CAS NO: | 71203-35-5 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 407.49 |
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Formula | C22H21N3O3S |
CAS No. | 71203-35-5 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 81 mg/mL (198.8 mM) |
Water: <1 mg/mL | |
Ethanol: <1 mg/mL | |
Solubility (In vivo) | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 10mg/mL |
Synonyms | CID-2950007; ML-141; CID2950007; ML 141; CID 2950007; ML141 |
In Vitro | In vitro activity: ML141 enhances the ability of TMX to suppress BLBC cell growth through both induction of cell death and suppression of cell division. ML141 also significantly protects neuroblastoma cells from metformin-induced apoptosis. Moreover, ML141 diminishes K. pneumoniae invasion in a dose-dependent manner. Kinase Assay: Wild-type GST-Cdc42 (4 μM) is bound to GSH-beads overnight at 4°C. Cdc42 on GSH-beads is depleted of nucleotide by incubating with 10 mM EDTA containing buffer for 20 min at 30°C, washing twice with NP- HPS buffer, then re-suspended in the same buffer containing 1 mM EDTA/or 1 mM MgCl2, 1 mM DTT and 0.1% BSA. Cdc42 unbound sites are blocked by incubation of protein–bead complex for 15 min at RT. Thirty μL of this suspension is incubated with 20 mM inhibitor for 3 min at RT and added 30 μL of various concentrations of ice cold BODIPY-FL-GTP. Samples incubated at 4° C for 45 min and binding of fluorescent nucleotide to enzyme is measured using an Accuri flow cytometer. Raw data are exported and plotted using GraphPad Prism software. Cell Assay: Cells [Basal-B (MDA-MB 231 and HCC38) and Basal-A with HER2 amplification (HCC1954) cells] are incubated with 500 nM Calcein-AM and 1 μM PI for 15 min, after which live cells and dead cells (represented by positivity of Calcein-AM and PI staining, respectively) are counted utilizing the adherent cell Celigo(TM) cytometer. |
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In Vivo | In NOD/SCID mice bearing MDA-MB 231 derived tumors, ML141 (1 mg/day i.p.), via inhibition of Cdc42, enables TMX to suppress growth of MDA-MB 231 derived tumors. In addition, ML141 (10 mg/kg i.p.) enhances G-CSF-induced hematopoietic stem and progenitor cell mobilization in mice. |
Animal model | NOD/SCID mice bearing MDA-MB 231 derived tumors |
Formulation & Dosage | Dissolved in Corn oil; 1 mg/kg daily; i.p. injection |
References | Oncotarget. 2014 Nov 30;5(22):11709-22; EMBO Mol Med. 2013 May;5(5):723-36. |