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

Dasatinib hydrochloride (Synonyms: BMS-354825 hydrochloride)

Cat. No.: HY-10181A Purity: 98.86%
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 hydrochloride (BMS-354825 hydrochloride) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor, with Ki values of 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride has potent antitumor activity.

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

Dasatinib hydrochloride Chemical Structure

Dasatinib hydrochloride Chemical Structure

CAS No. : 854001-07-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1  mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
100 mg USD 66 In-stock
Estimated Time of Arrival: December 31
200 mg USD 78 In-stock
Estimated Time of Arrival: December 31
500 mg USD 118 In-stock
Estimated Time of Arrival: December 31
1 g   Get quote  
5 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 37 publication(s) in Google Scholar

Other Forms of Dasatinib hydrochloride:

Top Publications Citing Use of Products

    Dasatinib hydrochloride 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.

    Dasatinib hydrochloride 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 hydrochloride 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 hydrochloride 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 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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Dasatinib hydrochloride (BMS-354825 hydrochloride) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor, with Ki values of 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride has potent antitumor activity[1].

    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

    524.47

    Formula

    C₂₂H₂₇Cl₂N₇O₂S

    CAS No.

    854001-07-3

    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 provided by MCE.
    References

    Purity: 98.86%

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

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

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Dasatinib hydrochloride
    Cat. No.:
    HY-10181A
    Quantity:
    MCE Japan Authorized Agent: