1. MAPK/ERK Pathway Protein Tyrosine Kinase/RTK Autophagy Apoptosis
  2. Raf VEGFR Autophagy Apoptosis
  3. RAF265

RAF265 is a potent and orally active RAF/VEGFR2 inhibitor.

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

RAF265 Chemical Structure

RAF265 Chemical Structure

CAS No. : 927880-90-8

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
5 mg USD 116 In-stock
10 mg USD 198 In-stock
25 mg USD 376 In-stock
50 mg USD 616 In-stock
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200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 9 publication(s) in Google Scholar

Top Publications Citing Use of Products

    RAF265 purchased from MedChemExpress. Usage Cited in: J Med Virol. 2022 Oct 17.  [Abstract]

    RAF265 (5, 10, 25 μM; 24 h) significantly reduces the levels of B‐Raf and p‐Mnk1 in a dose‐dependent manner in vero cells.

    RAF265 purchased from MedChemExpress. Usage Cited in: J Med Virol. 2022 Oct 17.  [Abstract]

    Cells are infected with HSV-1 for 1 h, washed three times, are then treated with RAF265 at 37°C for different times (1, 2, or 3 h). After 24 h, cell lysate is harvested for WB to detect the level of viral protein.

    RAF265 purchased from MedChemExpress. Usage Cited in: J Med Virol. 2022 Oct 17.  [Abstract]

    Vero cells infected with 50 MOI HSV-1 are treated with DMSO or RAF265 at 25 μM for 4 h at 37°C, fixed, incubated with anti-ICP5 mouse mono-antibody overnight, and stained with FITC-conjugated secondary antibody.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    RAF265 is a potent and orally active RAF/VEGFR2 inhibitor.

    IC50 & Target[1]

    VEGFR2

     

    RAF

     

    In Vitro

    The MTT assay reveals that in HT29 and MDAMB231 cells, RAF265 alone shows significant activity with IC20 values of 1 to 3 μM and IC50 values of 5 to 10 μM. In A549 and HCT116 cells, IC20 values are 1 μM for both, but RAF265 concentrations up to 10 μM do not reach IC50 values. However, in the presence of 1 nM RAD001, the IC50 for RAF265 is 5 μM in A549 cells and 10 μM in HCT116 cells[1].

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

    In Vivo

    In single-compound efficacy studies, optimal dosing of RAD001 and RAF265 is 5 to 12 mg/kg daily and 30 mg/kg every two days, respectively. However, combination tolerability studies in nontumor-bearing mice defin dose-limiting toxicity as a 10% weight loss with the combination of RAD001 at a dose of 12 mg/kg daily and RAF265 at a dose of 20 mg/kg every two days. Therefore, the combination of RAF265 at a dose of 12 mg/kg qd and RAD001 at a dose of 12 mg/kg qd seems to be the maximal tolerated dose. RAD001 and RAF265 are both given at a dose of 12 mg/kg qd, alone or concurrently, over 6 days. After a 2-day stop, the compounds are given for another 6 days, and the treatment is then stopped. To confirm the potential of the combination of RAF265 and RAD001, the antitumor effect of the combination is tested in HCT116 xenografts (KRAS mut, PIK3CA mut). In HCT116 xenografts, RAD001 or RAF265 given alone shows 60% to 65% and 71% to 72% TVI%, respectively[1].

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

    Clinical Trial
    Molecular Weight

    518.41

    Formula

    C24H16F6N6O

    CAS No.
    Appearance

    Solid

    Color

    White to khaki

    SMILES

    FC(F)(C1=CN=C(N1)C2=NC=CC(OC3=CC=C4N(C(NC5=CC=C(C(F)(F)F)C=C5)=NC4=C3)C)=C2)F

    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 : ≥ 26 mg/mL (50.15 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 10 mg/mL (19.29 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9290 mL 9.6449 mL 19.2898 mL
    5 mM 0.3858 mL 1.9290 mL 3.8580 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
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    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)

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    Volume (start)

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    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% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1 mg/mL (1.93 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 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% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: 1 mg/mL (1.93 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 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: 99.90%

    References
    Cell Assay
    [1]

    The MTT assay and Bliss additivism model are used to assess the effect of the combination on cell viability. Human A549 and H460 lung, HT29 and HCT 116 colon, and MDAMB231 breast cancer cell lines are used. In each well of a 96-well plate, 1×104 cells are grown in 200 μL of medium. After 24 h, RAD001, RAF265, or the combination is added to achieve a final concentration of 0.1 to 10 nM and 0.1 to 10 μM, respectively. After 48 h of treatment, 20 μL of 5 mg/mL MTT solution in PBS is added to each well. After 4 h, supernatant is removed and formazan crystals are discarded in 200 μL of DMSO. Absorbance is then measured at 595 nm using an absorbance plate reader. Data are expressed as the percentage of viable cells in treated relative to nontreated conditions[1].

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

    Animal Administration
    [1]

    Mice[1]
    The efficacy of the combination is also tested in vivo. A total of 3×106 A549, H460, HCT116, or MDAMB231 cells are injected s.c. into the flank region of 6-wk-old female athymic mice. When tumors reach 50 mm3, the mice are randomized into four groups (n=7/group) for the following treatment: vehicle, RAF265 (12 mg/kg daily), RAD001 (12 mg/kg daily), or both. All drug are administered over 14 d (6 d on, 2 d off, 6 d on), and the drug combination is administered concurrently. Control mice receive the respective vehicles of both drugs. Animal weight and tumor volumes are taken twice weekly and expressed relative to initial tumor volume. Tumors are measured until achieving a relative volume of 10 times the initial volume, and the time to this end point is noted. Drug efficacy is assessed based on the tumor growth curve, growth delay, and tumor volume inhibition percentage. The tumor growth curve is designed to depict the evolution of the relative tumor size over time. The tumor volume inhibition percentage (TVI%) is calculated[1].

    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
    Ethanol / DMSO 1 mM 1.9290 mL 9.6449 mL 19.2898 mL 48.2244 mL
    5 mM 0.3858 mL 1.9290 mL 3.8580 mL 9.6449 mL
    10 mM 0.1929 mL 0.9645 mL 1.9290 mL 4.8224 mL
    15 mM 0.1286 mL 0.6430 mL 1.2860 mL 3.2150 mL
    DMSO 20 mM 0.0964 mL 0.4822 mL 0.9645 mL 2.4112 mL
    25 mM 0.0772 mL 0.3858 mL 0.7716 mL 1.9290 mL
    30 mM 0.0643 mL 0.3215 mL 0.6430 mL 1.6075 mL
    40 mM 0.0482 mL 0.2411 mL 0.4822 mL 1.2056 mL
    50 mM 0.0386 mL 0.1929 mL 0.3858 mL 0.9645 mL
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    • 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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    Product Name:
    RAF265
    Cat. No.:
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