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

Dasatinib hydrochloride (Synonyms: BMS 354825 hydrochloride)

Cat. No.: HY-10181A Purity: 98.84%
Handling Instructions

Dasatinib hydrochloride is a potent and dual AblWT/Src inhibitor IC50 of 0.6 nM/0.8 nM respectively; also inhibits c-KitWT/c-KitD816V with IC50 of 79 nM/37 nM.

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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100 mg USD 66 In-stock
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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 Afatinib 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 Cladribine, Dasatinib or Gefitinib 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 Vorinostat 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

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Dasatinib hydrochloride is a potent and dual AblWT/Src inhibitor IC50 of 0.6 nM/0.8 nM respectively; also inhibits c-KitWT/c-KitD816V with IC50 of 79 nM/37 nM.

    IC50 & Target

    IC50: 0.6 nM/0.8 nM (AblWT/Src)[1]
    IC50: 79 nM/37 nM (c-KitWT/c-KitD816V)[2]

    In Vitro

    Dasatinib potently inhibits wild-type Abl kinase and all mutants except T315I over a narrow range (IC50≤1.7 nM). Dasatinib (IC50: 0.8 nM) displays 325-fold greater potency compared with Imatinib against cells expressing wild-type Bcr-Abl in Ba/F3 cells[1].

    In Vivo

    Daily treatment with Dasatinib (50 mg/kg) is initiated on day 10. Using this approach, a significant inhibition of BCPAP orthotopic tumor growth is observed 6 days after treatment (day 16, P=0.014), which is sustained through days 23 and 29 (P=0.0003), compared with vehicle-treated mice[3]. Metabolism studies of Dasatinib (50 mg/kg) in rat suggested that Dasatinib is the major circulating component, whereas multiple metabolites contributed to the remaining 40-60% of the sample radioactivity at 4 h post dose[4].

    Clinical Trial
    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 : 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.
    References
    Kinase Assay
    [1]

    Kinase assays using wild-type and mutant glutathione S-transferase (GST)-Abl fusion proteins (c-Abl amino acids 220-498) are done with minor alterations. GST-Abl fusion proteins are released from glutathione-Sepharose beads before use; the concentration of ATP is 5 μM. Immediately before use in kinase autophosphorylation and in vitro peptide substrate phosphorylation assays, GST-Abl kinase domain fusion proteins are treated with LAR tyrosine phosphatase. After 1-hour incubation at 30°C, LAR phosphatase is inactivated by addition of sodium vanadate (1 mM). Immunoblot analysis comparing untreated GST-Abl kinase to dephosphorylated GST-Abl kinase is routinely done using phosphotyrosine-specific antibody 4G10 to confirm complete (>95%) dephosphorylation of tyrosine residues and c-Abl antibody CST 2862 to confirm equal loading of GST-Abl kinase. The inhibitor concentration ranges for IC50 determinations are 0 to 5,000 nM (Imatinib and AMN107) or 0 to 32 nM (Dasatinib). The Dasatinib concentration range is extended to 1,000 nM for mutant T315I. These same inhibitor concentrations are used for the in vitro peptide substrate phosphorylation assays. The three inhibitors are tested over these same concentration ranges against GST-Src kinase and GST-Lyn kinase.

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

    Cell Assay
    [1]

    Ba/F3 cell lines are plated in triplicate and incubated with escalating concentrations of Imatinib, AMN107, or Dasatinib for 72 hours. Proliferation is measured using a methanethiosulfonate-based viability assay (CellTiter96 Aqueous One Solution Reagent). IC50 and IC90 values are reported as the mean of three independent experiments done in quadruplicate. The inhibitor concentration ranges for IC50 and IC90determinations are 0 to 2,000 nM (Imatinib and AMN107) or 0 to 32 nM (Dasatinib). The imatinib concentration range is extended to 6,400 nM for mutants with IC50>2,000 nM. The Dasatinib concentration range is extended to 200 nM for mutant T315I.

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

    Animal Administration
    [3][4]

    Mice[3]
    Male athymic nude mice (25 grams; 5-week old) are used. Dasatinib (50 mg/kg) is prepared for daily oral gavage (5 d/wk) in 80 mM sodium citrate buffer, pH 3.0. For the orthotopic murine model, mice are randomized on day 10 based on bioluminescence activity to receive drug or vehicle. In the metastatic murine model, mice receives dasatinib or vehicle, as described earlier, starting 2 days before intracardiac injection (pretreatment), or on day 11 following randomization (posttreatment).
    Rats[4]
    Dasatinib is dosed to male Wistar-Han (WH) rats at 50 mg/kg orally in 0.5% methylcellulose. The automated rat blood collection device is programmed to collect 200 μL of blood at predetermined intervals. At each time point, the accusampler is programmed to directly spot 20 μL of blood twice (two spots) onto the DBS card. The remaining 160 μL of liquid blood is collected into sodium EDTA-containing tubes. Plasma samples are obtained after immediate centrifugation of blood at 11,000 rpm for 5 min. The plasma samples are stored at −80°C until analyses. The DBS samples are dried under room temperature for a minimum of 2 h and stored in a plastic bag in the dessicator until sample analysis.

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

    References
    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

    Purity: 98.84%

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    Product Name:
    Dasatinib hydrochloride
    Cat. No.:
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    Dasatinib hydrochloride

    Cat. No.: HY-10181A