PF299804 (Dacomitinib, PF299)

Catalog No. A11051

PF299804是一种有效的，可口服的酪氨酸激酶人表皮生长因子受体（HER）1（EGFR），HER2和HER4不可逆抑制剂。

Product Citations

Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
Momeny M, .et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells, Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
Majid Momeny, .et al. Dacomitinib, a pan-inhibitor of ErbB receptors, suppresses growth and invasive capacity of chemoresistant ovarian carcinoma cells, Sci Rep, 2017, 7: 4204 PMID: 28646172
Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358

Technical details

Catalog Num	A11051
M. Wt	469.9
Formula	C24H25ClFN5O2
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1110813-31-4
Synonyms	PF-299804, Dacomitinib, PF-299
SMILES	COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)/C=C/CN4CCCCC4

Biological Activity

PF299804是一种有效的，可口服的酪氨酸激酶人表皮生长因子受体（HER）1（EGFR），HER2和HER4不可逆抑制剂。

Targets

EGFR (Cell-free assay)	ErbB2 (Cell-free assay)	ErbB4 (Cell-free assay)
6.0 nM	45.7 nM	73.7 nM

Solubility *

In vitro (25°C)	DMSO	17 mg/mL (36.17 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	1% DMSO+30% polyethylene glycol+1% Tween 80, pH 9	9 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	21.28 mL	106.41 mL	212.81 mL
0.5 mM	4.26 mL	21.28 mL	42.56 mL
1 mM	2.13 mL	10.64 mL	21.28 mL
5 mM	0.43 mL	2.13 mL	4.26 mL

*The above data is based on the productmolecular weight 469.9 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.