CAS Number: 341031-54-7

Formula: C22H27FN4O2.C4H6O5.

Molecular Weight: 532.566 g/mol

Method of Analysis: In house Monograph

Application: Sunitinib is an indolinone derivative and tyrosine kinase inhibitor with potential antineoplastic activity. It is an oral, small-molecule, multi-targeted receptor tyrosine kinase (TTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). Sunitinib was, therefore, the first cancer drug simultaneously approved for two different indications. Sunitinib inhibits cellular signaling by targeting multiple RTKs. These include all platelet-derived growth factor receptors (PDGF-R) and vascular endothelial growth factor receptors (VEGF-R). Sunitinib also inhibits KIT (CD117), the RTK that drives the majority of GISTs. In addition, sunitinib inhibits other RTKs including RET, CSF-1R, and flt3. The fact that sunitinib targets many different receptors, leads to many of its side effects such as the classic hand-foot syndrome, stomatitis, and other dermatologic toxicities.

Mechanism:

Sunitinib’s inhibition include all receptors for platelet-derived growth factor (PDGF-Rs) and vascular endothelial growth factor receptors (VEGFRs), which play a role in both tumor angiogenesis and tumor cell proliferation. The simultaneous inhibition of these targets therefore reduces tumor vascularization and triggers cancer cell apoptosis and thus results in tumor shrinkage. This agent also inhibits the phosphorylation of Fms-related tyrosine kinase 3 (FLT3), another receptor tyrosine kinase expressed by some leukemic cells. Furthermore, Sunitinib inhibits CD117 (c-KIT), the receptor tyrosine kinase that (when improperly activated by mutation) drives the majority of gastrointestinal stromal cell tumors. Therefore, Sunitinib has been recommended as a second-line therapy for patients whose tumors develop mutations in c-KIT that make them resistant to imatinib, or who cannot tolerate the drug. In addition, sunitinib binds other receptors, which include: RET, CD114, CD135.

Storage conditions: Preserve in well-closed container, at room temperature.

Packaging: Polyethylene nylon plastic bag