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

RAF265  (Synonyms: CHIR-265)

Cat. No.: HY-10248 Purity: 99.90%
COA Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 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
100 mg   Get quote  
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

RAF265 Related Antibodies

Top Publications Citing Use of Products

    RAF265 purchased from MCE. 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 MCE. 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 MCE. 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.

    View All Raf Isoform Specific Products:

    View All Isoforms
    BRaf c-Raf Raf

    View All VEGFR Isoform Specific Products:

    View All Isoforms
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    • 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].

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

    RAF265 Related Antibodies
    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].

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

    518.41

    Appearance

    Solid

    Formula

    C24H16F6N6O
    CAS No.
    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)

    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
    10 mM 0.1929 mL 0.9645 mL 1.9290 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% EtOH    90% corn oil

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

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.90%

    COA (247 KB) LCMS (269 KB)

    Handling Instructions (2659 KB)
    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
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    RAF265 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.

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
    C1   V1   C2   V2

    Keywords:

    RAF265927880-90-8CHIR-265RAF 265RAF-265CHIR265CHIR 265RafVEGFRAutophagyApoptosisRaf kinasesVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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