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Dasatinib (BMS-354825)

Catalog No. S1021 5 5 10 Customer Review(s) Product Citations26 Product Citation(s)
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Dasatinib (BMS-354825) Chemical Structure

Bio Information

Dasatinib (BMS-354825) is an ATP-competitive, dual SRC/ABL inhibitor. Dasatinib is a potent inhibitor of imatinib-resistant KIT activation loop mutants and induces apoptosis in mast cell and leukemic cell lines expressing these mutations. Dasatinib sensitively inhibits all members of the Src family, including c-Src, Lck, Fyn, and Yes (IC50 < 1.1nmol/L). At higher concentrations (3 to 28 nmol/L), dasatinib also inhibits the Src kinases Abl, c-Kit, PDGFR, and EphA2. [1]

References:

[1] Clinical Cancer Research October 2005;11;6924

Chemical Information

Molecular Weight (WM): 488.01
Formula:

C22H26ClN7O2S
Solubility(R.T.:25°C): DMSO 98mg/mL 
Water <1mg/mL 
Ethanol <1mg/mL 

Quality Control

View current batch:
H-NMR HPLC H-NMR HPLC H-NMR HPLC H-NMR HPLC H-NMR HPLC H-NMR HPLC

Research Area

Angiogenesis >> Src >> Src Inhibitors

Recommended Screening Libraries

Related Inhibitors

Information  
Axitinib (AG-013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.
  • 50mg
  • $ 70
  • 100mg
  • $ 120
Saracatinib (AZD0530) is a Src inhibitor for c-Src and v-Abl with IC50 of 2.7 nM and 30 nM, respectively.
  • 10mg
  • $ 70
  • 25mg
  • $ 170
Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM, respectively.
  • 10mg
  • $ 70
  • 50mg
  • $ 270
Dovitinib (TKI258, CHIR258) is a novel multi-target inhibitor for Flt3, c-Kit, FGFR1/3, VEGFR1/2/3, PDGFRα/β with IC50 of 1 nM, 2 nM, 8 nM/9 nM and 10 nM/13 nM/8 nM, 210 nM/27 nM respectively.
  • 10mg
  • $ 170
  • 25mg
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Imatinib Mesylate is orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively.
  • 100mg
  • $ 147
  • 250mg
  • $ 220

Related Antibodies

Information  
Reactivity: 薛亚红

Dasatinib (BMS-354825) has been referenced in 26 publications.

Decoupling of tumor-initiating activity from stable immunophenotype in HoxA9-Meis1-driven AML.
Dasatinib inhibits proinflammatory functions of mature human neutrophils.
Combinatory action of VEGFR2 and MAP kinase pathways maintains endothelial-cell integrity.
STAT5A-mediated SOCS2 expression regulates Jak2 and STAT3 activity following c-Src inhibition in head and neck squamous carcinoma.
Dasatinib plus Nutlin-3 shows synergistic antileukemic activity in both p53wild-type and p53mutated B chronic lymphocytic leukemias by inhibiting the Akt pathway.
Azacytidine and erlotinib exert synergistic effects against acute myeloid leukemia.
Exosomes released by K562 chronic myeloid leukemia cells promote angiogenesis in a src-dependent fashion.
Andes virus infection of lymphatic endothelial cells causes giant cell and enhanced permeability responses that are rapamycin and vascular endothelial growth factor C sensitive.
VEGFR2 and Src kinase inhibitors suppress Andes virus-induced endothelial cell permeability.
MCL1 down-regulation plays a critical role in mediating the higher anti-leukaemic activity of the multi‐kinase inhibitor Sorafenib with respect to Dasatinib.
Role of E-cadherin in antimigratory and antiinvasive efficacy of silibinin in prostate cancer cells.
Tyrosine kinase inhibitors for the treatment of acute myeloid leukemia: delineation of anti-leukemic mechanisms of action.
Cyclophilin D Extramitochondrial Signaling Controls Cell Cycle Progression and Chemokine-Directed Cell Motility.
Role of increased guanosine triphosphate cyclohydrolase-1 expression and tetrahydrobiopterin levels upon T cell activation.
Effects of the hedgehog inhibitor GDC-0449, alone or in combination with dasatinib, on BCR-ABL-positive leukemia cells.
Molecular characterization of c-Abl/c-Src kinase inhibitors targeted against murine tumour progenitor cells that express stem cell markers.
The immune inhibitory receptor osteoactivin is upregulated in monocyte-derived dendritic cells by BCR–ABL tyrosine kinase inhibitors.
Intracellular Retention of ABL Kinase Inhibitors Determines Commitment to Apoptosis in CML Cells.
p38α MAP Kinase Dimers with Swapped Activation Segments and a Novel Catalytic Loop Conformation.
Dasatinib, a small molecule inhibitor of the Src kinase, reduces the growth and activates apoptosis in pre-neoplastic Barrett's esophagus cell lines: Evidence for a noninvasive treatment of high-grade dysplasia.
Anti-leukemic activity of Dasatinib in both p53wild-type and p53mutated B malignant cells.
Novel, activating KIT-N822I mutation in familial cutaneous mastocytosis.
Amplification of CRKL Induces Transformation and Epidermal Growth Factor Receptor Inhibitor Resistance in Human Non-Small Cell Lung Cancers.
Direct effect of dasatinib on proliferation and cytotoxicity of natural killer cells in in vitro study.
Development and Validation of a High-Throughput Intrinsic ATPase Activity Assay for the Discovery of MEKK2 Inhibitors.
High-performance liquid chromatography with ultraviolet detection and protein precipitation as a way of quantitative determination of nilotinib with and without internal …

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Average Customer Review

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  • Data from [Invest New Drugs 2010;30(1), 417-422]
    Dasatinib (BMS-354825) purchased from Selleck


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  • Data from [Biochem Pharmacol 2011;82(10), 1457-1466]
    Dasatinib (BMS-354825) purchased from Selleck


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  • Data from [Invest New Drugs 2010;30(1), 417-422]
    Dasatinib (BMS-354825) purchased from Selleck


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  • Data from [Invest New Drugs 2010;30(1), 417-422]
    Dasatinib (BMS-354825) purchased from Selleck


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  • Data from [Clin Cancer Res 2011;17, 762-770]
    Dasatinib (BMS-354825) purchased from Selleck


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  • Data from [Clin Cancer Res 2011;17, 762-770]
    Dasatinib (BMS-354825) purchased from Selleck


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  • Data from [Clin Cancer Res 2011;17, 762-770]
    Dasatinib (BMS-354825) purchased from Selleck


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  • ;Dr Thomas Kruwel of Fraunhofer-Institute for Toxicology and Experimental Medicine-Dasatinib (BMS-354825) purchased from Selleck
    Dasatinib (BMS-354825) purchased from Selleck


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  • Data from [Biochem Pharmacol 2011;82(10), 1457-1466]
    Dasatinib (BMS-354825) purchased from Selleck


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  • Data from [Cell Res 2011;21, 1080-1087]
    Dasatinib (BMS-354825) purchased from Selleck

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Data from [Invest New Drugs 2010;30(1), 417-422]


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Data from [Biochem Pharmacol 2011;82(10), 1457-1466]

+ See All 10 Customer Reviews of Dasatinib (BMS-354825)

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