4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}benzamide
Nilotinib & its intermediates
CAS: 641571-10-0
Molecular Formula: C28H22F3N7O
4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}benzamide - Names and Identifiers
4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}benzamide - Physico-chemical Properties
| Molecular Formula | C28H22F3N7O |
| Molar Mass | 529.52 |
| Density | 1.36 |
| Melting Point | 231-233 °C |
| Solubility | Soluble in DMSO (up to 50 mg/ml) |
| Appearance | Beige powder. |
| Color | Off-white |
| Storage Condition | -20°C Freezer |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| Refractive Index | 1.65 |
| Use | Intermediate |
| In vitro study | Nilotinib acts on activated HSCs, inhibiting proliferation, migration, and actin formation, as well as α-SMA and collagen expression. Nilotinib induced apoptosis in HSCs, associated with decreased bcl-2 expression, increased p53 expression, PARP cleavage, and increased PPARγ and TRAIL-R expression. Nilotinib also induced cell cycle arrest with increased expression of p27 and downregulation of cyclin D1. Nilotinib not only inhibits PDGFR activation, but also TGFRII via Src. Nilotinib significantly inhibited PDGF-and TGFβ-stimulated ERK and Akt phosphorylation. Furthermore, Nilotinib acts on human HSCs to inhibit PDGF and TGF β-activated phosphorylated forms of Abl. Nilotinib inhibits most Imatinib-resistant BCR-ABL mutations, except for T315I. Nilotinib inhibits PDGF-DD-regulated ERK1/2 activation, basic and PDGF-DD-regulated PDGFR-β and AKT activation, and schwannoma cell proliferation. Nilotinib is more potent than Imatinib, exerting its maximum inhibitory effect at concentrations lower than steady-state plasma levels. Nilotinib also significantly reduced TGF-β1 and platelet-derived growth factor (PDGF) gene expression levels. Nilotinib treatment also significantly inhibited PDGF-induced lung fibroblast proliferation. |
| In vivo study | Nilotinib acts on CCl 4 and BDL-induced fibrosis, reducing collagen deposition and α-SMA expression. Nilotinib can induce apoptosis of HSC, which is related to the down-regulation of bcl-2. Nilotinib light lung injury and degree of fibrosis. Nilotinib therapy significantly reduced hydroxyproline levels on days 14 and 21, accompanied by reduced levels of transforming growth factor (TGF)-β1 and PDGFR-β expression. |
4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}benzamide - Risk and Safety
| HS Code | 29335990 |
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Product Name: Nilotinib Visit Supplier Webpage Request for quotationCAS: 641571-10-0
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: Nilotinib & its intermediates Request for quotation
CAS: 641571-10-0
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
CAS: 641571-10-0
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
Spot supply
Product Name: Nilotinib (AMN-107) Visit Supplier Webpage Request for quotationCAS: 641571-10-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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