Neratinib (HKI-272)

Name: Neratinib (HKI-272)
Brand: Adooq Bioscience
SKU: A10638
Rating: 100 (2 reviews)

Catalog No.: A10638

HER2 inhibitor

Product Citations (2)

Neratinib (HKI-272) Chemical Structure

CAS NO. 698387-09-6

Neratinib (HKI-272) is a tyrosine kinase inhibitor.

Availability: In stock

Package	Price	Qty
5 mg	Regular Price: $50.00 Special Price $40.00
10 mg	Regular Price: $75.00 Special Price $60.00
25 mg	Regular Price: $100.00 Special Price $80.00
100 mg	Regular Price: $220.00 Special Price $176.00
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Products are for laboratory research use only. Not for human use. We do not sell to patients.

Adooq Products cited in reputable paper

Publications Citing Use of Adooq Neratinib (HKI-272)

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

Biological Activity

Neratinib (HKI-272) is a tyrosine kinase inhibitor.

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.

Chemical Properties

Catalog Num	A10638
Actions	Inhibitor
CAS No.	698387-09-6
Formula	C30H29ClN6O3
M. Wt	557.0
Purity	>98%
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
Storage	Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.