Regorafenib

• 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].

• 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 :

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