Welcome to LookChem.com Sign In|Join Free

CAS

  • or

475207-59-1

Post Buying Request

475207-59-1 Suppliers

Recommended suppliersmore

  • Product
  • FOB Price
  • Min.Order
  • Supply Ability
  • Supplier
  • Contact Supplier

475207-59-1 Usage

Indications and Usage

Sorafenib tosylate is a new type of multi-target antitumor drug, was developed by the German Bayer Pharmaceuticals, and displayed expansive antitumor activity in preclinical animal tests. Sorafenib tosylate is mainly used in advanced liver cancer treatment and is well tolerated.

Mechanisms of Action

Sorafenib tosylate can simultaneously affect tumor cells and tumor blood vessels. It has a double antitumor effect: it can block the cell signal transduction pathways mediated by RAF/MEK/ERK to directly inhibit tumor cell growth, while also inhibiting VEGF and platelet derived growth factors (PDGF) receptors to prevent the formation of new tumor blood vessels, thus indirectly inhibiting tumor cell growth.

Clinical Research

In a stage three randomized clinical study of American and European treatments for advanced kidney cancer, 903 cases advanced kidney patients who had experienced one unsuccessful systematic treatment (biological immunity or chemotherapy) were randomly split into two groups. One group received sorafenib tosylate, while the other received a placebo. Mid-term analysis found already 222 deaths and the objective efficacy of the two groups to be 10% and 2%, while 74% and 53% of patients had stabilized conditions. The sorafenib tosylate group’s survival period was longer than that of the placebo group, with the risk ratio as 0.72. However, this different does not have statistical significance, as this is only a mid-term analysis, and final analysis after treatment will yield the correct survival period comparison. 602 advanced liver cancer patients selected from the USA, Europe, Australia, and other countries and areas, who did not receive systematic treatment, were included in a study. Results showed that compared to the placebo, taking sorafenib tosylate could extend their total survival period of patients with late stage or primary liver cancer by about 44% and their extend disease progression period by about 73%.

Adverse reactions

Manageable diarrhea, rashes, fatigue, hand-foot syndrome, hypertension, alopecia, nausea, vomiting, and loss of appetite.

Description

Sorafenib (475207-59-1) was initially developed as a Raf kinase inhibitor, IC50 = 6 nM, but has been shown to inhibit many receptor tyrosine kinases including BRAF (IC50 = 22 nM); VEGFR-2 (IC50 = 90 nM); VEGFR-3 (IC50 = 20 nM); PDGFR-β (IC50 = 57 nM); Flt3 (IC50 = 58 nM); c-KIT (IC50 = 68 nM); FGFR-1 (IC50 = 580 nM).1?Paradoxically more potent in a cellular assay (IC50 = 20 nM) compared to an isolated enzyme assay (IC50 = 107 nM) for c-Fms.2?Inhibits activation of MAPK pathway and ERK phosphorylation.3?Induces caspase-independent apoptosis in melanoma cells.4?Sorafenib is a clinically useful anticancer agent.

Uses

Different sources of media describe the Uses of 475207-59-1 differently. You can refer to the following data:
1. Sorafenib Tosylate (Bay 43-9006) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively
2. An inhibitor of Flk-1 (VEGFR), PDGFR and Raf kinases.

Brand name

Nexavar (Bayer).

General Description

Sorafenib is available in 200-mg tablets for oral administrationand is used in the treatment of RCC and colon cancer.The agent is classified as a multikinase inhibitor because ofits action on numerous kinase enzymes including thePDGF-R, VEGF-R, Kit, and Raf. Sorafenib is 39% to 48% bioavailable and CYP3A4-mediated metabolism giveseight identified metabolites including the N-oxide, which isequally active with the parent. However, the majority of thedrug in plasma is present as the parent compound.Sorafenib is highly protein bound (99.5%). The drug iseliminated primarily in the feces (77%) with 19% appearingin the urine as glucuronides (UGT1A1) and has a eliminationhalf-life of 24 to 48 hours. The most commonly seentoxicity is skin rash that normally occurs within the first6 weeks of therapy. Other adverse effects include hypertension,fatigue, increased wound healing time, and increasedrisk of bleeding.

References

1) Wilhelm et al. (2004), BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis; Cancer Res., 64 7099 2) Guo et al. (2006), Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors; Mol. Cancer Ther., 5 1007 3) Wilhelm et al. (2003), The novel Raf inhibitor BAY 43-9006 blocks signaling and proliferation in BRAF mutant and wildtype melanoma and colorectal tumor cell lies; Proc. Am. Assoc. Cancer Res., 44 106609 4) Panka et al. (2006), The Raf inhibitor BAY 43-9006 (Sorafenib) induces caspase-independent apoptosis in melanoma cells; Cancer Res., 66 1611

Check Digit Verification of cas no

The CAS Registry Mumber 475207-59-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,7,5,2,0 and 7 respectively; the second part has 2 digits, 5 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 475207-59:
(8*4)+(7*7)+(6*5)+(5*2)+(4*0)+(3*7)+(2*5)+(1*9)=161
161 % 10 = 1
So 475207-59-1 is a valid CAS Registry Number.

475207-59-1SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 19, 2017

Revision Date: Aug 19, 2017

1.Identification

1.1 GHS Product identifier

Product name Sorafenib Tosylate

1.2 Other means of identification

Product number -
Other names 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide,4-methylbenzenesulfonic acid

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:475207-59-1 SDS

475207-59-1Upstream product

475207-59-1Downstream Products

Post a RFQ

Enter 15 to 2000 letters.Word count: 0 letters

Attach files(File Format: Jpeg, Jpg, Gif, Png, PDF, PPT, Zip, Rar,Word or Excel Maximum File Size: 3MB)

1

What can I do for you?
Get Best Price

Get Best Price for 475207-59-1