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Kobe0065 Ras inhibitor

Name: Kobe0065
Brand: Selleck Chemicals
SKU: S8303
Rating: 5 (3 reviews)

Cat.No.S8303

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.

Chemical Structure

Molecular Weight: 449.79

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.26

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated KRas Aurora Kinase Casein Kinase
Other Ras Inhibitors	ERAS-0015 RMC5127 Salirasib RBC8 BQU57 CID-1067700 (ML282) ADT-007 MCP110 Perillyl alcohol Kobe2602

Chemical Information, Storage & Stability

Molecular Weight	449.79	Formula	C₁₅H₁₁ClF₃N₅O₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	436133-68-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Solubility

In vitro
Batch:

DMSO : 89 mg/mL (197.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 13 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	H-Ras-cRaf1 interaction
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.
In vivo	Kobe0065 has antitumor activity. The compound-treated tumours show a prominent increase of apoptotic cells without any significant body weight loss.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23630290/

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