Cat. No.: HY-10248

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RAF265

(Synonyms: CHIR-265)

6 Cited Publications

Customer Review

Based on 6 publication(s) in Google Scholar

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

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

Purity: 99.80%
CAS No.: 927880-90-8
Formula: C₂₄H₁₆F₆N₆O
Molecular Weight:518.41

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

RAF265 Chemical Structure

CAS No.: 927880-90-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (6)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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

IC₅₀ & Target^[1]

VEGFR2

RAF

All Raf Isoforms :

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.04 μM Compound: 1; RAF265	Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant	[PMID: 26396681]
A-375	IC₅₀	0.04 μM Compound: 1; RAF265	Inhibition of B-RAF V600E mutant in human A375 cells assessed as phosphorylation of ERK Inhibition of B-RAF V600E mutant in human A375 cells assessed as phosphorylation of ERK	[PMID: 26396681]
Malme-3M	IC₅₀	0.04 μM Compound: 1; RAF265	Antiproliferative activity against human MALME-3M cells harboring B-RAF V600E mutant Antiproliferative activity against human MALME-3M cells harboring B-RAF V600E mutant	[PMID: 26396681]
Malme-3M	IC₅₀	0.04 μM Compound: 1; RAF265	Inhibition of B-RAF V600E mutant in human Malme-3M cells assessed as phosphorylation of ERK Inhibition of B-RAF V600E mutant in human Malme-3M cells assessed as phosphorylation of ERK	[PMID: 26396681]
Malme-3M	IC₅₀	140 nM Compound: CHIR-265, RAF-265	Growth inhibition of MALME-3M cells Growth inhibition of MALME-3M cells	[PMID: 21576023]
SK-MEL-28	IC₅₀	0.14 μM Compound: 1; RAF265	Inhibition of B-RAF V600E mutant in human SK-MEL-28 cells assessed as phosphorylation of ERK Inhibition of B-RAF V600E mutant in human SK-MEL-28 cells assessed as phosphorylation of ERK	[PMID: 26396681]
SK-MEL-28	IC₅₀	0.16 μM Compound: 1; RAF265	Antiproliferative activity against human SK-MEL-28 cells harboring B-RAF V600E mutant Antiproliferative activity against human SK-MEL-28 cells harboring B-RAF V600E mutant	[PMID: 26396681]
SK-MEL-28	IC₅₀	140 nM Compound: CHIR-265, RAF-265	Growth inhibition of SK-MEL-28 cells Growth inhibition of SK-MEL-28 cells	[PMID: 21576023]

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 927880-90-8
Appearance Solid
Molecular Weight 518.41
Formula C₂₄H₁₆F₆N₆O
Color White to yellow
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
Synonyms

CHIR-265
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

Publications (6)

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Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Clin Sci (Lond)

A pan-RAF inhibitor LY3009120 inhibits necroptosis by preventing phosphorylation of RIPK1 and alleviates dextran sulfate sodium-induced colitis. [Abstract]

2019 Apr 16;133(8):919-932. PMID: 30944150
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
Viruses

Small-Molecule RAF265 as an Antiviral Therapy Acts against PEDV Infection. [Abstract]

2022 Oct 15;14(10):2261. PMID: 36298816
J Med Virol

Small molecule RAF265 as an antiviral therapy acts against HSV-1 by regulating cytoskeleton rearrangement and cellular translation machinery. [Abstract]

2023 Jan;95(1):e28226. PMID: 36251738

RAF265 purchased from MedChemExpress. Usage Cited in: J Med Virol. 2023 Jan;95(1):e28226. [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. 2023 Jan;95(1):e28226. [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.

RAF265 purchased from MedChemExpress. Usage Cited in: J Med Virol. 2023 Jan;95(1):e28226. [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.
BMC Pulm Med

The combination therapy of isomucronulatol 7-O-beta-glucoside (IMG) and CEP-9722 targeting ferroptosis-related biomarkers in non-small cell lung cancer (NSCLC). [Abstract]

2023 May 11;23(1):162. PMID: 37165402

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (192.90 mM; ultrasonic and warming and heat to 60°C; 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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 (4.82 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (4.82 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

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.

Protocol 4

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.

Protocol 5

Add each solvent one by one: 10% EtOH 90% Corn Oil

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

This protocol yields a clear solution of 1 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocol

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].

MedChemExpress (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].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Mordant P, et al. Dependence on phosphoinositide 3-kinase and RAS-RAF pathways drive the activity of RAF265, a novel RAF/VEGFR2 inhibitor, and RAD001 (Everolimus) in combination. Mol Cancer Ther. 2010 Feb;9(2):358-68. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
	60 mM	0.0321 mL	0.1607 mL	0.3215 mL	0.8037 mL
	80 mM	0.0241 mL	0.1206 mL	0.2411 mL	0.6028 mL
	100 mM	0.0193 mL	0.0964 mL	0.1929 mL	0.4822 mL

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RAF265

Anti-Infection Compound Library

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Anti-Breast Cancer Compound Library

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Anti-Pancreatic Cancer Compound Library

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Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) RAF265

All Raf Isoforms

All VEGFR Isoforms

Biological Activity

Chemical Information

Publications (6)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

RAF265 Related Classifications

HY-10248 Related Classifications