VOLITINIB (AZD6094, SAVOLITINIB)

Background Information:

Volitinib (AZD6094, HMPL-504, Savolitinib) is an orally bioavailable
ATP-competitive small molecule c-Met kinase inhibitor, binding to the
enzyme potently with IC50 of 4 nM, and highly selective (>650 fold
selectivity) over a panel of 265 kinases. Demonstrated selectivity for
MET-driven disease, with MET amplified cell lines being most sensitive
(IC50s of 1nM), and Displayed potent anti-tumor activity in
cMET-dysregulated GC patient-derived tumor xenograft (PDX) models.

Reference:

1. A.G. Schuller, et al, The MET Inhibitor AZD6094 (Savolitinib,
HMPL-504) Induces Regression in Papillary Renal Cell Carcinoma
Patient-Derived Xenograft Models. Clin Cancer Res. 2015 Jun 15;
21(12):2811-9. doi: 10.1158/1078-0432.CCR-14-2685. Epub 2015 Mar 16.
2. P. G. Gavine, et al, Volitinib, a potent and highly selective c-Met
inhibitor, effectively blocks c-Met signaling and growth in c-MET
amplified gastric cancer patient-derived tumor xenograft models, Mol
Oncol. 2015 Jan; 9(1):323-33. doi: 10.1016/j.molonc.2014.08.015. Epub
2014 Sep 10.*Confirmed precisely by a high-precision quantitative
elemental analysis.

APIM050255: VOLITINIB (AZD6094, SAVOLITINIB)

CAS No.: 1313725-88-0.
Molecular Formula: C₁₇H₁₅N₉ ? 2HCl ?2H₂O.
Molecular Weight: 454.3.
Purity: 100% optical purity (Chiral HPLC), 99.8% chemical purity (HPLC at 215 and 254 nm).
QC: HPLC-MS, ¹HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO (22.7mg/ml, 50mM).
Storage: Store at 0°C (short term), -20°C (long term), desiccated.