MGCD516 (SITRAVATINIB)

Background Information:

MGCD516 is a clinical stage, orally available and potent small
molecule inhibitor, targeting a closely related family of Receptor
Tyrosine Kinases (RTKs) including RET, TRK, DDR2, MET, Axl , KIT, as
well as VEGFR and PDGFR family members. RTKs inhibited by MGCD516 are
genetically altered in a variety of cancers, including non-small cell
lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC),
functioning as oncogenic drivers promoting cancer development and
progression. Alterations in these RTKs have also been implicated in
tumor resistance mechanisms. MGCD516 has demonstrated broad antitumor
activity including demonstration of tumor regression in preclinical
models harboring genetic dysregulation of MGCD516 targets including MET
amplification, METex14del, RET rearrangement and CHR4q12 amplification.
It is currently in clinical evaluations.

APIM050197: MGCD516 (SITRAVATINIB)

CAS No.: 1123837-84-2.
Molecular Formula: C33H29F2N5O4S? 0.3H2O.
Molecular Weight: 635.1.
Purity: >98.5% by HPLC.
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0-4 °C (short term), -20 °C (long term), desiccated.