Lexibulin,917111-44-5

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Lexibulin

CAS No. : 917111-44-5

MCE 国际站：Lexibulin

产品活性：Lexibulin (CYT-997) 是微管蛋白聚集强效抑制剂，对多种癌细胞的 IC50 值为 10-100n M，体外体内具有高效的细胞毒性和血管增生阻断作用。Lexibulin 可诱导细胞凋亡 (apoptosis)，并诱导 GC 细胞中的线粒体 ROS 生成。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton  |  NF-κB  |  Metabolic Enzyme/Protease  |  Immunology/Inflammation  |  Apoptosis

作用靶点：Microtubule/Tubulin  |  Reactive Oxygen Species  |  Apoptosis

In Vitro: Lexibulin (CYT-997) prevents 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. Lexibulin is also capable of reversibly disrupting the microtubule network in cells, visualized using fluorescence microscopy. Thus, treatment of A549 cells with Lexibulin (1 μM) 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 are evident, including loss of adhesion and cell rounding. The effect of 1 hour of treatment with Lexibulin is reversible and cells rapidly recovered their normal microtubule architecture. Taken together, the data indicates that Lexibulin 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 Lexibulin (1 μM) had 38% and 43% of cells in G2-M at the same time points. Furthermore, at 24 hours post-Lexibulin treatment, only 66% of total cells are 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. Consistent with the disruption of cellular tubulin, Lexibulin potently inhibits proliferation, induces cell cycle arrest and most importantly apoptosis of both human myeloma cell lines (HMCLs) and primary MM cells.

In Vivo: iIn a xenograft model using the human prostate cancer cell line PC3, oral dosing of Lexibulin (CYT-997) is initiated 13 days after cell implantation by which time palpable tumors were evident. A dose-dependent inhibition of tumor growth was apparent with Lexibulin (CYT-997), which at the highest dose was equivalent to parenterally administered paclitaxel. A single dose of Lexibulin (CYT-997) (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. Lexibulin (CYT-997) treatment (15 mg/kg/day) significantly prolongs the survival in a murine model of aggressive systemic myelomatosis.

相关产品：Covalent Screening Library Plus  |  Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Immunology/Inflammation Compound Library  |  Metabolism/Protease Compound Library  |  NF-κB Signaling Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Covalent Screening Library  |  Antioxidant Compound Library  |  Oxygen Sensing Compound Library  |  Ferroptosis Compound Library  |  Pyroptosis Compound Library  |  Cytoskeleton Compound Library  |  Orally Active Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Mitochondria-Targeted Compound Library  |  Targeted Diversity Library  |  Protein-protein Interaction Inhibitor Library  |  Heterocyclic Compound Library  |  Cell Death Library  |  MG-132  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  LY294002  |  Tamoxifen  |  Paclitaxel  |  Y-27632  |  Acetylcysteine  |  Angiotensin II human  |  2-Deoxy-D-glucose  |  Staurosporine  |  H2DCFDA  |  SB-431542  |  Actinomycin D  |  Deferoxamine mesylate  |  Bortezomib  |  5-Fluorouracil  |  Trametinib  |  Sorafenib  |  Oxaliplatin  |  Gemcitabine  |  Temozolomide  |  Rotenone  |  Mdivi-1  |  Elesclomol  |  Ruxolitinib  |  Decitabine  |  SP600125  |  MK-2206 dihydrochloride  |  Etoposide

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds