Art. -Nr.: HY-147268

Exarafenib

(Synonyms: RAF/KIN_2787)

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Exarafenib (RAF/KIN_2787) is an orally-available, selective pan-RAF inhibitor. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. Exarafenib has anticancer activity.

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Reinheit: 99.68%
CAS. Nr.: 2639957-39-2
Formel: C₂₆H₃₄F₃N₅O₃
Molecular Weight:521.58

Speicherung:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Exarafenib Chemical Structure

CAS. Nr.: 2639957-39-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

RAF

p38 MAPK

Alle Raf Isoform-spezifische Produkte anzeigen :

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

In Vitro

Exarafenib (RAF/KIN_2787; 1-10000 nM; 24 h) inhibits RAF-dependent melanoma cell line growth. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines^[1].

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

Cell Viability Assay^[1]

Cell Line:

Melanoma cell (A375 BRAF^V600E, HMVII BRAF^G469V; NRAS^Q61K, WM3629 BRAF^D594G; NRAS^G12D, SKMEL2 NRAS^Q61R)
Concentration:

1-10000 nM
Incubation Time:

24 h
Result:

Inhibited RAF-dependent melanoma cell line growth.

In Vivo

Exarafenib (RAF/KIN_2787; 3-30 mg/kg; Orally; twice daily; 29 days) is effective against BRAF^mut & NRAS^mut human melanoma xenografts in vivo^[1].

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

Animal Model:

BALB/c nude mice xenograft models of BRAF and NRAS-mutant melanoma^[1]
Dosage:

3, 5, 10, 20, 30 mg/kg
Administration:

Orally; twice daily (BID); 29 days
Result:

Was effective against BRAF^mut & NRAS^mut human melanoma xenografts in vivo.

Clinical Trial

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

Chemical Information

CAS. Nr. 2639957-39-2
Appearance Solid
Molecular Weight 521.58
Formel C₂₆H₃₄F₃N₅O₃
Color White to yellow
SMILES

CC1=CC=C(NC(N2C[C@@H](CC2)CC(F)(F)F)=O)C=C1C3=CC(N[C@H](C)CO)=NC(N4CCOCC4)=C3
Synonyms

RAF/KIN_2787
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (191.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.9173 mL

9.5863 mL

19.1725 mL

5 mM

0.3835 mL

1.9173 mL

3.8345 mL

10 mM

0.1917 mL

0.9586 mL

1.9173 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (4.79 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.

Protocol 2

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

Solubility: 2.5 mg/mL (4.79 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 20% SBE-β-CD in Saline, 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

Verweise

[1]. Miller N, et, al. Antitumor activity of KIN-2787, a next-generation pan-RAF inhibitor, in combination with MEK inhibition in preclinical models of human NRAS mutant melanoma.2022 Jun 2;40(16): e15099.

[2]. WHO Drug Information. International Nonproprietary Names for Pharmaceutical

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9173 mL	9.5863 mL	19.1725 mL	47.9313 mL
	5 mM	0.3835 mL	1.9173 mL	3.8345 mL	9.5863 mL
	10 mM	0.1917 mL	0.9586 mL	1.9173 mL	4.7931 mL
	15 mM	0.1278 mL	0.6391 mL	1.2782 mL	3.1954 mL
	20 mM	0.0959 mL	0.4793 mL	0.9586 mL	2.3966 mL
	25 mM	0.0767 mL	0.3835 mL	0.7669 mL	1.9173 mL
	30 mM	0.0639 mL	0.3195 mL	0.6391 mL	1.5977 mL
	40 mM	0.0479 mL	0.2397 mL	0.4793 mL	1.1983 mL
	50 mM	0.0383 mL	0.1917 mL	0.3835 mL	0.9586 mL
	60 mM	0.0320 mL	0.1598 mL	0.3195 mL	0.7989 mL
	80 mM	0.0240 mL	0.1198 mL	0.2397 mL	0.5991 mL
	100 mM	0.0192 mL	0.0959 mL	0.1917 mL	0.4793 mL

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Exarafenib

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Alle Raf Isoform-spezifische Produkte anzeigen

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Exarafenib Related Classifications

HY-147268 Related Classifications