Chemical Property of Dacomitinib
Chemical Property:
- Appearance/Colour:White to Off-White Solid
- Melting Point:>187°C (dec.)
- Boiling Point:665.7±55.0 °C(Predicted)
- PKA:12.05±0.43(Predicted)
- PSA：79.38000
- Density:1.344
- LogP:5.23900
- Storage Temp.:Refrigerator
- Solubility.:DMSO (Slightly), Methanol (Slightly, Heated)
- XLogP3:4.4
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:7
- Rotatable Bond Count:7
- Exact Mass:469.1680809
- Heavy Atom Count:33
- Complexity:665
- Purity/Quality:
-
99% *data from raw suppliers
Dacomitinib *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
-
SDS file from LookChem
Useful:
- Drug Classes:Antineoplastic Agents
- Canonical SMILES:COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)C=CCN4CCCCC4
- Isomeric SMILES:COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)/C=C/CN4CCCCC4
- Recent ClinicalTrials:Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial
- Recent EU Clinical Trials:ERIS- EGFR-Mutated Lung Cancer in Randomized Investigator-Initiated Study
- Recent NIPH Clinical Trials:A phase II study to evaluate prophylactic treatment of dacomitinib-induced dermatologic adverse events in EGFR-mutated advanced non-small cell lung cancer
-
Description
Dacomitinib is a selective and irreversible inhibitor of EGFR. It is a drug candidate for the treatment of non-small cell lung carcinoma. It is current under the Phase III clinical trials. It also shows potential for the treatment of HER-2 amplified breast cancer cells lines that are resistant to trastuzumab and lapatinib. The epidermal growth factor receptors (EGFR), whose members include ErbB1 (HER1), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4), are receptor tyrosine kinases that are often over-expressed in cancer. PF-299804 is a second generation pan-ErbB receptor tyrosine kinase inhibitor (IC50s = 6, 45.7, and 73.7 nM for ErbB1, ErbB2, and ErbB4, respectively) that irreversibly binds to the ATP site in the catalytic domains of ErbB receptors. At 15 mg/kg, it demonstrates antitumor activity ranging from delay in tumor growth to complete regression in various tumor xenograft models expressing either wild-type ErbB or mutant ErbB family members that show resistance to first generation ErbB kinase inhibitors.
-
Uses
Dacomitinib (PF299804), which name is (E)-N-[4-(3-chloro-4-fluoroanilino)-7- methoxyquinazolin-6-yl]-4-piperidin-1-ylbut-2-enamide, is a potent, orally available, highly selective, irreversible small-molecule tyrosine kinase inhibitor (TKI) of tyrosine kinase human epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4. It is most effective against EGFR with IC50 of 6 nM. It is highly effective against NSCLCs carrying EGFR or ERBB2 mutant (anti-Gefitinib) and EGFR T790M mutant. Dacomitinib is an Erb-inhibitor, or an inhibitor of the members of the epidermal growth factor receptor family. Used as an ant-cancer agent due to observation of over-expressed epidermal growth factor receptor in nearly all cases of squamous cell carcinoma in the head and neck.
