Neratinib (HKI-272)

Catalog No. A10638

Neratinib (HKI-272)是一种酪氨酸激酶抑制剂。

Product Citations

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
Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961

Technical details

Catalog Num	A10638
M. Wt	557.0
Formula	C30H29ClN6O3
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	698387-09-6
Synonyms
SMILES	CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)/C=C/CN(C)C

Biological Activity

Neratinib (HKI-272)是一种酪氨酸激酶抑制剂。

Targets

Target	Value
HER2	IC50: 59nM
EGFR	IC50: 92nM
KDR	IC50: 800nM
Src	IC50: 1.4μM
PDK-1	IC50: >5μM
IKK2	IC50: >9μM
CDK2/CyclinE	IC50: >18μM
CDK1/CyclinB1	IC50: >18μM
C-Raf/MEK1	IC50: >18μM
Tpl-2	IC50: >18μM
Akt	IC50: >20μM
c-Met	IC50: >35μM
MK2	IC50: >45μM
CDK4/CyclinD1	IC50: >50μM

Solubility *

In vitro (25°C)	DMSO	Warmed: 4 mg/mL (7.18 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	30% PEG400+0.5% Tween80+5% propylene glycol	4 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	17.95 mL	89.77 mL	179.53 mL
0.5 mM	3.59 mL	17.95 mL	35.91 mL
1 mM	1.8 mL	8.98 mL	17.95 mL
5 mM	0.36 mL	1.8 mL	3.59 mL

*The above data is based on the productmolecular weight 557.0 . 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.