Regorafenib

Regorafenib

• CAS Number: 755037-03-7
• UNSPSC Description: 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].
• Target Antigen: 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)|H2O : < 0.1 mg/mL
• 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 Weight: 482.82
• 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)
• Clinical Information: Launched