PELITINIB
Synonym(s):(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide;EKB 569;EKB-569;WAY-EKB-569
- CAS NO.:257933-82-7
- Empirical Formula: C24H23ClFN5O2
- Molecular Weight: 467.92
- MDL number: MFCD09837868
- EINECS: 803-625-4
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is PELITINIB?
Description
Pelitinib is a cyanoquinoline that irreversibly inhibits the EGFR receptor tyrosine kinase (IC50 = 39 nM). It inhibits HER2 with a much weaker potency (IC50 = 1.2 μM). By disrupting Akt and MAPK pathways, pelitinib can induce apoptosis and suppress the growth of tumor cell lines, displaying particularly strong efficacy against hepatocellular carcinoma cells (IC50s = ~2 μM).
Chemical properties
Off-White Solid
The Uses of PELITINIB
Labelled Pelitinib (P218702). A tyrosine kinase inhibitor; it is used to prepare formulation for treating primary or secondary cancer.
The Uses of PELITINIB
Pelitinib is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity.
The Uses of PELITINIB
An EGFR inhibitor
What are the applications of Application
Pelitinib is an EGFR inhibitor
Definition
ChEBI: Pelitinib is an aminoquinoline, a nitrile, a monocarboxylic acid amide and a member of monochlorobenzenes. It has a role as a protein kinase inhibitor.
storage
Store at -20°C
References
[1] torrance cj, jackson pe, montgomery e, kinzler kw, vogelstein b, wissner a, nunes m, frost p, discafani cm. combinatorial chemoprevention of intestinal neoplasia. nat med. 2000 sep;6(9):1024-8.
[2] nunes m, shi c, greenberger lm. 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. mol cancer ther. 2004 jan;3(1):21-7.
Properties of PELITINIB
Melting point: | 173-178°C |
Boiling point: | 655.5±55.0 °C(Predicted) |
Density | 1.34 |
storage temp. | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
solubility | DMSO: soluble5mg/mL, clear (warmed) |
form | powder |
pka | 12.23±0.43(Predicted) |
color | white to beige |
Safety information for PELITINIB
Signal word | Danger |
Pictogram(s) |
Skull and Crossbones Acute Toxicity GHS06 |
GHS Hazard Statements |
H301:Acute toxicity,oral |
Precautionary Statement Codes |
P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. |
Computed Descriptors for PELITINIB
Related products of tetrahydrofuran
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