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Published TCIMAIL newest issue No.197
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CAS RN: 257933-82-7 | Product Number: P2529
Pelitinib
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Purity: >97.0%(HPLC)
Synonyms:
- EKB 569
- (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-dimethylamino-2-butenamide
Product Documents:
| Size | Unit Price | Belgium | Japan* | Quantity |
|---|---|---|---|---|
| 25MG |
€59.00
|
1 | 35 |
|
| 100MG |
€180.00
|
1 | 5 |
|
*Stock available in Belgium will be delivered in 1 to 3 days
*Stock available in Japan will be delivered in 1 to 2 weeks (excludes regulated items and dry ice shipments).
| Product Number | P2529 |
| Purity / Analysis Method | >97.0%(HPLC) |
| Molecular Formula / Molecular Weight | C__2__4H__2__3ClFN__5O__2 = 467.93 |
| Physical State (20 deg.C) | Solid |
| Storage Temperature | Frozen (<0°C) |
| Condition to Avoid | Light Sensitive,Heat Sensitive |
| Packaging and Container | 25MG-Glass Bottle with Plastic Insert (View image) |
| CAS RN | 257933-82-7 |
| Reaxys Registry Number | 9301287 |
| PubChem Substance ID | 354335185 |
| MDL Number | MFCD09837868 |
Specifications
| Appearance | White to Light yellow powder to crystal |
| Purity(HPLC) | min. 97.0 area% |
Properties (reference)
| Melting Point | 198 °C |
| Solubility in water | Soluble |
GHS
| Pictogram |
|
| Signal Word | Danger |
| Hazard Statements | H301 + H311 + H331 : Toxic if swallowed, in contact with skin or if inhaled. H315 : Causes skin irritation. H319 : Causes serious eye irritation. |
| Precautionary Statements | P261 : Avoid breathing dust. P264 : Wash skin thoroughly after handling. P280 : Wear protective gloves/ protective clothing/ eye protection/ face protection/ hearing protection. P301 + P310 + P330 : IF SWALLOWED: Immediately call a POISON CENTER/doctor. Rinse mouth. P302 + P352 + P312 : IF ON SKIN: Wash with plenty of water. Call a POISON CENTER/doctor if you feel unwell. P403 + P233 : Store in a well-ventilated place. Keep container tightly closed. |
Related Laws:
Transport Information:
| UN Number | UN2811 |
| Class | 6.1 |
| Packing Group | III |
| HS Number | 2933499090 |
Application
Pelitinib: An Irreversible Inhibitor of the Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase
Pelitinib (EKB-569) is an irreversible inhibitor of epidermal growth factor receptor (EGFR, also known as ErbB-1) tyrosine kinase. EGFR is the cell-surface receptor for members of the epidermal growth factors (EGFs) that play a central role in regulating cell division and death. EGFR tyrosine kinase is activated by binding of EGFs. This binding causes cell differentiation and proliferation. Therefore, pelitinib is often used for cancer research. For your reference, a related product [C3315] is a synthetic intermediate of pelitinib and neratinib (HKI-272). (The product is for research purpose only.)
References
- Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes
- The development of HKI-272 and related compounds for the treatment of cancer (a review)
- Irreversible EGFR inhibitor EKB-569 targets low-LET γ-radiation-triggered rel orchestration and potentiates cell death in squamous cell carcinoma
- Novel EGFR-TK inhibitor EKB-569 inhibits hepatocellular carcinoma cell proliferation by AKT and MAPK pathways
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