CYT997 (Lexibulin)
CYT997 (Lexibulin)
CAS: 917111-44-5
Molecular Formula: C24H30N6O2
CYT997 (Lexibulin) - Names and Identifiers
| Name | CYT997 (Lexibulin) |
| Synonyms | CYT997 CS-347 CYT-997 CYT 997 Lexibulin LEXIBULIN. CYT997 (Lexibulin) 1-ethyl-3-(2-methoxy-4-(5-methyl-4-((S)-1-(pyridin-3-yl)butylamino)pyrimidin-2-yl)phenyl)urea (S)-1-ethyl-3-(2-methoxy-4-(5-methyl-4-((1-(pyridin-3-yl)butyl)amino)pyrimidin-2-yl)phenyl)urea N-Ethyl-N'-[2-methoxy-4-[5-methyl-4-[[(1S)-1-(3-pyridinyl)butyl]amino]-2-pyrimidinyl]phenyl]urea |
| CAS | 917111-44-5 |
| EINECS | 604-604-1 |
CYT997 (Lexibulin) - Physico-chemical Properties
| Molecular Formula | C24H30N6O2 |
| Molar Mass | 434.53 |
| Density | 1.195 |
| Boling Point | 546.9±50.0 °C(Predicted) |
| pKa | 14.01±0.70(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | CYT997(1 μm) treatment of A549 cells for 24 hours induced rapid microtubule recombination, including disruption of the existing microtubule network and accumulation of some cytoplasmic tubulin in the plaque, this results in significant changes in cell morphology, including loss of adherent cells and cell reduction. CYT997 is toxic to 16 cancer cells, and IC50 ranges from 9 nM for HepG2 cells to 101 nM for KHOS/NP cells. CYT997 effectively acts on HCT15 cells and has a multi-drug resistance mechanism Pgp(MDR is consistent with CYT997 destroying cell tubulin, CYT997 effectively inhibits proliferation, induces cell cycle arrest, and induces human bone marrow cell line (HMCLs) and apoptosis of primary MM cells. |
| In vivo study | The Half-Life of cyto997 in rats treated orally (2.5 hours) is slightly longer than that of intravenous injection (1.5 hours), and the absolute oral bioavailability is 50% to 70%. CYT997 Oral treatment of mice bearing PC3 xenografts, compared with Paclitaxel, more effective in inhibiting tumor growth, this effect is dose-dependent. CYT997 was also effective in homotopic models carrying mouse breast cancer 4T1 cells, some of which were treated with anti-Paclitaxel. CYT997 administered intraperitoneally to liver metastases at a dose of 7.5 mg/kg significantly reduced blood flow at 6 hours to a similar extent to the positive control treated with CA4P at a dose of 100 mg/kg. Consistent with in vitro anti-Myeloma activity, CYT997 treatment at a dose of 15 mg/kg per day in a mouse model of activated systemic myeloid leukemia significantly prolonged life. |
CYT997 (Lexibulin) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.301 ml | 11.507 ml | 23.013 ml |
| 5 mM | 0.46 ml | 2.301 ml | 4.603 ml |
| 10 mM | 0.23 ml | 1.151 ml | 2.301 ml |
| 5 mM | 0.046 ml | 0.23 ml | 0.46 ml |
Last Update：2024-01-02 23:10:35
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Mobile: 18021002903
QQ: 3008007409
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