Nilotinib & its intermediates
Nilotinib & its intermediates
CAS: 641571-10-0
Molecular Formula: C28H22F3N7O
Nilotinib & its intermediates - Names and Identifiers
Nilotinib & its intermediates - 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. |
Nilotinib & its intermediates - Risk and Safety
| HS Code | 29335990 |
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