Chemical Information:| Product Name | Neratinib(HKI-272) |
| Molecular Formula | C30H29ClN6O3 |
| Molecular Weight | 557.04 |
| Storage | Store at -20°C |
| Targets | HER2 | EGFR | KDR | Src |
| IC50 | 59 nM | 92 nM | 800 nM | 1.4 μM |
| Dosage | ~80 mg/kg/day |
| Stability | 3 years - 20 ºC powder 6 months -80 ºC dissolved in a solvent |
| Solubility | Soluble in DMSO > 10 mM |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ºC and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20ºC for several months. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
Details:Synonyms:(E)-N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide
Description:Neratinib (HKI-272) is a highly selective inhibitor of HER2 and EGFR in a cell-free assay was 59 nM and 92 nM IC50; weak inhibition of KDR and Src, of Akt, CDK1 / 2/4, IKK- 2, MK-2, PDK1, c-Raf and c-Met is no significant inhibition.
Application:
Neratinib weak inhibition of KDR tyrosine kinase and Src, IC50 were 0.8 μM and 1.4 μM, compared with the HER-2, activity weak 14 and 24 times respectively. Neratinib effect on other wire - threonine kinases such as Akt, cyclin D1 / cdk4, cyclin E / cdk2, cyclin B1 / cdk1, IKK-2, MK-2, PDK1, c-Raf, and Tpl-2, and tyramine c-Met kinase inactive. Neratinib selective inhibition of transfection HER-2 (3T3 / neu) in 3T3 cells, also inhibit two other SK-Br-3 and BT474 cells proliferation HER-2- overexpressing, IC50 of 2-3 nM, and untransfected 3T3 cells and EGFR- and HER-2-negative MDA-MB-435 and SW620 cells compared to 230 times higher than the effect. Neratinib also EGFR- dependent inhibition of A431 cell proliferation, IC50 of 81 nM. Neratinib role in BT474 cells, reduced HER-2 receptor autophosphorylation, IC50 of 5 nM, acting on the A431 cells, decreased EGF-dependent EGFR phosphorylation, IC50 of 3 nM. Neratinib inhibition of HER-2, resulting in the downstream MAPK and Akt pathway was inhibited, IC50 of 2 nM, more effective than Trastuzumab. Neratinib role in BT474 cells, inhibition of cyclin D1 expression and Rb- susceptibility gene product phosphorylation, IC50 of 9 nM, resulting in cell cycle stopped at G1-S phase, and ultimately reduce cell proliferation.
Notification:This compound is used only for research and not for human trials!
Other Small Molecular API:| AZD9291 | 1421373-65-0 |
| E7080 | 417716-92-8 |
| Afatinib diMaleate | 439081-18-2 |
| XL184 S-MALATE | 1140909-48-3 |
| Crizotinib | 877399-52-5 |
| Axitinib | 319460-85-0 |
| WZ4002 | 1213269-23-8 |
| Vandetanib | 443913-73-3 |
| Sunitinib | 557795-19-4 |
| Regorafenib | 755037-03-7 |
| Imatinib | 152459-95-5 |
| Foretinib | 849217-64-7 |
| trametinib | 871700-17-3 |
| Tivozanib | 475108-18-0 |
| Pelitinib | 257933-82-7 |
| Cediranib | 288383-20-0 |
| Selumetinib | 606143-52-6 |
| Tozasertib | 639089-54-6 |
| CapMatinib | 1029712-80-8 |
| Amuvatinib | 850879-09-3 |
| Lestaurtinib | 111358-88-4 |
| Brivanib | 649735-46-6 |
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