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

Dasatinib hydrochloride  (Synonyms: BMS-354825 hydrochloride)

Cat. No.: HY-10181A Purity: 98.86%
COA Handling Instructions

Dasatinib hydrochloride (BMS-354825 hydrochloride) est un inhibiteur double de Src/Bcr-Abl qui est très puissant, l'ATP compétitif, oralement actif, avec Ki des valeurs de 16 pM et 30 pM pour Src et Bcr-Abl, respectivement. Dasatinib hydrochloride a une activité puissante antitumorale.

Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride also induces apoptosis and autophagy.

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

Dasatinib hydrochloride Chemical Structure

Dasatinib hydrochloride Chemical Structure

CAS No. : 854001-07-3

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10 mM * 1 mL in DMSO USD 73 In-stock
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Customer Review

Based on 76 publication(s) in Google Scholar

Other Forms of Dasatinib hydrochloride:

Top Publications Citing Use of Products

70 Publications Citing Use of MCE Dasatinib hydrochloride

WB
IF

    Dasatinib hydrochloride purchased from MCE. Usage Cited in: Nat Cell Biol. 2023 Mar;25(3):493-507.  [Abstract]

    Dasatinib (50 nM; 24 or 48 h) significantly decreases MED8A and D458 cell migration.

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

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

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

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

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

    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 hydrochloride 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 hydrochloride purchased from MCE. Usage Cited in: Leukemia. 2012 Oct;26(10):2233-44.  [Abstract]

    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.

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    Description

    Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively[1]. Dasatinib hydrochloride also induces apoptosis and autophagy.

    IC50 & Target[1]

    Bcr-Abl

    1.0 nM (IC50)

    Src

    0.5 nM (IC50)

    lck

    0.4 nM (IC50)

    Yes

    0.5 nM (IC50)

    c-kit

    5.0 nM (IC50)

    PDGFRβ

    28 nM (IC50)

    p38

    100 nM (IC50)

    Her1

    180 nM (IC50)

    Her2

    710 nM (IC50)

    FGFR-1

    880 nM (IC50)

    MEK

    1700 nM (IC50)

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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

    524.47

    Appearance

    Solid

    Formula

    C22H27Cl2N7O2S
    CAS No.
    SMILES

    O=C(C1=CN=C(S1)NC2=NC(C)=NC(N3CCN(CC3)CCO)=C2)NC4=C(C=CC=C4Cl)C.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
    Solvent & Solubility
    In Vitro: 

    DMSO : 15 mg/mL (28.60 mM; Need ultrasonic and warming)

    H2O : 10 mg/mL (19.07 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9067 mL 9.5334 mL 19.0669 mL
    5 mM 0.3813 mL 1.9067 mL 3.8134 mL
    10 mM 0.1907 mL 0.9533 mL 1.9067 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: ≥ 3.33 mg/mL (6.35 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 3.33 mg/mL (6.35 mM); Clear solution

    • 3.

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

      Solubility: ≥ 3.33 mg/mL (6.35 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 98.86%

    COA (247 KB) LCMS (122 KB)

    Handling Instructions (2659 KB)
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Dasatinib854001-07-3BMS-354825BMS354825BMS 354825Bcr-AblSrcAutophagyApoptosisorallyactiveantitumorantiproliferativeK562CMLPC3prostateMDA-MB-231breastWiDrcolonInhibitorinhibitorinhibit

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