Pelitinib (EKB-569)

Catalog No. A10706

Pelitinib (EKB-569)是一种有效的,不可逆EGFR抑制剂,IC50为38.5 nM

Product Citations

Shi P, .et al. The Third-Generation EGFR Inhibitor, Osimertinib, Promotes c-FLIP Degradation, Enhancing Apoptosis Including TRAIL-Induced Apoptosis in NSCLC Cells with Activating EGFR Mutations, Transl Oncol, 2019, Mar 8;12(5):705-713 PMID: 30856555

Technical details

Catalog Num	A10706
M. Wt	467.9
Formula	C24H23ClFN5O2
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	257933-82-7
Synonyms	WAY-EKB 569
SMILES	CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)F)Cl)C#N)NC(=O)/C=C/CN(C)C

Biological Activity

Pelitinib (EKB-569)是一种有效的,不可逆EGFR抑制剂,IC50为38.5 nM

Targets

Target	Value
EGFR	IC50: 38.5nM
Src	IC50: 282nM
MEK/ERK	IC50: 800nM
ErbB2	IC50: 1.255μM
Raf	IC50: 3.353μM
c-Met	IC50: 4.1μM
CDK4	IC50: >20μM

Solubility *

In vitro	DMSO	12 mg/mL (25.64 mM)
	Water	Insoluble
	Ethanol	Insoluble
* <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	21.37 mL	106.86 mL	213.72 mL
0.5 mM	4.27 mL	21.37 mL	42.74 mL
1 mM	2.14 mL	10.69 mL	21.37 mL
5 mM	0.43 mL	2.14 mL	4.27 mL

*The above data is based on the productmolecular weight 467.9 . 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.