SUNITINIB MALATE

PRODUCT IDENTIFICATION

CAS NO. 557795-19-4 (base)
341031-54-7 (malate)
SUNITINIB MALATE 
EINECS NO.  
FORMULA C22H27FN4O2 · C4H6O5
MOL WT. 532.56

TOXICITY

 

H.S. CODE

2933.99.7500
SYNONYMS Sunitinib malate; Sutent;
N-(2-(Diethylamino)ethyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene) methyl)-2,4-dimethyl- 1H-pyrrole-3-carboxamide;
SMILES c1c(F)cc2\C(C(Nc2c1)=O)=C\c1[nH]c(c(C(NCCN(CC)CC)=O) c1C)C.C ([C@@H](C(=O)O)O)C(O)=O

CLASSIFICATION

Angiogenesis modulating agent, Antineoplastic, Receptor tyrosine kinase inhibitor, Indole, Pyrrole

EXTRA NOTES

Inhibits VEGF-R2 and PDGF-Rbeta tyrosine kinase; has antineoplastic activity.

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE

brown to orange solid

MELTING POINT

198 C

BOILING POINT

 

SPECIFIC GRAVITY  
SOLUBILITY IN WATER

 

SOLVENT SOLUBILITY

 

pH  
VAPOR DENSITY

 

REFRACTIVE INDEX

 

NFPA RATINGS

Health hazard: 2, Fire: 0, Reactivity Hazard: 0

AUTOIGNITION

 

FLASH POINT

 

STABILITY Stable under normal conditions.

EXTERNAL LINKS & GENERAL DESCRIPTION

Wikipedia Linking

Google Scholar Search

Drug Information Portal (U.S. National Library of Medicine) - Sunitinib malate

http://www.medsafe.govt.nz/
Mechanism of action: Sunitinib is a small molecule that simultaneously inhibits multiple receptor tyrosine kinases (RTKs) that are implicated in tumour growth, pathologic angiogenesis and metastatic progression of cancer. Sunitinib was evaluated for its inhibitory activity against a wide range of kinases and was identified as a potent inhibitor of platelet-derived growth factor receptor β (PDGFRβ), vascular endothelial growth factor receptors (VEGFR1, VEGFR2 and VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony stimulating factor receptor Type 1 (CSF-1R) and the glial cell-line derived neurotrophic factor receptor (RET). Inhibition of the tyrosine kinase activity of these RTKs by sunitinib has been demonstrated in biochemical and cellular assays, and inhibition of function has been demonstrated in cell proliferation assays in which the activity of PDGFRα was inhibited. The primary metabolite exhibits similar potency compared to sunitinib in biochemical and cellular assays for inhibition of PDGFRβ, VEGFR2 and KIT tyrosine kinase activities. Sunitinib inhibited the phosphorylation of multiple RTKs (PDGFR, VEGFR2, KIT) in tumour xenografts expressing RTK targets in vivo and demonstrated inhibition of tumour growth or tumour regression, and/or inhibited metastases in some experimental models of cancer. Consistent with its multi-targeted profile, sunitinib demonstrated the ability to directly inhibit growth of tumour cells expressing dysregulated RTK targets (PDGFR, RET, FLT3 or KIT) and to inhibit tumour angiogenesis.

http://www.medilexicon.com/
Sutent (sunitinib malate) an oral multi-kinase inhibitor and works by blocking multiple molecular targets implicated in the growth, proliferation and spread of cancer. Sutent is specifically indicated for the treatment of progressive, well-differentiated pancreatic neuroendocrine tumors in patients with unresectable locally advanced or metastatic disease. Sutent is supplied as a tablet for oral administration. The recommended dose for pancreatic meuroendocrine tumors is 37.5 mg taken orally once daily continuously without a scheduled off-treatment period.

http://www.sigmaaldrich.com/
Sunitinib malate is a receptor tyrosine kinase inhibitor, which targets VEGF-R1, VEGF-R2, VEGF-R3, PDGF-Rα, PDGF-Rβ, KIT, FLT3, CSF-1R, and RET. Sunitinib malate is an anticancer drug.

SALES SPECIFICATION

APPEARANCE

brown to orange solid

IDENTIFICATION

passes Test A, B

PURITY

99.0% min

LOSS ON DRYING

0.5% max

IMPURITY

Individual Impurity: 0.5% max
Total Impurity: 1.0% max

HEAVY METALS

20ppm max

RESIDUE ON IGNITION

0.25% max

TRANSPORTATION
PACKING
 
HAZARD CLASS  
UN NO.  
SAFETY INFORMATION

GHS

 

SIGNAL WORD Danger

PICTOGRAMS

HAZARD STATEMENTS

H360 May damage fertility or the unborn child.
H372 Causes damage to organs through prolonged or repeated exposure if swallowed.

PRECAUTIONARY STATEMENTS

P201 Obtain special instructions before use.
P308 + P313 IF exposed or concerned: Get medical advice/ attention.

EC DIRECTIVES

 

HAZARD CODES

T Toxic

RISK PHRASES

61 May cause harm to the unborn child
2  
Risk of explosion by shock, friction, fire or other sources of ignition
48/25
Toxic: danger of serious damage to health by prolonged exposure if swallowed

SAFETY PHRASES

53 Avoid exposure - obtain special instruction before use
22
Do not breathe dust
36/37
Wear suitable protective clothing and gloves

PRICE INFORMATION