Neratinib (HKI-272)

Catalog No.: A10638

HER2 inhibitor

Neratinib (HKI-272)

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
$50.00
10 mg
$75.00
25 mg
$100.00
100 mg
$220.00
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  • 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
HER2IC50: 59nM
EGFRIC50: 92nM
KDRIC50: 800nM
SrcIC50: 1.4μM
PDK-1IC50: >5μM
IKK2IC50: >9μM
CDK2/CyclinEIC50: >18μM
CDK1/CyclinB1IC50: >18μM
C-Raf/MEK1IC50: >18μM
Tpl-2IC50: >18μM
AktIC50: >20μM
c-MetIC50: >35μM
MK2IC50: >45μM
CDK4/CyclinD1IC50: >50μM
In vitro (25°C) DMSO 2 mg/mL (3.59 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 5 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.
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.

Catalog Num A10638
Actions Inhibitor
M. Wt 557.0
Formula C30H29ClN6O3
Solubility DMSO>4mg/mL Water<1mg/mL Ethanol>2mg/mL
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 698387-09-6
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

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