CYT997 (Lexibulin)CAS# 917111-44-5 |
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Quality Control & MSDS
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| Cas No. | 917111-44-5 | SDF | Download SDF |
| PubChem ID | 11351021 | Appearance | Powder |
| Formula | C24H30N6O2 | M.Wt | 434.53 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | CYT-997 | ||
| Solubility | DMSO : ≥ 100 mg/mL (230.13 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 1-ethyl-3-[2-methoxy-4-[5-methyl-4-[[(1S)-1-pyridin-3-ylbutyl]amino]pyrimidin-2-yl]phenyl]urea | ||
| SMILES | CCCC(C1=CN=CC=C1)NC2=NC(=NC=C2C)C3=CC(=C(C=C3)NC(=O)NCC)OC | ||
| Standard InChIKey | MTJHLONVHHPNSI-IBGZPJMESA-N | ||
| Standard InChI | InChI=1S/C24H30N6O2/c1-5-8-19(18-9-7-12-25-15-18)28-22-16(3)14-27-23(30-22)17-10-11-20(21(13-17)32-4)29-24(31)26-6-2/h7,9-15,19H,5-6,8H2,1-4H3,(H2,26,29,31)(H,27,28,30)/t19-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Lexibulin(CYT-997) is a potent tubulin polymerisation inhibitor with IC50 of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo.
IC50 value: 10-100 nM(cell assay) [1]
Target: tubulin polymerisation inhibitor
in vitro: CYT997 prevented the in vitro polymerization of tubulin with an IC50 of ～3 μmol/L (compared with the half-maximal inhibitory concentration of 2 μmol/L for colchicine under identical conditions) as determined using the conventional turbidimetric assay for tubulin polymerization. CYT997 was also capable of reversibly disrupting the microtubule network in cells, visualized using fluorescence microscopy. Thus, treatment of A549 cells with CYT997 (1 μmol/L) lead to the rapid reorganization of microtubules, including the destruction of the existing microtubule network and accumulation of tubulin in plaques within the cytoplasm of some cells. After 24 hours, major alterations in cell morphology were evident, including loss of adhesion and cell rounding. The effect of 1 hour of treatment with CYT997 was reversible and cells rapidly recovered their normal microtubule architecture. Taken together, the data indicates that CYT997 belongs to the class of anticancer agents that disrupt, rather than stabilize, tubulin-containing structures. Although vehicle-treated cells show 15% and 19% in G2-M phase at 15 and 24 hours (respectively), cells treated with CYT997 (1 μmol/L) had 38% and 43% of cells in G2-M at the same time points. Furthermore, at 24 hours post-CYT997 treatment, only 66% of total cells were in the G1, S, and G2-M phases, which suggests that cells blocked at the G2-M boundary do not exit back to G1, as in the normal cell cycle, but most likely are driven towards apoptosis and cell death [1]. Consistent with the disruption of cellular tubulin, CYT997 potently inhibits proliferation, induces cell cycle arrest and most importantly apoptosis of both human myeloma cell lines (HMCLs) and primary MM cells [2].
in vivo: In a xenograft model using the human prostate cancer cell line PC3, oral dosing of CYT997 was initiated 13 days after cell implantation by which time palpable tumors were evident. A dose-dependent inhibition of tumor growth was apparent with CYT997, which at the highest dose was equivalent to parenterally administered paclitaxel. A single dose of CYT997 (7.5 mg/kg i.p.) clearly decreased blood flow in liver metastases, and a significant reduction in blood flow was present 6 hours postdose [1]. CYT997 treatment (15 mg/kg/day) significantly prolongs the survival in a murine model of aggressive systemic myelomatosis [2]. References: | |||||
CYT997 (Lexibulin) Dilution Calculator
CYT997 (Lexibulin) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3013 mL | 11.5067 mL | 23.0134 mL | 46.0267 mL | 57.5334 mL |
| 5 mM | 0.4603 mL | 2.3013 mL | 4.6027 mL | 9.2053 mL | 11.5067 mL |
| 10 mM | 0.2301 mL | 1.1507 mL | 2.3013 mL | 4.6027 mL | 5.7533 mL |
| 50 mM | 0.046 mL | 0.2301 mL | 0.4603 mL | 0.9205 mL | 1.1507 mL |
| 100 mM | 0.023 mL | 0.1151 mL | 0.2301 mL | 0.4603 mL | 0.5753 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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CYT997 is a potent microtubule polymerization inhibitor with IC50 of 10-100 nM in cancer cell lines. Phase 1/2.
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CYT997(Lexibulin) induces apoptosis and autophagy through the activation of mutually reinforced ER stress and ROS in osteosarcoma.[Pubmed:30704503]
J Exp Clin Cancer Res. 2019 Jan 31;38(1):44.
BACKGROUND: Osteosarcoma (OS) is a common malignant cancer in children and adolescents and has a cure rate that has not improved in the last two decades. CYT997 (Lexibulin) is a novel potent microtubule-targeting agent with various anticancer activities, such as proliferation inhibition, vascular disruption, and cell cycle arrest and apoptosis induction, in multiple cancers. However, the direct cytotoxic mechanisms of CYT997 have not yet been fully characterized. METHODS: We evaluated apoptosis and autophagy in human osteosarcomas after treatment with CYT997 and investigated the underlying mechanisms. To explore relationships, we used the reactive oxygen species (ROS) scavenger N-acetyl cysteine (NAC), PERK inhibitor GSK2606414, ERO1 inhibitor EN460 and mitochondrial targeted protection peptide elamipretide. BALB/c-nu mice were inoculated with 143B tumor cells to investigate the in vivo effect of CYT997. RESULTS: We explored the efficacy and mechanism of CYT997 in osteosarcoma (OS) in vitro and in vivo and demonstrated that CYT997 potently suppresses cell viability and induces apoptosis and autophagy. CYT997 triggered production of ROS and exerted lethal effects via endoplasmic reticulum (ER) stress in OS cells. NAC attenuated these effects. The PERK inhibitor GSK2606414, which can block the ER stress pathway, reduced ROS production and enhanced cell viability. Moreover, activation of ERO1 in the ER stress pathway was responsible for inducing ROS production. ROS produced by the mitochondrial pathway also aggravate ER stress. Protection of mitochondria can reduce apoptosis and autophagy. Finally, CYT997 prominently reduced tumor growth in vivo. CONCLUSIONS: This study suggests that CYT997 induces apoptosis and autophagy in OS cells by triggering mutually enhanced ER stress and ROS and may thus be a promising agent against OS.
