daily [1].

Synonyms	BAY 73-4506, Fluoro-Sorafenib
Molecular Weight	482.82
Formula	C21H15ClF4N4O3
CAS No.	755037-03-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90 mg/mL (186.4 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Carr BI, et al. Fluoro-Sorafenib (Regorafenib) effects on hepatoma cells: growth inhibition, quiescence, and recovery. J Cell Physiol. 2013 Feb;228(2):292-7. 2. 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 Jul 1;129(1):245-55. 3. Zopf D, et al. Pharmacologic activity and pharmacokinetics of metabolites of regorafenib in preclinical models. Cancer Med. 2016 Nov;5(11):3176-3185. 4. Duan F, Huang R, Zhang F, et al. Biphasic modulation of insulin signaling enables highly efficient hematopoietic differentiation from human pluripotent stem cells[J]. Stem cell research & therapy. 2018 Jul 27;9(1):205.

Citations

1. Huang M, Chen M, Qi M, et al. Perivascular cell‐derived extracellular vesicles stimulate colorectal cancer revascularization after withdrawal of antiangiogenic drugs. Journal of Extracellular Vesicles. 2021, 10(7): e12096. 2. Duan F, Huang R, Zhang F, et al. Biphasic modulation of insulin signaling enables highly efficient hematopoietic differentiation from human pluripotent stem cells. Stem Cell Research & Therapy. 2018 Jul 27;9(1):205 3. Wang C, Huang M, Lin Y, et al.ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy.Nature Metabolism.2023: 1-22.

Related compound libraries

This product is contained In the following compound libraries：

FDA-Approved Kinase Inhibitor Library Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library EMA Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library

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Keywords

Regorafenib 755037-03-7 Angiogenesis Apoptosis Autophagy MAPK Tyrosine Kinase/Adaptors c-RET Raf VEGFR c-Kit PDGFR HUVECs Vascular endothelial growth factor receptor Colo-205 FGFR SCFR RET NIH-3T3 antiangiogenic Antitumorigenic inhibit HAoSMCs BAY 73-4506 Platelet-derived growth factor receptor tumor Inhibitor Hep3B cell CD117 Fluoro-Sorafenib Raf kinases Fibroblast growth factor receptor 786-O inhibitor

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