Regorafenib CAS 755037-03-7 API Active Pharmaceutical Ingredient

Product Description:

Product Name:Regorafenib CAS 755037-03-7

Synonyms:

4-[4-({[4-chioro-3-(trifluoroMethyl)phenyl]carbaMoyl}aMino)-3-fluorophenoxy]-pyridine-2-carboxylic acid Methylamide;

4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide;

Chemical & Physical Properties

Appearance: White powder

Assay: NLT99%

Melting point: 206.0 to 210.0℃

Boiling point:513.4±50.0 ℃(Predicted)

Density:1.491±0.06 g/cm3(Predicted)

Flash Point:264.3±30.1 °C

Water solubility:DMSO (Slightly), Methanol (Slightly)

Application:

1.Regorafenib is a new type of oral multi-target protein kinase inhibitor, which can block tumor cell proliferation, inhibit tumor angiogenesis and regulate tumor microenvironment, and has good anti-tumor activity.

2. Regorafenib has pharmacological effects and is a more potent oral TKIs synthesized on the basis of sorafenib. It is a novel oral small molecule tyrosine kinase inhibitor that can inhibit multiple tyrosine kinase targets, mainly by inhibiting VEGF receptors. VEGFR1, VEGFR2, VEGFR3 tyrosine kinase receptor TIE-2 and platelet-derived growth factor receptor activity inhibit neovascularization.

3. For clinical studies, first of all, phase 1 clinical studies: Foreign scholars have conducted a number of phase I clinical studies to evaluate the safety of regafenib, to determine its maximum tolerated dose (MTD), and to roughly evaluate its efficacy in refractory solid tumors; This is followed by a Phase 3 clinical study that may become another treatment option for refractory mCRC following multiline therapy.

4. The adverse reactions were similar to those common to other small-molecule targeted drugs after treatment with regafenib, including hand and foot syndrome, fatigue, diarrhea, hypertension, rash or peeling, etc.

5.However, most patients could still tolerate it by adjusting the drug dose.

6. The safety of low birth weight infants, newborns, infants or children has not been established. The elderly have reduced physical function, and should be carefully administered while observing the patient's condition.

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