Dacomitinib
Tocris Bioscience, part of Bio-Techne | Catalog # 6231
Potent irreversible pan ErbB inhibitor
Key Product Details
Description
Potent irreversible pan ErbB inhibitor
Alternative Names
PF00299804
Product Description
Dacomitinib is a potent irreversible pan ErbB inhibitor (IC50 values are 6.0, 45.7 and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively). Inhibits mutant and wild type forms of ErbB, including EGFR T780M, and shows activity in NSCLC cell lines sensitive and resistant to Iressa (Cat. No. 3000). Inhibits tumor growth. Orally bioavailable.Licensing Information
Sold for research purposes under agreement from Pfizer Inc.Product Specifications
Molecular Weight
469.94
Formula
C24H25ClFN5O2
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide
CAS Number
1110813-31-4
PubChem ID
11511120
InChI Key
LVXJQMNHJWSHET-AATRIKPKSA-N
SMILES
O=C(/C=C/CN1CCCCC1)NC2=C(OC)C=C(N=CN=C3NC4=CC=C(F)C(Cl)=C4)C3=C2
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 46.99 | 100 | |
| DMSO | 46.99 | 100 |
Preparing Stock Solutions
for Dacomitinib
The following data is based on the product molecular weight 469.94
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.13 mL | 10.64 mL | 21.28 mL |
| 5 mM | 0.43 mL | 2.13 mL | 4.26 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.13 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Gonzales Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor. Mol.Cancer.Ther. 2008 PMID: 18606718
- Li A ROR1-HER3-lncRNA signalling axis modulates the Hippo-YAP pathway to regulate bone metastasis. Nat.Cell.Biol. 2017 PMID: 28114269
- Engelman PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefi. Cancer.Res. 2007 PMID: 18089823
Product Specific Notices for Dacomitinib
For research use only
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