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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 |
|---|---|
| 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 |
| 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. |
|||
| 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 |
| 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. |
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