2. Protein Tyrosine Kinase/RTK
  3. Src Bcr-Abl
  4. Bosutinib hydrate

Bosutinib hydrate  (Synonyms: SKI-606 hydrate)

Cat. No.: HY-10158A Purity: 99.97%
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Bosutinib hydrate is an oraly activel Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively.

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

CAS No. : 918639-08-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of Bosutinib hydrate:

Bosutinib hydrate Related Antibodies

Top Publications Citing Use of Products

    Bosutinib hydrate purchased from MedChemExpress. Usage Cited in: Sci Adv. 2024 Dec 13;10(50):eadq4274.  [Abstract]

    Bright-field microscopy images of 3D sphere cultures of MIA PaCa-2R and mKRC.1 with vehicles, MRTX849, dasatinib, DGY-06-116, and Bosutinib (0.1 μM) as well as combinations, after 7 days of treatment.

    Bosutinib hydrate purchased from MedChemExpress. Usage Cited in: Sci Adv. 2024 Dec 13;10(50):eadq4274.  [Abstract]

    The combined use of Bosutinib (0.1 μM), DGY-06-116, or Dasatinib with MRTX849 demonstrated a similar synergistic effect in mKRC.1 cells.

    Bosutinib hydrate purchased from MedChemExpress. Usage Cited in: Sci Adv. 2024 Dec 13;10(50):eadq4274.  [Abstract]

    Representative images of H&E staining of the liver, lung, pancreas, and spleen from mice bearing mKRC.1 tumors, treated with either vehicle or the combination of MRTX849 and Bosutinib.

    Bosutinib hydrate purchased from MedChemExpress. Usage Cited in: Life Sci Alliance. 2022 Dec 20;6(3):e202201616.

    Primary neurons from embryo brains of of WT rats and Tspan7−/− rats at E17 were cultured for 6 d. The WT neurons were treated without or with 10 μM Bosutinib for 4 h. Then phosphorylated and total SRC, PSD95, SYN, GluR1, and GluR2 in the primary neurons were detected with Western blot.

    Bosutinib hydrate purchased from MedChemExpress. Usage Cited in: Saudi J Biol Sci. 2022 Apr;29(4):2323-2328.

    K562 cells were incubated with Bosutinib (BOS) (250 nM) in the absence or addition of Boc-D-FMK (5 μM) for up to 48 h. Cell cycle phase distribution was assessed using flow cytometry, PI labeling of total DNA content, and the Guava Cell Cycle Assay software module. Left to right; colored areas indicate sub-G1, G0/G1, S and G2/M phases.

    View All Src Isoform Specific Products:

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    Lck Fyn Blk Fgr Hck Lyn Yes SRC-3

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    Abl Bcr-Abl

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Bosutinib hydrate is an oraly activel Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively[1].

    IC50 & Target

    IC50: 314 nmol/L (Csk, Src family protein tyrosine kinases); IC50: 2.4 nmol/L(Abl kinase).
    In Vitro

    Bosutinib hydrate is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range[2].

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

    Bosutinib hydrate Related Antibodies

    Cell Proliferation Assay[2]

    Cell Line: The leukemic Bcr-Abl+ cell lines (KCL22, K562, KU812, and Lama84)
    Concentration: 0.1 μmol/L
    Incubation Time: 72 h
    Result: Inhibited several human CML derived cell lines with IC50 values ranging from 1 to 20 nmol/L.
    In Vivo

    Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) hydrate has activity against human KU812 xenografts in nude mice. Bosutinib (150 mg/kg; once daily, 5 days weekly) hydrate has activity against syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts[2].

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

    Animal Model: KU812CM L xenograft model[2]
    Dosage: 75 mg/kg twice daily or 150 mg/kg once daily
    Administration: Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily)
    Result: Had the therapeutic activity and produced a dose- and schedule-dependent weight loss.
    Animal Model: Syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts[2]
    Dosage: 150 mg/kg
    Administration: Bosutinib (150 mg/kg; once daily, 5 days weekly)
    Result: Decreased the rate of tumor growth and prolonged event-free survival of mice.
    Clinical Trial
    Molecular Weight

    548.46

    Formula

    C26H31Cl2N5O4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CN1CCN(CC1)CCCOC2=C(C=C3C(NC4=CC(OC)=C(C=C4Cl)Cl)=C(C=NC3=C2)C#N)OC.O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (182.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8233 mL 9.1164 mL 18.2329 mL
    5 mM 0.3647 mL 1.8233 mL 3.6466 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.97%

    SDS (537 KB)

    COA (251 KB) HNMR (284 KB) LCMS (103 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8233 mL 9.1164 mL 18.2329 mL 45.5822 mL
    5 mM 0.3647 mL 1.8233 mL 3.6466 mL 9.1164 mL
    10 mM 0.1823 mL 0.9116 mL 1.8233 mL 4.5582 mL
    15 mM 0.1216 mL 0.6078 mL 1.2155 mL 3.0388 mL
    20 mM 0.0912 mL 0.4558 mL 0.9116 mL 2.2791 mL
    25 mM 0.0729 mL 0.3647 mL 0.7293 mL 1.8233 mL
    30 mM 0.0608 mL 0.3039 mL 0.6078 mL 1.5194 mL
    40 mM 0.0456 mL 0.2279 mL 0.4558 mL 1.1396 mL
    50 mM 0.0365 mL 0.1823 mL 0.3647 mL 0.9116 mL
    60 mM 0.0304 mL 0.1519 mL 0.3039 mL 0.7597 mL
    80 mM 0.0228 mL 0.1140 mL 0.2279 mL 0.5698 mL
    100 mM 0.0182 mL 0.0912 mL 0.1823 mL 0.4558 mL
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    Bosutinib hydrate Related Classifications

    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.

    Keywords:

    Bosutinib918639-08-4SKI-606SKI606SKI 606SrcBcr-AblOralSrc/Abl tyrosine kinase inhibitorcancerInhibitorinhibitorinhibit

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