Regorafenib 99% White Powder CAS 755037-03-7

Regorafenib 99% white powder is a chemical substance with the molecular formula C21H15N4O3F4Cl, molecular weight: 482.8154, melting point: 206.0 to 210.0 °C, boiling point: 513.4±50.0 °C(Predicted). It is a white-like powder, and its hydrate is pink to light brown solid powder, which is slightly soluble in ethanol, methanol, and ethyl.

Regorafenib is a small molecule multi-kinase inhibitor, and its molecular structure is similar to sorafenib, with the only difference being the fluorine atom in the middle benzene ring. It is a new molecular targeted drug developed by Bayer Company, and it was approved by the Food and Drug Administration (FDA) on September 27th, 2012 for the treatment of metastatic colorectal cancer. Regorafenib is a new type of multi-target protein kinase inhibitor, which can block tumor cell proliferation, inhibit tumor angiogenesis and regulate tumor microenvironment, and has good anti-tumor activity.

What is Regorafenib?

Regorafenib 99% white powder can effectively block many protein kinases involved in tumor angiogenesis (VEGFR-1, 2, 3, TIE2), tumorigenesis (KIT, RET, RAF-1, BRAF), tumor metastasis (VEGFR3, PDGFR, FGFR) and tumor immunity (CSF1R). It is not an exaggeration to deal with 12 targets in one breath and call it a universal targeting drug. Up to now, Regorafenib has been approved for the treatment of metastatic colorectal cancer (mCRC), metastatic gastrointestinal stromal tumor (GIST), and second-line treatment of hepatocellular carcinoma (HCC).

There are so many targets, that it is destined that Regorafenib will not be ordinary. Compared with his previous sorafenib, Regorafenib has not changed much, but only an F atom is added on the basis of the sorafenib molecular formula. However, it is the optimization of such an F atom that Bayer Company has developed for 12 years. This added F atom has greatly increased the biological activity of Regorafenib, giving it the opportunity to reduce the dosage and increase the curative effect. It can be seen that Regorafenib.

How does Regorafenib work?

In vitro and in vivo preclinical studies show that Regorafenib 99% White Powder has a wide range of anti-tumor activities. As a multi-target kinase inhibitor. A number of protein kinases whose targeting effects involve tumor angiogenesis and tumor cell proliferation. These kinases include:

① Vascular endothelial growth factor receptor-1 (VEGFR-1), VEGFR-2, VEGFR-3, and tyrosine-protein kinase receptor-2 (TIE-2) related to tumor angiogenesis;

② Proto-oncogene C. Kit, tyrosine-protein kinase receptor RET, proto-oncogene C-RAF, serine/threonine-protein kinase B(BRAF), mitogen-activated protein (MAP) kinase p38 related to tumor cell proliferation:

③ Platelet-derived growth factor receptor-13 (PDGFR-13) and fibroblast growth factor receptor-1 (FGFR-1) are related to the tumor microenvironment. It has multiple anti-tumor effects of blocking tumor angiogenesis and inhibiting tumor cell proliferation by blocking and inhibiting the activity of the above kinases.

What are the adverse reactions to Regorafenib?

The most common adverse reactions (≥30%) are fatigue/fatigue, loss of appetite, food intake, skin reaction of hands and feet, etc. Early clinical trials observed that his most common adverse reactions were skin toxicity and thyroid dysfunction, which were similar to those of other similar multi-target kinase inhibitors.

Most adverse reactions are mild and moderate, which can be controlled by clinical treatment.

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Note: This compound should be used for research purposes only. These claims have not been evaluated by the Food and Drug Administration. Please consult your doctor and learn about available studies before using them. This product is not intended to diagnose, treat, cure or prevent any disease.

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