2. Protein Tyrosine Kinase/RTK
  3. c-Met/HGFR TAM Receptor
  4. BMS 777607

BMS 777607  (Synonyms: BMS 817378)

Cat. No.: HY-12076 Purity: 99.33%
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BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases.

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

BMS 777607 Chemical Structure

BMS 777607 Chemical Structure

CAS No. : 1025720-94-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 105 In-stock
Solution
10 mM * 1 mL in DMSO USD 105 In-stock
Solid
1 mg USD 37 In-stock
5 mg USD 92 In-stock
10 mg USD 158 In-stock
50 mg USD 462 In-stock
100 mg USD 818 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 13 publication(s) in Google Scholar

BMS 777607 Related Antibodies

Top Publications Citing Use of Products

    BMS 777607 purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2019 Aug 1;381(1):50-56.  [Abstract]

    Western analysis of the effect of BMS-777607 on the expression of osteogenic biomarkers during the osteoblastic differentiation of cultured preosteoblastic cells for 4 days.

    BMS 777607 purchased from MedChemExpress. Usage Cited in: Taiwan J Obstet Gynecol. 2019 Jan;58(1):145-152.  [Abstract]

    Western blot of cell cycle- and mitosis-associated proteins in SKOV3 cells treated with BMS-777607 for 48 h.

    BMS 777607 purchased from MedChemExpress. Usage Cited in: Taiwan J Obstet Gynecol. 2019 Jan;58(1):145-152.  [Abstract]

    Western blot of c-MET signaling-associated proteins of the SKOV3 cells treated with BMS-777607.

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    Axl Mer Tyro3

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases[1].

    IC50 & Target

    Axl

     

    Tyro3

     

    In Vitro

    BMS 777607 is a selective ATP-competitive Met kinase inhibitor which potently blocks the autophosphorylation of c-Met with IC50 of 20 nM in GTL-16 cell lysates, and demonstrates selective inhibition of proliferation in Met-driven tumor cell lines, such as GTL-16 cell line, H1993 and U87[1]. BMS 777607 inhibits hepatocyte growth factor (HGF)-triggered c-Met autophosphorylation with IC50 of < 1 nM in PC-3 and DU145 prostate cancer cells. BMS 777607 has little effect on tumor cell growth, but exhibits inhibitory effect on HGF-induced cell scattering in PC-3 and DU145 cells, with almost complete inhibition at 0.5 μM. BMS 777607 also suppresses stimulated cell migration and invasion in a dose-dependent fashion (IC50 < 0.1 μM) in both cell lines[2]. Application of BMS 777607 (appr 10 μM) to the highly metastatic murine KHT cells for 2 hours potently eliminates basal levels of autophosphorylated c-Met with IC50 of 10 nM without affecting the total c-Met, leading to dose-dependent inhibition of phosphorylation of downstream signaling molecules including ERK, Akt, p70S6K and S6. Treatment with BMS 777607 (appr 1 μM) for 24 hours potently inhibits the KHT cell scatter, motility and invasion at doses in the nanomolar range which consists with MET gene knockdown, and modestly affects cell proliferation and colony formation[3].

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

    BMS 777607 Related Antibodies
    In Vivo

    Oral administration of BMS 777607 (6.25-50 mg/kg) significantly reduces tumor volumes of the GTL-16 human tumor xenografts in athymic mice with no observed toxicity[1]. Administration of BMS 777607 (25 mg/kg/day) decreases the number of KHT lung tumor nodules (28.3%), improves the morphological hemorrhage, and significantly impairs the metastatic phenotype in the 6-8 week-old female C3H/HeJ mice injected with rodent fibrosarcoma KHT cells without apparent systemic toxicity compared to the control treatment. A low dose of BMS 777607 (10 mg/kg) also offers a mild but not significant inhibition of lung nodule formation compared to the vehicle control[3].

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

    512.89

    Formula

    C25H19ClF2N4O4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=CC=C(C(F)=C1)OC2=C(C(N)=NC=C2)Cl)C3=C(C=CN(C3=O)C4=CC=C(C=C4)F)OCC
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 39 mg/mL (76.04 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9497 mL 9.7487 mL 19.4974 mL
    5 mM 0.3899 mL 1.9497 mL 3.8995 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    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.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.33%

    COA (247 KB) HNMR (284 KB) LCMS (96 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [3]

    KHT cells are exposed to serial dilution of BMS 777607 for 96 hours, then the MTT assay and trypan blue exclusion are used for the determination of cell proliferation and cell death, respectively. KHT cell colonies are incubated with BMS 777607 for 24 hours and then stained with crystal violet (0.1%) and photographed for the assessment of cell scattering. 2 mm scratch on the confluent KHT cell monolayer is made using a sterilized 1 mL pipette tip followed by treated with BMS 777607 for 24 hours, then the number of cells that have migrated into the denuded area is counted on 4 random fields for the evaluation of cell migration. For the examination of cell invasion, the commercial transwell inserts (8 μM pore membrane) pre-loaded with Matrigel are incubated with serum-free medium in the presence or absence of BMS 777607 at 37°C for 2 hours to allow rehydration of Matrigel. Then cells suspended in serum-free medium are loaded onto the top chamber (5×103/insert) and complete medium (containing 10% FBS) is used in the lower chamber as a chemoattractant. After incubation for 24 hours, the Matrigel is removed and the inserts are stained with crystal violet. Invaded cells on the underside of the filter are photographed and counted.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    The pharemacokinetics of BMS 777607 are characterized in male Balb/C mice. Two groups of animals (N=6 per group, 20-25 g) are fasted overnight and receive BMS 777607 either as an intravenous (IV) bolus dose (5 mg/kg) via the tail vein or by gavage (10 mg/kg). The mice are fed 6 h after dosing. Blood samples (appr 0.2 mL) are obtained by retro-orbital bleeding at 0.05 (or 0.25 for oral), 0.5, 1, 3, 6, 8 and 24 h post dose. Within each group, half of the animals are bled at 0.05 (or 0.25 for oral), 1, 6 and 24 h, the other half are bled at 0.5, 3, and 8 h, resulting in a composite pharmacokinetic profile (3 mice per time point). Blood samples are allowed to coagulate and centrifuged at 4°C (1500-2000 ×g) to obtain serum. Serum samples are stored at appr 20°C until analysis by LC/MS/MS.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9497 mL 9.7487 mL 19.4974 mL 48.7434 mL
    5 mM 0.3899 mL 1.9497 mL 3.8995 mL 9.7487 mL
    10 mM 0.1950 mL 0.9749 mL 1.9497 mL 4.8743 mL
    15 mM 0.1300 mL 0.6499 mL 1.2998 mL 3.2496 mL
    20 mM 0.0975 mL 0.4874 mL 0.9749 mL 2.4372 mL
    25 mM 0.0780 mL 0.3899 mL 0.7799 mL 1.9497 mL
    30 mM 0.0650 mL 0.3250 mL 0.6499 mL 1.6248 mL
    40 mM 0.0487 mL 0.2437 mL 0.4874 mL 1.2186 mL
    50 mM 0.0390 mL 0.1950 mL 0.3899 mL 0.9749 mL
    60 mM 0.0325 mL 0.1625 mL 0.3250 mL 0.8124 mL
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    BMS 777607 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:

    BMS 7776071025720-94-8BMS 817378BMS777607BMS-777607BMS817378BMS-817378c-Met/HGFRTAM ReceptorTyro3AxlMerInhibitorinhibitorinhibit

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