CAS |
755037-03-7 |
Chinese Name |
瑞戈非尼 |
English Name |
Regorafenib |
Synonym |
Fluoro-Sorafenib;瑞格非尼;BAY 73-4506 |
Purity |
HPLC≥98% |
Unit |
Bottle |
Molecular Formula |
C21H15ClF4N4O3 |
Molecular Weight |
482.82 |
Appearance |
White to light red solid |
Storage |
Powder : -20℃, 2 years;In solvent(mother liquid): -20℃, 1 month; -80℃, 6 months |
Solubility |
Soluble in DMSO≥5mg/ml |
MDL |
MFCD16038047 |
EC |
EINECS 815-051-1 |
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 |
Description |
Regorafenib is a multi-targeted receptor tyrosine kinase inhibitor that inhibits VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1. |
Target Point |
VEGFR |
Passage |
Angiogenesis;Protein Tyrosine Kinase/RTK |
IC50 |
VEGFR2:4.2 nM ; PDGFRβ:22 nM ; Raf-1:2.5 nM [1-5] |
Data Literature Source |
[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-Sorafenib (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 Trifluridine/Tipiracil and Regorafenib in Human Colorectal Cancer Cells. Int J Mol Sci. 2018 Sep 25;19(10). pii: E2915. |
Specification |
10mg 10mM*1mL in DMSO 50mg 100mg |