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Kobe2602

Cat. No. M8954
Kobe2602 Structure
Size Price Availability Quantity
10mg USD 150 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 419.31
Formula C14H9F4N5O4S
CAS Number 454453-49-7
Purity >98%
Solubility DMSO: 10 mg/mL
Storage at -20°C
References

Discovery of small-molecule Ras inhibitors that display antitumor activity by interfering with Ras·GTP-effector interaction.
Shima F, et al. Enzymes. 2013;34 Pt. B:1-23. PMID: 25034098.

In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction.
Shima F, et al. Proc Natl Acad Sci U S A. 2013 May 14;110(20):8182-7. PMID: 23630290.

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Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD, exhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Kobe2602 supplier, Ras, inhibitors

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