1. Protein Tyrosine Kinase/RTK
    Autophagy
    Apoptosis
  2. Bcr-Abl
    Src
    Autophagy
    Apoptosis
  3. Dasatinib

Dasatinib (Synonyms: BMS-354825)

Cat. No.: HY-10181 Purity: 99.85%
Handling Instructions

Dasatinib (BMS-354825) est un double Bcr-Abl et Src famille tyrosine kinase puissant et oralement actif avec des IC50s de 0,6 nM, 0,8 nM, respectivement. Dasatinib inhibe également Abl, Src, Fyn, c-Kit et c-KitD816V avec des IC50 de 2,8 nM, 79 nM et 37 nM, respectivement. Dasatinib induit également l'apoptose et l'autophagie. Dasatinib présente une activité puissante antitumorale et a le potentiel de traiter la leucémie myéloïde chronique (LMC).

Dasatinib (BMS-354825) ist ein hochwirksamer, ATP-kompetitiver, oral aktiver dualer Src/Bcr-Abl-Inhibitor mit starker Antitumor-Aktivität. Die Ki-Werte von 16 pM und 30 pM für Src bzw. Bcr-Abl.

Dasatinib (BMS-354825) is a potent and orally active dual Bcr-Abl and Src family tyrosine kinase inhibitor with IC50s of 0.6 nM, 0.8 nM, respectively. Dasatinib also inhibits Abl, Src, Fyn, c-Kit and c-KitD816V with IC50s of 2.8 nM, 79 nM and 37 nM, respectively. Dasatinib also induces apoptosis and autophagy. Dasatinib shows potently antitumor activity and has the potential for chronic myelogenous leukemia (CML) treatment.

For research use only. We do not sell to patients.

Dasatinib Chemical Structure

Dasatinib Chemical Structure

CAS No. : 302962-49-8

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Customer Review

Based on 37 publication(s) in Google Scholar

Other Forms of Dasatinib:

Top Publications Citing Use of Products

    Dasatinib purchased from MCE. Usage Cited in: Leukemia. 2012 Oct;26(10):2233-44.

    Drug combination effect on phosphorylation of AKT. Expression of phospho-AKT and total AKT in MOLM13 cells treated for 15 minutes with DMSO vehicle, PKC412 (2.5 nM), Dasatinib (165 nM), or a combination of both. Protein lysates are prepared from MOLM13 cells, and are analyzed via immunoblotting with antibodies to phospho-AKT and total AKT.

    Dasatinib purchased from MCE. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775.

    Changes in Bcl-2 protein expression in MCF-7 cells after treatment with NSC 105014, Dasatinib or ZD1839 alone or in combination for 12 h. Expression of Bcl-2 protein is analyzed by western blotting analysis.

    Dasatinib purchased from MCE. Usage Cited in: Biol Pharm Bull. 2017;40(10):1747-1753.

    Synergistic Decrease Bcl-2 Expression by the Combination of SAHA with Dasatinib in MCF-7 Cells.

    Dasatinib purchased from MCE. Usage Cited in: Kawasaki Medical Journal. 43(2):63-78,2017.

    Western blot analysis of effects of Dasatinib (10 or 100nM) on c-Src, p-SrcY416, FAK and p-FAKY861 expression levels in KTC-1 cells and band intensities for p-SrcY416.

    Dasatinib purchased from MCE. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109.

    YSE450-R and EC109-R cells are treated with 200 nM BIBW 2992 alone or in combination with 100 nM Dasatinib for 48 h.
    • Biological Activity

    • Purity & Documentation

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    Description

    Dasatinib (BMS-354825) is a potent and orally active dual Bcr-Abl and Src family tyrosine kinase inhibitor with IC50s of 0.6 nM, 0.8 nM, respectively. Dasatinib also inhibits Abl, Src, Fyn, c-Kit and c-KitD816V with IC50s of 2.8 nM, 79 nM and 37 nM, respectively. Dasatinib also induces apoptosis and autophagy. Dasatinib shows potently antitumor activity and has the potential for chronic myelogenous leukemia (CML) treatment[1][2].

    IC50 & Target

    Ki: 16 pM (Src), 30 pM (Bcr-Abl)[1]
    IC50: <1.0 (Bcr-Abl), 0.50 (Src), 0.40 (Lck), 0.50 (Yes), 5.0 (c-Kit), 28 (PDGFRβ), 100 (p38), 180 (Her1), 720 (Her2), 880 (FGFR-1), 1700 (MEK)[1]

    In Vitro

    Dasatinib demonstrates significant activity against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK with IC50s of <1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively[1].
    Dasatinib shows antiproliferative activities aversus K562 chronic myelogenous leukemia (CML), PC3 human prostate tumor, MDA-MB-231 human breast tumor, and WiDr human colon tumor cell lines with IC50s of <1.0 nM, 9.4 nM, 12 nM, and 52 nM, respectively[1].

    In Vivo

    Dasatinib (5 mg/kg and 50 mg/kg, qd×10d, 5 on-2 off) possesses potent antitumor activity and a high safety margin in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels[1].
    Dasatinib (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib (10 mg/kg) demonstrates favorable half-lives (t1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (Fpo) in this study is 27%[1].

    Animal Model: Nude mice bearing K562 xenografts
    Dosage: 5 mg/kg and 50 mg/kg
    Administration: Oral administration on a 5 day on and 2 day off schedule.
    Result: Showed partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed.
    Animal Model: Sprague-Dawley Rats
    Dosage: 10 mg/kg (Pharmacokinetic Analysis)
    Administration: Oral and i.v.
    Result: Cmax of 13.2 and 0.5 μM for i.v. and oral, respectively.
    Clinical Trial
    Molecular Weight

    488.01

    Formula

    C₂₂H₂₆ClN₇O₂S

    CAS No.

    302962-49-8

    SMILES

    O=C(C1=CN=C(S1)NC2=NC(C)=NC(N3CCN(CC3)CCO)=C2)NC4=C(C=CC=C4Cl)C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 35.35 mg/mL (72.44 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0491 mL 10.2457 mL 20.4914 mL
    5 mM 0.4098 mL 2.0491 mL 4.0983 mL
    10 mM 0.2049 mL 1.0246 mL 2.0491 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.85%

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    Keywords:

    DasatinibBMS-354825BMS354825BMS 354825Bcr-AblSrcAutophagyApoptosisorallyactiveantitumorantiproliferativeK562CMLPC3prostateMDA-MB-231breastWiDrcolonInhibitorinhibitorinhibit

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