Regorafenib
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 202436

CAS#: 755037-03-7

Description: Regorafenib, also known as BAY 73-4506 ; is a n orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds to and inhibits vascular endothelial growth factor receptors (VEGFRs) 2 and 3, and Ret, Kit, PDGFR and Raf kinases, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. Regorafenib demonstrated to increase the overall survival of patients with metastatic colorectal cancer and has been approved by the US FDA on September 27, 2012.


Price and Availability

Size
Price

100mg
USD 90
1g
USD 450
10g
USD 1950
100g
Ask price
Size
Price

200mg
USD 150
2g
USD 750
20g
USD 2650
Size
Price

500mg
USD 250
5g
USD 1250
50g
USD 3950

Regorafenib (99%) is in stock. The same day shipping out after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 202436
Name: Regorafenib
CAS#: 755037-03-7
Chemical Formula: C21H15ClF4N4O3
Exact Mass: 482.07688
Molecular Weight: 482.81541
Elemental Analysis: C, 52.24; H, 3.13; Cl, 7.34; F, 15.74; N, 11.60; O, 9.94


Synonym: BAY 734506; BAY734506; BAY-734506; Regorafenib. trade name: Stivarga.

IUPAC/Chemical Name: 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide

InChi Key: ZFLJHSQHILSNCM-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H27N7O/c1-2-4-15(5-3-1)24-20-18-19(23-14-22-18)26-21(27-20)25-16-6-8-17(9-7-16)28-10-12-29-13-11-28/h6-9,14-15H,1-5,10-13H2,(H3,22,23,24,25,26,27)

SMILES Code: C12=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC(NC5CCCCC5)=C1NC=N2


Technical Data

Appearance:
Off-white to light pink solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

 
 


References

1: Ravi S, Singal AK. Regorafenib: an evidence-based review of its potential in patients with advanced liver cancer. Core Evid. 2014 Jul 17;9:81-7. doi: 10.2147/CE.S48626. eCollection 2014. Review. PubMed PMID: 25114628; PubMed Central PMCID: PMC4109634.

2: Abdel-Rahman O, Fouad M. Risk of cardiovascular toxicities in patients with solid tumors treated with sunitinib, axitinib, cediranib or regorafenib: An updated systematic review and comparative meta-analysis. Crit Rev Oncol Hematol. 2014 Jul 1. pii: S1040-8428(14)00114-0. doi: 10.1016/j.critrevonc.2014.06.003. [Epub ahead of print] Review. PubMed PMID: 25028151.

3: Khan G, Moss RA, Braiteh F, Saltzman M. Proactive strategies for regorafenib in metastatic colorectal cancer: implications for optimal patient management. Cancer Manag Res. 2014 Mar 4;6:93-103. doi: 10.2147/CMAR.S52217. eCollection 2014. Review. PubMed PMID: 24623990; PubMed Central PMCID: PMC3949557.

4: De Wit M, Boers-Doets CB, Saettini A, Vermeersch K, de Juan CR, Ouwerkerk J, Raynard SS, Bazin A, Cremolini C. Prevention and management of adverse events related to regorafenib. Support Care Cancer. 2014 Mar;22(3):837-46. doi: 10.1007/s00520-013-2085-z. Epub 2013 Dec 14. Review. PubMed PMID: 24337717; PubMed Central PMCID: PMC3913844.

5: Lyseng-Williamson KA. Regorafenib: a guide to its use in advanced gastrointestinal stromal tumor (GIST) after failure of imatinib and sunitinib. BioDrugs. 2013 Oct;27(5):525-31. doi: 10.1007/s40259-013-0061-2. Review. PubMed PMID: 23975637.

6: Regorafenib (Stivarga) for metastatic colorectal cancer and GIST. Med Lett Drugs Ther. 2013 Apr 29;55(1415):e36. Review. PubMed PMID: 23836345.

7: Sirohi B, Philip DS, Shrikhande SV. Regorafenib: carving a niche in the crowded therapeutic landscape. Expert Rev Anticancer Ther. 2013 Apr;13(4):385-93. doi: 10.1586/era.13.12. Review. PubMed PMID: 23560833.

8: Davis SL, Eckhardt SG, Messersmith WA, Jimeno A. The development of regorafenib and its current and potential future role in cancer therapy. Drugs Today (Barc). 2013 Feb;49(2):105-15. doi: 10.1358/dot.2013.49.2.1930525. Review. PubMed PMID: 23462625.

9: Roman D, Whiteside R. Regorafenib: Adding to the Armamentarium for Refractory Colorectal Cancer and GIST. J Adv Pract Oncol. 2013 Mar;4(2):118-22. Review. PubMed PMID: 25031991; PubMed Central PMCID: PMC4093419.

10: Aprile G, Macerelli M, Giuliani F. Regorafenib for gastrointestinal malignancies : from preclinical data to clinical results of a novel multi-target inhibitor. BioDrugs. 2013 Jun;27(3):213-24. doi: 10.1007/s40259-013-0014-9. Review. PubMed PMID: 23435872.

11: Strumberg D, Schultheis B. Regorafenib for cancer. Expert Opin Investig Drugs. 2012 Jun;21(6):879-89. doi: 10.1517/13543784.2012.684752. Review. PubMed PMID: 22577890.