Regorafenib Hydrochloride - CAS 835621-07-3
Catalog number: B0084-459775
Category: Inhibitor
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Molecular Formula:
C21H16Cl2F4N4O3
Molecular Weight:
519.28
COA:
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Targets:
VEGFR
Description:
Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1.
Purity:
>98%
Synonyms:
BAY73-4506 hydrochloride
MSDS:
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InChIKey:
ACSWJKPZXNIVMY-UHFFFAOYSA-N
InChI:
InChI=1S/C21H15ClF4N4O3.ClH/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26;/h2-10H,1H3,(H,27,31)(H2,29,30,32);1H
Canonical SMILES:
CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F.Cl
1.Sorafenib/regorafenib and phosphatidyl inositol 3 kinase/thymoma viral proto-oncogene inhibition interact to kill tumor cells.
Sajithlal GB1, Hamed HA, Cruickshanks N, Booth L, Tavallai S, Syed J, Grant S, Poklepovic A, Dent P. Mol Pharmacol. 2013 Oct;84(4):562-71. doi: 10.1124/mol.113.088005. Epub 2013 Jul 22.
The present studies were undertaken to determine whether the multikinase inhibitors sorafenib/regorafenib cooperated with clinically relevant , phosphatidyl inositol 3 kinase (PI3K)-thymoma viral proto-oncogene (AKT) inhibitors to kill tumor cells. In liver, colorectal, lung, breast, kidney, and brain cancer cells, at clinically achievable doses, sorafenib/regorafenib and the PI3K inhibitor acetic acid (1S,4E,10R,11R,13S,14R)-[4-diallylaminomethylene-6-hydroxy-1-methoxymethyl-10,13-dimethyl-3,7,17-trioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester (PX-866) cooperated in a greater than additive fashion to kill tumor cells. Cells lacking phosphatase and tensin homolog were as sensitive to the drug combination as cells expressing the protein. Similar data were obtained using the AKT inhibitors perifosine and 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f] [1,6]naphthyridin-3(2H)-one hydrochloride (MK2206).
2.Modulation of Regorafenib effects on HCC cell lines by epidermal growth factor.
D'Alessandro R1, Refolo MG, Lippolis C, Carella N, Messa C, Cavallini A, Carr BI. Cancer Chemother Pharmacol. 2015 Jun;75(6):1237-45. doi: 10.1007/s00280-015-2751-6. Epub 2015 Apr 24.
PURPOSE: Blood platelet numbers are correlated to growth and aggressiveness of several tumor types, including hepatocellular carcinoma (HCC). We previously found that platelet lysates (hPLs) also stimulated growth and migration, and antagonized the growth-inhibitory and apoptotic effects of both Sorafenib and Regorafenib, two multikinase inhibitors, on three HCC cell lines. In this study, in vitro function of human epidermal growth factor (EGF) with and without Sorafenib or Regorafenib was investigated.
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CAS 835621-07-3 Regorafenib Hydrochloride

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