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

RAF265 (Synonyms: CHIR-265)

Cat. No.: HY-10248 Purity: 99.89%
Handling Instructions

RAF265 is a potent 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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10 mM * 1 mL in DMSO USD 164 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 708 In-stock
Estimated Time of Arrival: December 31
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Based on 3 publication(s) in Google Scholar

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Description

RAF265 is a potent 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].

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].

Clinical Trial
Molecular Weight

518.41

Formula

C₂₄H₁₆F₆N₆O

CAS No.

927880-90-8

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 6 months
  -20°C 1 month
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 provided by MCE.
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

Purity: 99.89%

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RAF265
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