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CAS RN: 755037-03-7 | Product Number: R0142

Regorafenib

Purity: >98.0%(HPLC)

Synonyms:

Documents:

SDS | Specifications | C of A & Other Certificates | Analytical Charts

Size	Unit Price	Hyderabad	Japan*	Quantity
25MG	₹6,500.00	2	≥40
100MG	₹10,640.00	Contact Us	25

*Upon orders receipt, Hyderabad stocks will be dispatched on the same day.
*Items available in Japan warehouse will be dispatched in 10-12 working days.
*INR price is exclusive of domestic taxes applicable.
*TCI frequently reviews storage conditions to optimize them. Please note that the latest information on the storage temperature for the products is described on our website.

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General Information plus

Product Number	R0142
Purity / Analysis Method	>98.0%(HPLC)
Molecular Formula / Molecular Weight	C__2__1H__1__5ClF__4N__4O__3 = 482.82
Physical State (20 deg.C)	Solid
Storage Temperature	Frozen (<0°C)
Condition to Avoid	Heat Sensitive
CAS RN	755037-03-7
Reaxys Registry Number	14359949
PubChem Substance ID	354334233
MDL Number	MFCD16038047

Specifications & Properties plus

Specifications

Appearance	White to Light yellow to Light orange powder to crystal
Purity(HPLC)	min. 98.0 area%
Elemental analysis(Nitrogen)	11.00 to 12.20 %

Properties (reference)

Melting Point

208 °C

Safety & Regulations plus

GHS

Pictogram
Signal Word	Warning
Hazard Statements	H302 : Harmful if swallowed. H361 : Suspected of damaging fertility or the unborn child. H373 : May cause damage to organs through prolonged or repeated exposure.
Precautionary Statements	P501 : Dispose of contents/ container to an approved waste disposal plant. P260 : Do not breathe dust/ fume/ gas/ mist/ vapors/ spray. P270 : Do not eat, drink or smoke when using this product. P202 : Do not handle until all safety precautions have been read and understood. P201 : Obtain special instructions before use. P264 : Wash skin thoroughly after handling. P280 : Wear protective gloves/ protective clothing/ eye protection/ face protection. P308 + P313 : IF exposed or concerned: Get medical advice/ attention. P301 + P312 + P330 : IF SWALLOWED: Call a POISON CENTER/doctor if you feel unwell. Rinse mouth. P405 : Store locked up.

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Applications plus

Application

Regorafenib: A Multikinase Inhibitor of Tumour Angiogenesis, Oncogenesis and the Tumour Microenvironment

Regorafenib (BAY 73-4506) is a potent diphenylurea multikinase inhibitor of tumour angiogenesis (VEGFR1，VEGFR2，VEGFR3，TIE2), oncogenesis (KIT, RET, RAF-1, BRAF, BRAF^V600E), and the tumour microenvironment (PDGFR-β, FGFR). Regorafenib has promising antineoplastic activity in various tumor types. Regorafenib is mainly metabolized by CYP3A4, and the major human metabolites M-2 (N-oxide) and M-5 (N-oxide and N-desmethyl) are reported to exhibited similar efficacies compared to regorafenib in in vitro and in vivo models. For your reference, [A2979] is a key synthetic intermediate of regorafenib. (The product is for research purpose only.)

References

Regorafenib (BAY 73-4506): A new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity
- S. M. Wilhelm, J. Dumas, L. Adnane, M. Lynch, C. A. Carter, G. Schütz, K.-H. Thierauch, D. Zopf, Int. J. Cancer. 2011, 129, 245.
Regorafenib for cancer (a review)
- D. Strumberg, B. Schultheis, Expert Opin. Invest. Drugs 2012, 21, 879.
Regorafenib in Japanese patients with solid tumors: phase I study of safety, efficacy, and pharmacokinetics
- Y. Sunakawa, J. Furuse, T. Okusaka, M. Ikeda, F. Nagashima, H. Ueno, S. Mitsunaga, K. Hashizume, Y. Ito, Y. Sasaki, Invest. New Drugs 2014, 32, 104.
A validated assay for the simultaneous quantification of six tyrosine kinase inhibitors and two active metabolites in human serum using liquid chromatography coupled with tandem mass spectrometry
- N. P. van Erp, D. de Wit, H.-J. Guchelaar, H. Gelderblom, T. J. Hessing, J. den Hartigha, J. Chromatogr. B 2013, 937, 33.
Determination of regorafenib (BAY 73-4506) and its major human metabolites BAY 75-7495 (M-2) and BAY 81-8752 (M-5) in human plasma by stable-isotope dilution liquid chromatography-tandem mass spectrometry
- F.-T. Hafner, D. Werner, M. Kaiser, Bioanalysis 2014, 6, 1923.

PubMed Literature

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Antimicrobials and Antitumors for Research and Experimental Use

Pharmaceutical Ingredients for Research and Experimental Use

Antitumor Molecular-Targeted Agents

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CAS RN: 755037-03-7 | Product Number: R0142