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Kobe2602

Cat. No. M8954
Kobe2602 Structure
Size Price Availability Quantity
10mg USD 150  USD150 In stock
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Quality Control & Documentation
Biological Activity

Kobe2602 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD. Kobe2602 at 20 μM efficiently inhibited the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-Ras G12V. Moreover, Kobe2602 exhibits antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-ras(G12V) gene by oral administration.

Chemical Information
Molecular Weight 419.31
Formula C14H9F4N5O4S
CAS Number 454453-49-7
Solubility (25°C) DMSO: 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Shima F, et al. Enzymes. Discovery of small-molecule Ras inhibitors that display antitumor activity by interfering with Ras·GTP-effector interaction.

[2] Shima F, et al. Proc Natl Acad Sci U S A. In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction.

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  Catalog
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Keywords: Kobe2602 supplier, Ras, inhibitors, activators


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