Canertinib (CI-1033)

Catalog No. A10211

Canertinib (CI-1033)是一种不可逆的酪氨酸激酶抑制剂，对EGFR（IC50 0.8 nM），HER-2（IC50 19 nM）和ErbB-4（IC50 7 nM）具有活性。

Product Citations

Fukuda N, .et al. Rapid Evaluation of Tyrosine Kinase Activity of Membrane Integrated Human Epidermal Growth Factor Receptor Using the Yeast Gγ Recruitment System, ACS Synth Biol., 2015, 4(4):421-9 PMID: 25006755

Technical details

Catalog Num	A10211
M. Wt	485.9
Formula	C24H25ClFN5O3
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	267243-28-7
Synonyms	CI-1033, CI1033, PD-183805
SMILES	C=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4

Biological Activity

Canertinib (CI-1033)是一种不可逆的酪氨酸激酶抑制剂，对EGFR（IC50 0.8 nM），HER-2（IC50 19 nM）和ErbB-4（IC50 7 nM）具有活性。

Targets

EGFR (Cell-free assay)	ErbB2 (Cell-free assay)
1.5 nM	9.0 nM

Solubility *

In vitro (25°C)	DMSO	2 mg/mL (4.11 mM)
	Water	Insoluble
	Ethanol	8 mg/mL (16.46 mM)
In vivo	30% propylene glycol, 5% Tween 80, 65% D5W	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	20.58 mL	102.9 mL	205.8 mL
0.5 mM	4.12 mL	20.58 mL	41.16 mL
1 mM	2.06 mL	10.29 mL	20.58 mL
5 mM	0.41 mL	2.06 mL	4.12 mL

*The above data is based on the productmolecular weight 485.9. 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.