Home Cell Cycle Ras inhibitor Kobe0065 For research use only.

Kobe0065

Kobe0065 is an H-Ras-cRaf1 interaction inhibitor, exhibiting 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 Chemical Structure

Kobe0065 Chemical Structure

CAS: 436133-68-5

Selleck's Kobe0065 has been cited by 2 publications

Purity & Quality Control

Batch: S830301 DMSO] 89 mg/mL] false] Ethanol] 13 mg/mL] false] Water] Insoluble] false Purity: 99.26%
99.26

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Biological Activity

Description Kobe0065 is an H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
Targets
H-Ras-cRaf1 interaction [1]
In vitro
In vitro Kobe0065-family compounds bind to Ras⋅GTP and exhibit antiproliferative activity toward cancer cells carrying the activated ras oncogenes. The compounds efficiently inhibit the interaction of Ras⋅GTP with their multiple effectors including Raf, PI3K, and RalGDS and a regulator/effector Sos and show rather broad binding specificity toward various Ras family small GTPases, which may account for their higher potency at the cellular level compared with that of the in vitro binding inhibition[1].
Cell Research Cell lines NIH 3T3 cells
Concentrations 2 and 20 μM
Incubation Time 1 h
Method NIH 3T3 cells are transfected with pEF-BOS-HA-H-Ras(G12V) or an empty vector and treated with the 2 and 20 μM compound or the vehicle (DMSO) in the presence of 2% FBS for 1 h. Cell lysate is subjected to detection of c-Raf-1 coimmunoprecipitated with an anti-H-Ras antibody and total c-Raf-1 by Western blotting with an anti-c-Raf-1 antibody. Immunoprecipitated H-Ras(G12V) are detected by an anti-HA antibody.
In Vivo
In vivo Kobe0065 has antitumor activity. The compound-treated tumors show a prominent increase of apoptotic cells without any significant body weight loss[1].
Animal Research Animal Models A xenograft of SW480 cells in nude mice.
Dosages 80 mg/kg and 160 mg/kg
Administration oral administration

Chemical Information & Solubility

Molecular Weight 449.79 Formula

C15H11ClF3N5O4S
CAS No. 436133-68-5 SDF Download Kobe0065 SDF
Smiles CC1=C(C=C(C=C1)NC(=S)NNC2=C(C=C(C=C2[N+](=O)[O-])C(F)(F)F)[N+](=O)[O-])Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 89 mg/mL ( (197.87 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 13 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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