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Crizotinib CAS NO.877399-52-5
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- Product Details
Keywords
- PF 2341066
- 877399-52-5
- Crizotinib
Quick Details
- ProName: Crizotinib
- CasNo: 877399-52-5
- Molecular Formula: C21H22Cl2FN5O
- Appearance: Off-white to white solid powder
- Application: Crizotinib is an anti-cancer drug.Criz...
- DeliveryTime: Within 3-7 days after receipt of your ...
- PackAge: As customer request
- Port: Qingdao\Shanghai,China
- ProductionCapacity: 100 Kilogram/Week
- Purity: 99+%
- Storage: Store in a cool,dry place and keep awa...
- Transportation: By Sea/Air/Courier
- LimitNum: 0 Metric Ton
- Moisture Content: 0.1%max
- Impurity: 0.1%max
- Appearance: N/A
- Boiling point: 599.2±50.0 °C(Predicted)
- Density: 1.47±0.1 g/cm3(Predicted)
Superiority
Details
[Product Name]: Crizotinib
[Synonyms]:PF-2341066; 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-Pyridinamine;(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine;3-[(1R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]pyridin-2-amine;Crizotinib;PF 2341066;PF-02341066;PF-2341066/Crizotinib;3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine
[CAS]: 877399-52-5
[MF]: C21H22Cl2FN5O
[MW]: 450.343
[Purity]: 99%
[Appearance]: White Crystalline Powder
[Crizotinib COA]:
|
Test Items |
Specification |
Results |
|
Description |
White to off white crystalline powder |
Comply |
|
Melting point |
166-170°C |
167.3-168.1°C |
|
Identification |
Positive reaction |
Positive reaction |
|
Related substances |
≤1.0% |
0.16% |
|
Loss on drying |
≤0.5% |
0.06% |
|
Residue on ignition |
≤0.1% |
0.02% |
|
Chloride |
≤0.014% |
<0.014 |
|
Heavy Metals |
≤20ppm |
<20ppm |
|
Clarity of solution |
Conform to standard |
Complies |
|
Microbial Limit |
≤20ppm |
<20ppm |
|
Assay |
≥99.0% |
99.12% |
Crizotinib is an anti-cancer drug.Crizotinib has an aminopyridine structure, and functions as a protein kinase inhibitor by competitive binding within the ATP-binding pocket of target kinases.Crizotinib is currently thought to exert its effects through modulation of the growth, migration, and invasion of malignant cells.Other studies suggest that crizotinib might also act via inhibition of angiogenesis in malignant tumors.
[Packing]:
1. Food bag packing( Disguised package)
Usually products are send in discreet way,based on our rich in shipping products to every countries,we usually use disguised way.
The photo of food disguised package for your reference,which has passed through every countries smoothly,products are packed well in food box,which mixed with real visible chinese food,and in the express bill we will declare food and sample,customs just think it chinese food and release it.
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 # |
| 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. # |
| 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 |
