 |
|
|
|
Ruze supply good service, thanks.
 |
—— Gaurav
- I'm Online Chat Now
Off - White Solid 877399 52 5 Non Small Cell Lung Cancer Treatment Drugs Crizotinib
Product Details:
Payment & Shipping Terms:
|
Detailed Product Description
| Product Name: | Crizotinib | CAS: | 877399-52-5 |
|---|---|---|---|
| MF: | C21H22Cl2FN5O | MW: | 450.343 |
| EINECS: | 638-814-9 | Mol File: | 877399-52-5.mol |
Weifang Ruze New Material Co.,LTD a China supplier of Crizotinib (CAS No.: 877399-52-5),CAS 877399-52-5 offers for your requirements of RND, evaluation, pilots and commercial along with supportive technical package required for evaluation.
Crizotinib(CAS:877399-52-5)
[Product Name]:Crizotinib
[CAS ]:877399-52-5
[Appearance]:Off-white solid
[CAS ]:877399-52-5
[Molecular Formula]:C21h22cl2fn5o
[Molecular Weight]:450.34
[Purity]:≥99% by HPLC
[Stock]:12kg
[Biological description]
Potent, ATP-competitive inhibitor of c-MET and anaplastic lymphoma kinase (ALK) receptor tyrosine kinases (cell IC50 values are 8.0 and 20 nM respectively). Selective for c-MET and ALK against >120 different kinases. Displays antitumor efficacy in multiple tumor models; inhibits c-MET-dependent proliferation, migration and invasion of human tumor cells in vitro. Orally bioavailable.
[Please note]: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC PROCEDURES, NOT FOR USE IN HUMANS"
Crizotinib Chemical Properties
| storage temp. | room temp |
| form | powder |
| color | white to tan |
| CAS DataBase Reference | 877399-52-5 |
Safety Information
| Safety Statements | 24/25 |
| RIDADR | UN 3077 9 / PGIII |
| WGK Germany | 3 |
| HazardClass | IRRITANT |
| HS Code | 29333990 |
Crizotinib Usage And Synthesis
| Biological Activity | Potent inhibitor of c-MET and anaplastic lymphoma kinase (ALK) (cell IC50 values are 8.0 and 20 nM respectively). Selective for c-MET and ALK against >120 different kinases. Displays antitumor efficacy in multiple tumor models; inhibits c-MET-dependent proliferation, migration and invasion of human tumor cells in vitro. Orally bioavailable. |
| Mechanism of action | Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), and Recepteur d’Origine Nantais (RON). Translocations can affect the ALK gene resulting in the expression of oncogenic fusion proteins. The formation of ALK fusion proteins results in the activation and dysregulation of the gene's expression and signaling, which can contribute to increased cell proliferation and survival in tumors expressing these proteins. Crizotinib demonstrates concentration-dependent inhibition of ALK and c-Met phosphorylation in cell-based assays using tumor cell lines, and also demonstrates antitumor activity in mice bearing tumor xenografts that express EML4-or NPM-ALK fusion proteins or c-Met.Crizotinib is a multitargeted small molecule tyrosine kinase inhibitor, which had been originally developed as an inhibitor of the mesenchymal epithelial transition growth factor (c-MET); it is also a potent inhibitor of ALK phosphorylation and signal transduction. This inhibition is associated with G1-S phase cell cycle arrest and induction of apoptosis in positive cells in vitro and in vivo. Crizotinib also inhibits the related ROS1 receptor tyrosine kinase. References https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3876666/ |
| side effects | crizotinib (Xalkori) is an oral receptor tyrosine kinase inhibitor indicated for the treatment of patients with advanced or metastatic non-small cell lung cancer (NSCLC). Common side effects with Xalkori use include upper respiratory infection, nausea, vomiting, stomach pain, decreased appetite, insomnia, dizziness, tired feeling, diarrhea, constipation, rash or itching, cold symptoms (stuffy nose, sneezing, sore throat), numbness or tingling, or swelling in your hands or feet. http://www.rxlist.com/xalkori-side-effects-drug-center.htm |
| Description | In August 2011, the United States FDA approved crizotinib (PF- 02341066) for the treatment of anaplastic lymphoma kinase (ALK) rearranged non-small-cell lung cancer (NSCLC). Crizotinib is a dual ATP competitive inhibitor of tyrosine kinases c-MET (Mesenchymal-Epithelial Transition Factor) kinase (cellular IC50=8 nM) and ALK (cellular IC50=20 nM), both of which are important targets for cancer chemotherapy. When crizotinib was tested for selectivity versus other kinases it was found to have enzyme IC50's within 100-fold multiples of c-MET for 13 of the 120 kinases tested. In cellular assays, crizotinib was found to inhibit RON (recepteur d’origine nantais) kinase with a 10-fold selectivity window over c-MET. |
| Chemical Properties | White Solid |
| Originator | Pfizer (United States) |
| Uses | A potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). A potential antitumor agent. |
| Uses | Crizotinib is a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). Crizotinib is a potential antitumor agent. |
| Uses | PF-2341066 (Crizotinib) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM, respectivley |
| Definition | ChEBI: A 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine that has R configuration at the chiral centre. The active enantiomer, it acts as a kinase inhibitor and is used for the treatment of patients wi h locally advanced or metastatic non-small cell lung cancer (NSCLC) |
| Indications | Crizotinib (Xalkori(R), Pfizer), approved in 2011, was the first approved inhibitor targeting anaplastic lymphoma kinase (ALK). ROS protooncogene 1-encoded kinase (ROS1) of the tyrosine kinase insulin receptor class and MET proto-oncogene-encoded kinase of the hepatocyte growth factor receptor (HGFR) class are other kinases targeted by crizotinib.When approved in 2011, crizotinib was the first drug specifically targeting NSCLC patients. However, resistance to crizotinib was usually observed in approximately 8 months after initial application and more than half of crizotinib-treated patients experienced gastrointestinal side effects. In 2016,crizotinib was additionally approved for ROS1-positive NSCLC by FDA. |
| Brand name | Xalkori |
Weifang Ruze New Material Co.,LTD supply free sample and datebase on Crizotinib (CAS No.: 877399-52-5), if you want futher information about Crizotinib (CAS No.: 877399-52-5), please feel free to contract us.
Contact Details
Weifang Ruze New Material Co., Ltd.
Contact Person: Ruze02
Other Products
-
Assay 99% Incb28060 Pharmaceutical Intermediates Cas 1029712-80-8 Yellow Powder
-
Customer synthesis Non Small Cell Lung Cancer Medications Dacomitinib (PF299804,1110813-31-4)99% assay
-
CAS 1421373-65-0 Non Small Cell Lung Cancer Medications AZD-9291 (Osimertinib)
-
Non Small Cell Lung Cancer Medications Crizotinib CAS New Medication For Lung Cancer
-
C29H39ClN7O2P Non Small Cell Lung Cancer Medications Brigatinib 99% Assay
-
NSCLC Drugs Afatinib 439081-18-2 Irreversible EGFR / HER2 Inhibitor With EFGR Agents 99% Assay