1. GPCR/G Protein
    Apoptosis
  2. Ras
    Apoptosis
  3. Kobe0065

Kobe0065 

Cat. No.: HY-15716 Purity: 99.94%
Handling Instructions

Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.

For research use only. We do not sell to patients.

Kobe0065 Chemical Structure

Kobe0065 Chemical Structure

CAS No. : 436133-68-5

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
10 mg USD 72 In-stock
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50 mg USD 162 In-stock
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100 mg USD 264 In-stock
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200 mg USD 432 In-stock
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Based on 2 publication(s) in Google Scholar

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Description

Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.

IC50 & Target[1]

H-Ras

 

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]. The phosphorylation of downstream kinases MEK and ERK is effectively attenuated by 20 μM Kobe0065 and Kobe2602 in NIH3T3 cells transiently expressing H-RasG12V[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Kobe0065 and Kobe2602 exhibit antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-ras(G12V) gene by oral administration[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

449.79

Formula

C₁₅H₁₁ClF₃N₅O₄S

CAS No.

436133-68-5

SMILES

FC(C1=CC([N+]([O-])=O)=C(NNC(NC2=CC=C(C)C(Cl)=C2)=S)C([N+]([O-])=O)=C1)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 42.5 mg/mL (94.49 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2233 mL 11.1163 mL 22.2326 mL
5 mM 0.4447 mL 2.2233 mL 4.4465 mL
10 mM 0.2223 mL 1.1116 mL 2.2233 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Cells (2×103) are seeded in a 96-well plate and cultured in DMEM containing 2% (vol/vol) FBS in the presence of one of the compounds. Viable cell numbers are measured by formazan formation using a Cell Counting Kit 8. Apoptotic cells are detected by a standard TUNEL assay using an In Situ Cell Detection kit.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Cells (5×106) are implanted into the right flanks of female athymic nude mice (6-8 wk old). After tumor sizes reached appr 50 mm3 on average, compounds suspended in Cremophor:ethanol:water (1:1:6) are administered orally for five consecutive days per week for 17 d. Tumor volumes (V) are calculated. Dissected tumors after 17-d administration of the 80 mg/kg compounds are fixed in 4% (wt/vol) paraformaldehyde and embedded in paraffin. Their sections are subjected to immunohistochemistry with an anti-ERK1/2 antibody or an anti-CD31 antibody using a HISTMOUSE-PLUS kit. Apoptotic cells are detected by a TUNEL assay. Statistical significance for groups of three or more is determined by one-way ANOVA with Tukey’s test for post hoc analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

Kobe0065Kobe 0065Kobe-0065RasApoptosisInhibitorinhibitorinhibit

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