Neratinib Maleate
CAS No. 915942-22-2
Neratinib Maleate( —— )
Catalog No. M21827 CAS No. 915942-22-2
Irreversible ErbB receptor tyrosine kinase inhibitor.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
Size | Price / USD | Stock | Quantity |
100MG | Get Quote | In Stock |
|
200MG | Get Quote | In Stock |
|
500MG | Get Quote | In Stock |
|
1G | Get Quote | In Stock |
|
Biological Information
-
Product NameNeratinib Maleate
-
NoteResearch use only, not for human use.
-
Brief DescriptionIrreversible ErbB receptor tyrosine kinase inhibitor.
-
DescriptionIrreversible ErbB receptor tyrosine kinase inhibitor.(In Vitro):Neratinib displays no activity against other serine-threonine kinases such as Akt, cyclin D1/cdk4, cyclin E/cdk2, cyclin B1/cdk1, IKK-2, MK-2, PDK1, c-Raf, and Tpl-2, as well as the tyrosine kinase c-Met.Neratinib (0.5 ng/mL–5 μg/mL, 2 days) inhibits the proliferation of cell lines that show high levels of HER-2 (3T3/neu, SK-Br-3, and BT474) and is much less active in cell lines that express neither HER-2 nor EGFR (3T3, MDA-MB-435, and SW620) .Neratinib (0-2 nM, 12-16 h) arrests BT474 cell cycle at G1-S phase.Neratinib results in the inhibition of MAPK and Akt phosphorylation, down-regulation of cyclin D1 levels, and induction of p27.(In Vivo):Neratinib (HKI-272) (0-80 mg/kg/day; i.g.; 42 days) shows anticancer activities against cancer cells that expresses high levels of HER-2 or EGFR.
-
In VitroNeratinib displays no activity against other serine-threonine kinases such as Akt, cyclin D1/cdk4, cyclin E/cdk2, cyclin B1/cdk1, IKK-2, MK-2, PDK1, c-Raf, and Tpl-2, as well as the tyrosine kinase c-Met.Neratinib (0.5 ng/mL–5 μg/mL, 2 days) inhibits the proliferation of cell lines that show high levels of HER-2 (3T3/neu, SK-Br-3, and BT474) and is much less active in cell lines that express neither HER-2 nor EGFR (3T3, MDA-MB-435, and SW620) .Neratinib (0-2 nM, 12-16 h) arrests BT474 cell cycle at G1-S phase.Neratinib results in the inhibition of MAPK and Akt phosphorylation, down-regulation of cyclin D1 levels, and induction of p27. Cell Proliferation Assay Cell Line:3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620 Concentration:0.5 ng/mL–5 μg/mL Incubation Time:2 days (6 days for BT474)Result:Inhibited cell proliferation with IC50 values of 700 ± 78, 3 ± 0.14, 2 ± 0.18, 2 ± 0.06, 81± 9, 960 ± 165 and 690 ± 84 nM against 3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620 cells, respectively.Western Blot Analysis Cell Line:BT474 or A431 cells Concentration: 0, 2, 10, 50, 100 and 200 nM Incubation Time:3 h Result:Decreased ligand-independent receptor phosphorylation by 50% (IC50) at 5 nM in BT474 cells, repressed EGF-dependent phosphorylation of EGFR in A431 cells at a comparable dose (IC50 = 3 nM). Effectively repressed phosphorylation of MAPK and Akt in BT474 cells.Cell Cycle Analysis Cell Line:BT474 Concentration:0–2 nM Incubation Time:12–16 h Result:Blocked cell cycle progression, causing a G1-S arrest, a 50% decrease in the number of cells in the S (DNA synthesis) phase of the cell cycle was observed at a concentration of 2 nM.
-
In VivoNeratinib (HKI-272) (0-80 mg/kg/day; i.g.; 42 days) shows anticancer activities against cancer cells that expresses high levels of HER-2 or EGFR. Animal Model:Female athymic (nude) mice, tumor xenograft Dosage:10, 20, 40, 60 or 80 mg/kg/day Administration:Gavage, 42 days Result:Reduced tumor growth in a dose-dependent manner in 3T3/neu, BT474, SK-OV-3 and A431 xenografts, but was o inactive in xenografts of MX-1 and MCF-7. Inhibited phosphorylation of HER-2 in BT474 xenografts.
-
Synonyms——
-
PathwayOthers
-
TargetOther Targets
-
Recptor——
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number915942-22-2
-
Formula Weight673.11
-
Molecular FormulaC30H29ClN6O3·C4H4O4
-
Purity>98% (HPLC)
-
SolubilityIn Vitro:?DMSO : 250 mg/mL (371.41 mM)
-
SMILES——
-
Chemical Name(E)-N-[4-[3-Chloro-4-[(2-pyridinyl)methoxy]anilino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide maleate
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
molnova catalog
related products
-
Asperuloside
Asperuloside has anti-inflammatory activity.
-
Soyasaponin II
Soyasaponin II has antiviral effects, it can inhibit the replication of human cytomegalovirus, influenza virus, and human immunodeficiency virus type 1.
-
2-Hydroxypropiopheno...
2'-Hydroxypropiophenone is an agent that is derivatized salicylaldoxime.