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Kobe2602 

Cat. No.: HY-15717 Purity: 99.33%
Handling Instructions

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

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

Kobe2602 Chemical Structure

Kobe2602 Chemical Structure

CAS No. : 454453-49-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
50 mg USD 90 In-stock
Estimated Time of Arrival: December 31
250 mg USD 288 In-stock
Estimated Time of Arrival: December 31
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Description

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

IC50 & Target

Ki: 149 μM (Ras-Raf interaction)[1]

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-RasG12V[1].
Kobe2602 inhibits Ras⋅GTP but not Ras⋅GDP[1].
Kobe2602 (20 μM) inhibits the anchorage-dependent proliferation of H-rasG12V-transformed cells[1].

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

Cell Proliferation Assay[1]

Cell Line: H-rasG12V-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-RasG12V 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-rasG12V gene[1].

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.
Molecular Weight

419.31

Formula

C₁₄H₉F₄N₅O₄S

CAS No.

454453-49-7

SMILES

FC(C1=CC([N+]([O-])=O)=C(NNC(NC2=CC=C(F)C=C2)=S)C([N+]([O-])=O)=C1)(F)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 : 14.3 mg/mL (34.10 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
References
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Keywords:

Kobe2602Kobe 2602Kobe-2602RascarcinomaH-RasRafantiproliferativeInhibitorinhibitorinhibit

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Kobe2602
Cat. No.:
HY-15717
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