Regorafenib CAS: 755037-03-7

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Regorafenib CAS: 755037-03-7

Regorafenib CAS: 755037-03-7 Basic information

Regorafenib CAS: 755037-03-7 Chemical Properties

Regorafenib Basic information

Product Name:Regorafenib
Synonyms:Regorafenib;BAY 73-4506;4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide;BAY 73-4506(Regorafenib);4-(4-(3-(4-chloro-3-(trifluoroMethyl)phenyl)ureido)-3-fluorophenoxy)-N-MethylpicolinaMide;4-[4-({[4-chioro-3-(trifluoroMethyl)phenyl]carbaMoyl}aMino)-3-fluorophenoxy]-pyridine-2-carboxylic acid MethylaMide;REGORAFENIB BAY 73-4506 BAYER HEALTHCARE (SEE ALSO COLORECTAL, LUNG, STOMACH) PHASE II(REGORAFENIB) PHARMACEUTICALS (888) 842-2937WAYNE, NJ;Regorafenib (BAY 73-4506)
CAS:755037-03-7
MF:C21H15ClF4N4O3
MW:482.82
EINECS:815-051-1
Regorafenib Chemical Properties
Melting point 206.0 to 210.0 °C
Boiling point 513.4±50.0 °C(Predicted)
density 1.491±0.06 g/cm3(Predicted)
form White powder.
pka12.04±0.70(Predicted)

Product name

Regorafenib

 

CAS No.

 

755037-03-7

 

Batch No

 

180418

 

Date in produced

 

2018.04.18

 

Date submitted

 

2018.04.19

 

Quality standard

 

Eterprises standards

 

Storage conditions

 

Ambient Temperature

Item

Requirement

Results

Description

off-white to light pink powder

Conforms

Identification

 

HPLC

 

Conforms

Assay(HPLC)

99.0%

 

99.87%

Single impurity

0.10%

0.06%

 

Moisture

0.50%

 

0.04%

Residue on ignition

0.10%

 

0.02%

Melting point

205-210°C

206.7-208.5°C

 

 

 

 

Residual Solvents

MeOH£0.3%

ND

EtOH£0.5%

0.08%

Acetone£0.3%

0.11%

THF£0.1%

 

ND

 

Heavy metal

 

£10ppm

 

Conforms

 

Solubility

 

Soluble in DMSO and THF slightly soluble in MeOH, insoluble in H2O

Soluble in DMSO and THF slightly soluble in MeOH, insoluble in H2O

 

Conclusion

 

Conform to the Enterprise Standards

Regorafenib Usage And Synthesis
UsesIt inhibits PDGFR tyrosine kinase with IC50=83nM. It is useful for the treatment of inflammation and as an anti-proliferative agent.
UsesBAY 73-4506 (Regorafenib) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf.
UsesRegorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively


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