Axitinib CAS 319460-85-0 Raw Materials Powder

CAS: 319460-85-0

MF: C22H18N4OS

Specification​: 99% min Axitinib Powder

Sample: Axitinib Powder

Brand: Henrikang

Appearance: White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Axitinib Powder Usage and Synthesis .

Axitinib (Axitinib) is a multi-targeted small molecule inhibitor, with VEGFR, Kit, PDGFR, and RET as the primary targets, and is currently approved for the second-line treatment of advanced kidney cancer, meaning that advanced kidney cancer can be treated with Axitinib after failure of sotan treatment.

Axitinib Powder is an orally administered targeted therapeutic ingredient that is a tyrosine kinase inhibitor.Axitinib Raw Materials are used Axitinib Raw Materials are used primarily as a drug ingredient for the treatment of renal cell carcinoma (RCC) and thyroid cancer.

Axitinib CAS 319460-85-0 inhibits the activity of the Axitinib CAS 319460-85-0 inhibits the activity of the vascular endothelial growth factor receptor (VEGFR) activity, thereby stopping the growth and spread of tumor cells. China Pharmaceutical Company specializes in the export of axitinib API, welcome to cooperate.

In addition to kidney cancer, this drug has also been tried by patients in hepatocellular carcinoma, sarcoma, neuroendocrine tumors, and other solid tumors that are recognized to be sensitive to anti-angiogenic drugs and have a rich blood supply to the tumor, and has shown some efficacy.

Applications of Axitinib Powder ：

Axitinib is a multi-target small molecule inhibitor, the main targets are VEGFR, Kit, PDGFR (multi-target, anti-angiogenesis-based small molecule inhibitors, the targets are basically these, some can also inhibit MET, such as Cabozantinib).

Acitretinib 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. The solubility is 0.8mg/ml in pH1.2 hydrochloric acid solution at 20℃ and 0.2 microgram/ml in pH6.8 phosphate buffer solution, which is a typical pH-dependent drug.

The currently approved indication for marketing is the second-line treatment of advanced kidney cancer, which means that advanced kidney cancer can be treated with axitinib after failure of sotan treatment. In addition to kidney cancer, this drug has also been tried by patients in hepatocellular carcinoma, sarcoma, neuroendocrine tumors and other solid tumors that are recognized to be more sensitive to anti-angiogenic drugs and have rich tumor blood supply.

Pharmacological Effect of Axitinib Powder：

Axitinib (Axitinib) is a multitargeted tyrosine kinase inhibitor that inhibits the vascular endothelial growth factor receptors VEGFR1, VEGFR2, VEGFR3, platelet-derived growth factor receptor, and c-KIT. inhibitor or cytokine therapy failed in adult patients with progressive renal cell carcinoma (RCC).

Axitinib inhibits tyrosine kinase receptors, including the vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2 and VEGFR-3), at therapeutic doses. These receptors are associated with pathological angiogenesis, tumor growth and cancer progression. In vitro tests and in vivo mouse models have shown that axitinib inhibits VEGF-mediated endothelial cell proliferation and survival; in a tumor-bearing mouse model, axitinib inhibits tumor growth and phosphorylation of VEGFR-2.

Axitinib is a second-generation oral VEGFR-1, 2, and 3 selective inhibitor that blocks the VEGFR receptor at nanomolar drug concentration levels while achieving minimal inhibition of other target proteins and has a short half-life in humans.

A phase III randomized trial (AXIS) compared the efficacy of axitinib with sorafenib for the treatment of patients who were not responding to cytokine or other targeted drug therapy.

The trial enrolled 723 patients randomized to axitinib and improved their median progression-free survival from 5 months to 7 months, an improvement of 40.0 percent.

The overall median progression-free survival was 6.7 months in the axitinib group and 4.7 months in the sorafenib group (HR=0.67; 95% CI: 0.54 to 0.81). The most significant difference in progression-free survival was seen in patients who were not effective with cytokine therapy.

For patients who were not effective with sunitinib treatment (n=194 in the axitinib group and n=195 in the sorafenib group), progression-free survival was 4.8 months (95% CI, 4.5 to 6.4) in the axitinib group and 3.4 months (95% CI, 2.6 to 4.7) in the sorafenib group. the AXIS trial showed that axitinib had no less than grade 3 toxic effects, including 11.0 percent of patients with diarrhea, 16.0 percent with hypertension, and 11.0 percent with malaise.

This study initially established axitinib as a second-line treatment for metastatic kidney cancer. However, a recently reported analysis of overall survival showed that overall survival was similar in the axitinib and sorafenib groups, 20.1 months for axitinib and 19.2 months for sorafenib, with no significant difference.