Shopping Cart

Remove All

Your shopping cart is currently empty

Kobe0065

Select Batch

Purity:100%

Resource Download

COA HNMR LCMS

Kobe0065

Catalog No. T1876Cas No. 436133-68-5

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

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Pack Size	Price	Availability
5 mg	$39	In Stock
10 mg	$57	In Stock
25 mg	$98	In Stock
50 mg	$143	In Stock
100 mg	$233	In Stock
200 mg	$387	In Stock
500 mg	$646	In Stock

Bulk & Custom

Add to Cart

Questions

Related Compound Libraries of "Kobe0065"

Product Introduction

Bioactivity

Description	Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; shows potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
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].
In vivo	Kobe0065 has antitumor activity. The compound-treated tumors show a prominent increase of apoptotic cells without any significant body weight loss[1].
Kinase Assay	Determination of lipase activity: For determination of lipase activity, lysates are incubated with a substrate containing radiolabeled [9,10-3H(N)]-triolein. Subsequently, FA are extracted and quantitated by liquid scintilation counting. Data are presented as mean S.D. of triplicate determinations and representative for at least three independent experiments.
Cell Research	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.(Only for Reference)

Chemical Properties

Molecular Weight	449.79
Formula	C15H11ClF3N5O4S
Cas No.	436133-68-5

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 4.5 mg/mL (10 mM))

DMSO: 20 mg/ml

Solution Preparation Table

Ethanol

	1mg	5mg	10mg	50mg
10 mM	0.2223 mL	1.1116 mL	2.2233 mL	11.1163 mL
20 mM	0.1112 mL	0.5558 mL	1.1116 mL	5.5581 mL
50 mM	0.0445 mL	0.2223 mL	0.4447 mL	2.2233 mL
100 mM	0.0222 mL	0.1112 mL	0.2223 mL	1.1116 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

You can also refer to dose conversion for different animals. More

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc