Art. -Nr.: HY-15717

Kobe2602

1 Cited Publications

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Kobe2602 is a Ras-Raf interaction inhibitor. Kobe2602 inhibits the binding of H-Ras·GTP to c-Raf-1 RBD with a K_i of 149 μM. Kobe2602 has antitumor activity.

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Reinheit: 98.20%
CAS. Nr.: 454453-49-7
Formel: C₁₄H₉F₄N₅O₄S
Molecular Weight:419.31

Speicherung:

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

Kobe2602 Chemical Structure

CAS. Nr.: 454453-49-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Kobe2602 is a Ras-Raf interaction inhibitor. Kobe2602 inhibits the binding of H-Ras·GTP to c-Raf-1 RBD with a K_i of 149 μM. Kobe2602 has antitumor activity^[1].

IC₅₀ & Target

Ki: 149 μM (Ras-Raf interaction)^[1]

Alle Ras Isoform-spezifische Produkte anzeigen :

In Vitro

Kobe2602 (2-20 μM; 1 hour) exhibits Ras-Raf-binding inhibition in NIH 3T3 cells^[1].
Kobe2602 has IC₅₀ value of approximately 10 μM for the cellular Ras-Raf-binding inhibition^[1].
Kobe2602 (20 μM) efficiently inhibits the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-Ras^G12V^[1].
Kobe2602 inhibits Ras?GTP but not Ras?GDP^[1].
Kobe2602 (20 μM) inhibits the anchorage-dependent proliferation of H-Ras^G12V-transformed cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

H-ras^G12V-transformed NIH 3T3 cells
Concentration:

20 μM
Incubation Time:

24 hours , 48 hours, 72 hours
Result:

Efficiently inhibited colony formation in soft agar in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

NIH 3T3 cells
Concentration:

2 μM, 20 μM
Incubation Time:

1 hour
Result:

Effectively reduced the amount of c-Raf-1 associated with H-Ras^G12V in NIH 3T3 cells in a dose-dependent manner, indicating the inhibition of the cellular activity of Ras.

In Vivo

Kobe2602 (80 mg/kg; p.o.; five consecutive days per week; for 17 days) exhibits antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-Ras^G12V gene^[1].

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

Animal Model:

Female athymic nude mice (6-8 wk old), with SW480 cells xenograft^[1]
Dosage:

80 mg/kg
Administration:

Oral administration, five consecutive days per week, for 17 days
Result:

Caused inhibition of the tumor growth.

Chemical Information

CAS. Nr. 454453-49-7
Appearance Solid
Molecular Weight 419.31
Formel C₁₄H₉F₄N₅O₄S
Color Light yellow to brown
SMILES

FC(C1=CC([N+]([O-])=O)=C(NNC(NC2=CC=C(F)C=C2)=S)C([N+]([O-])=O)=C1)(F)F
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (1)

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Research Square Preprint

2024 Oct 10.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 250 mg/mL (596.22 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

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

2.3849 mL

11.9244 mL

23.8487 mL

5 mM

0.4770 mL

2.3849 mL

4.7697 mL

10 mM

0.2385 mL

1.1924 mL

2.3849 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.

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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (11.92 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

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

Solubility: ≥ 5 mg/mL (11.92 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). 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 DMSO stock solution (50.0 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 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]. Shima, Fumi, et al. In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction. Proceedings of the National Academy of Sciences of the United States of America (2013), 110(20), 8182-8187, S8182/1-S8182/10. [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
DMSO	1 mM	2.3849 mL	11.9244 mL	23.8487 mL	59.6218 mL
	5 mM	0.4770 mL	2.3849 mL	4.7697 mL	11.9244 mL
	10 mM	0.2385 mL	1.1924 mL	2.3849 mL	5.9622 mL
	15 mM	0.1590 mL	0.7950 mL	1.5899 mL	3.9748 mL
	20 mM	0.1192 mL	0.5962 mL	1.1924 mL	2.9811 mL
	25 mM	0.0954 mL	0.4770 mL	0.9539 mL	2.3849 mL
	30 mM	0.0795 mL	0.3975 mL	0.7950 mL	1.9874 mL
	40 mM	0.0596 mL	0.2981 mL	0.5962 mL	1.4905 mL
	50 mM	0.0477 mL	0.2385 mL	0.4770 mL	1.1924 mL
	60 mM	0.0397 mL	0.1987 mL	0.3975 mL	0.9937 mL
	80 mM	0.0298 mL	0.1491 mL	0.2981 mL	0.7453 mL
	100 mM	0.0238 mL	0.1192 mL	0.2385 mL	0.5962 mL

Keywords

Kobe2602

1 Cited Publications

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Kobe2602

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Bioactive Compound Library Max

Bioactive Compound Library

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High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Kobe2602

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Kobe2602

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Kobe2602

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Kobe2602 Related Classifications

HY-15717 Related Classifications