Axitinib Cas:319460-85-0

Acitinib (acitinib),
It is a multi-target small molecule inhibitor, the main targets are VEGFR, Kit, PDGFR, RET. The current approved indication for the market is second-line treatment of advanced kidney cancer, that is, acitinib can be selected for advanced kidney cancer after the failure of Sutent treatment. In addition to kidney cancer, this drug has also been tried by patients in liver cancer, sarcoma, neuroendocrine tumors and other recognized anti-angiogenic drugs are more sensitive to solid tumors with rich tumor blood supply, and also has a certain effect.

Intro
Acitinib is a white powder, melting point 218.4℃, slightly soluble in polyethylene glycol 400, slightly soluble in methanol or ethanol, very slightly soluble in acetonitrile, almost insoluble in water. At 20℃, the solubility of pH1.2 hydrochloric acid solution is 0.8mg/ml, and the solubility of pH6.8 phosphate buffer solution is 0.2 µg /ml, which is a typical PH-dependent drug.

Apply
Acitinib (Axitinib) is a multitarget tyrosine kinase inhibitor developed by Pfizer that inhibits vascular endothelial growth factor receptors VEGFR1, VEGFR2, VEGFR3, platelet-derived growth factor receptors and c-KIT. Acitinib is an antineoplastic drug primarily used in adult patients with advanced renal cell carcinoma (RCC) who have previously failed treatment with a tyrosine kinase inhibitor or cytokine.
Pharmacological action

At therapeutic doses

acitinib inhibits tyrosine kinase receptors, including vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, and VEGFR-3). These receptors are associated with pathological angiogenesis, tumor growth, and cancer progression. In vitro and in vivo mouse model tests showed that acitinib could inhibit VEGF mediated endothelial cell proliferation and survival. In a tumor-bearing mouse model, acitinib inhibited tumor growth and VEGFR-2 phosphorylation.