Name: Dasatinib (BMS-354825)
Price: 188.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Dasatinib is a small-molecule inhibitor of both the Src and Bcr-Abl tyrosine kinases with IC50 values of 0.5 nM and 1 nM. The oncogenic tyrosine kinase Bcr-Abl, plays a critical role in the pathogenesis of CML (chronic myelogenous leukemia). In most CML patients, the kinase domain of Bcr-Abl have mutations that interfere with binding to the first Abl kinase inhibitor, but Dasatinib bind more efficiently to these Abl kinase mutations and thus more effective than imatinib in inhibiting the proliferation cells with wild-type Bcr-Abl or Bcr-Abl mutants.
- Properties
  - Alternative Name
    
    Sprycel,dasatinibum,Dasatinib,BMS-354825, BMS354825, BMS 354825; N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide
    
    CAS Number
    
    302962-49-8
    
    Molecular Formula
    
    C22H26ClN7O2S
    
    Molecular Weight
    
    488.01
    
    Appearance
    
    A solid
    
    Purity
    
    99.86%
    
    Solubility
    
    ≥24.4 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Panneerselvam Jayabal, Fuchun Zhou, et al. "NELL2-cdc42 signaling regulates BAF complexes and Ewing sarcoma cell growth." Cell Rep. 2021 Jul 6;36(1):109254. PMID:34233189
    2. Bhola PD, Ahmed E, et al. "High-throughput dynamic BH3 profiling may quickly and accurately predict effective therapies in solid tumors." Sci Signal. 2020;13(636):eaay1451. PMID:32546544
    3. Panagi I, Jennings E, et al. "Salmonella Effector SteE Converts the Mammalian Serine/Threonine Kinase GSK3 into a Tyrosine Kinase to Direct Macrophage Polarization." Cell Host Microbe. 2020;27(1):41–53.e6. PMID:31862381
    4. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID:31063758
    5. Alzubi MA, Turner TH, et al. "Separation of breast cancer and organ microenvironment transcriptomes in metastases." Breast Cancer Res. 2019 Mar 6;21(1):36. PMID:30841919
    6. Cheriyan VT, Alsaab H, et al. "A CARP-1 functional mimetic compound is synergistic with BRAF-targeting in non-small cell lung cancers." Oncotarget. 2018 Jul 3;9(51):29680-29697. PMID:30038713
    7. Singleton KR, Crawford L, et al. "Melanoma Therapeutic Strategies that Select against Resistance by Exploiting MYC-Driven Evolutionary Convergence." Cell Rep. 2017 Dec 5;21(10):2796-2812. PMID:29212027
    8. Qian XL, Zhang J, et al."Dasatinib inhibits c-src phosphorylation and prevents the proliferation of Triple-Negative Breast Cancer (TNBC) cells which overexpress Syndecan-Binding Protein (SDCBP)." PLoS One. 2017 Jan 31;12(1):e0171169. PMID:28141839