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Kobe0065

Cat. No. M2608
Kobe0065 Structure
Size Price Availability Quantity
10mM*1mL USD 75  USD75 In stock
10mg USD 70  USD70 In stock
50mg USD 180  USD180 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Kobe0065 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. Kobe0065 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. Kobe0065 at 20 μM efficiently inhibited the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-Ras G12V, although the effect was slightly weaker than that of 2 μM sorafenib.

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 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.

Chemical Information
Molecular Weight 449.79
Formula C15H11ClF3N5O4S
CAS Number 436133-68-5
Purity >98%
Solubility DMSO
Storage at -20°C
References

[1] 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
Abmole Inhibitor Catalog 2017




Keywords: Kobe0065 supplier, Ras, inhibitors

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