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Cat. No. M3492
CYT997 Structure


Size Price Availability Quantity
5mg USD 105  USD105 In stock
10mg USD 185  USD185 In stock
25mg USD 360  USD360 In stock
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Quality Control & Documentation
Biological Activity

CYT997, a synthetic small molecule optimized for antiproliferative activity in a panel of cell-based assays, in which the compound shows an IC50 of between 1 and 100 nmol/L across a panel of cancer cell lines. The compound inhibits the polymerization of tubulin with an IC50 of ~3 μmol/L.CYT997 causes a significant increase of cells in the G2-M phase of the cell cycle.Caspase-3 activation is also observed in cells treated with CYT997 along with the generation of poly (ADP-ribose) polymerase.CYT997 exhibits vascular disrupting activity as measured in vitro by effects on the permeability of human umbilical vein endothelial cell monolayers, and in vivo by effects on tumor blood flow. CYT997 possesses a useful combination of pharmacologic and pharmacokinetic properties and has considerable potential as a novel anticancer agent.

Customer Product Validations & Biological Datas
Source J Hematol Oncol (2017). Figure 1. CYT997
Method MTS assays
Cell Lines DU145, PC3, LNCaP, and 22Rv1 cells
Concentrations 30, 60 nM
Incubation Time 48 h
Results A sharp decrease in activated STAT3 was observed in DU145 cells when exposed to CYT997
Protocol (for reference only)
Cell Experiment
Cell lines DU145, A549, Ramos, KHOS/NP, A375, HCT-15, HT1376, BT-20, A431, PA-1, U937, HepG2, TF-1, Baf3/TelJAK2, PC3, and K562
Preparation method Exposing the cells to various concentrations of CYT997 for ~72 hours. Assessing cell proliferation with either the Alamar blue or MTT assays. For MTT assays, adding 5 mg/mL of MTT to all wells, incubating plates for 6 hours at 37 °C, and then adding lysis buffer (10% SDS in 0.01 N HCl) and measuring absorbance at 620 nm in a BMG Technologies Lumistar or Polarstar plate reader. For Alamar blue assays, adding Alamar blue (10 μL/well) to each well and incubating the plates at 37 °C for 4 hours. Then measureing the fluorescence using a fluorescence plate reader with an excitation filter at 544 nm and an emission filter at 590 nm. For cell cycle analysis, cells are fixed and permeabilized with 70% ethanol in PBS and incubated at 4 °C overnight. RNase-treated samples (10 μg RNase/mL for 20 minutes at 37 °C) are stained with propidium iodide (5 μg/mL) at 4 °C for a minimum of 10 minutes. Cell cycle variables are determined by fluorescence-activated cell sorting (FACS) analysis using a Beckman-Coulter Quanta SC MPL system and analyzed using CXP Software. For apoptosis analysis, cells are detached and collected. Using the Vybrant Apoptosis Assay Kit to do Annexin staining . Storing cells on ice and analyzing on a Beckman Coulter Quanta MPL within 1 hour of preparation. Using two-channel analysis to determine Annexin V–positive cells .
Concentrations Dissolved in DMSO, final concentrations ~1 μM
Incubation time ~72 hours
Animal Experiment
Animal models Male nude mice inoculated s.c. with PC3 cells, and female BALB/c mice inoculated with 4T1 cells
Formulation Formulated in NMP/PEG300/saline
Dosages ~30 mg/kg/day
Administration Oral gavage thrice a day
Chemical Information
Molecular Weight 434.53
Formula C24H30N6O2
CAS Number 917111-44-5
Solubility (25°C) DMSO 77 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Ya Cao, et al. Mitochondrial ROS accumulation inhibiting JAK2/STAT3 pathway is a critical modulator of CYT997-induced autophagy and apoptosis in gastric cancer

[2] Zongyi Wang, et al. CYT997(Lexibulin) induces apoptosis and autophagy through the activation of mutually reinforced ER stress and ROS in osteosarcoma

[3] Xiangdong Zhao, et al. Intracellular reduction in ATP levels contributes to CYT997-induced suppression of metastasis of head and neck squamous carcinoma

[4] Yong Teng, et al. Augmentation of the anticancer activity of CYT997 in human prostate cancer by inhibiting Src activity

[5] Katherine Monaghan, et al. CYT997 causes apoptosis in human multiple myeloma

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Keywords: CYT997, Lexibulin supplier, Microtubule, inhibitors, activators

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