2. PI3K/Akt/mTOR
  3. Akt
  4. K-80003

K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.

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

K-80003 Chemical Structure

K-80003 Chemical Structure

CAS No. : 1292821-90-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

K-80003 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.

IC50 & Target

Akt[1]
In Vitro

When MCF-7 cells are cotreated with K-80003, TNFα-induced colocalization of tRXRα with p85α in the cytoplasm is inhibited, resulting in tRXRα nuclear localization. Western blotting shows that K-80003-stabilized tetrameric form of tRXRα is found exclusively in the nuclear fraction, while tRXRα monomer is distributed both in the nuclear and cytoplasmic fractions[2].

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

K-80003 Related Antibodies
In Vivo

K-80003 is a potent inhibitor of AKT activation by all-trans-retinoic acid. K-80003 displays enhanced efficacy in inhibiting tRXRα-dependent AKT activation and tRXRα tumor growth in animals. K-80003 has high affinity to RXRα but lacks COX inhibitory activity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

336.40

Formula

C22H21FO2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=C(C2=CC(F)=CC=C2/C1=C(C3=CC=C(C=C3)C(C)C)/[H])CC(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (89.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9727 mL 14.8633 mL 29.7265 mL
5 mM 0.5945 mL 2.9727 mL 5.9453 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 3 mg/mL (8.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Cell Assay
[2]

MCF-7 cells cotransfected with Myc-RXRα, Myc-tRXRα, tRXRα/L433D and p85α are pretreated with or without K-80003 (5 μM) for 3 h before exposed to TNFα (10 ng/mL) for 30 min. Cells are immunostained with anti-Myc and anti-p85α antibody, and their subcellular localization revealed by confocal microscopy. HEK293T cells cotransfected with Myc-tRXRα are treated with or without K-80003 (5 μM) for 6 h. Nuclear (N) and cytoplasmic (C) fractions are prepared, subjected to BS3 crosslinking, and analysed by western blotting using anti-Myc antibody. The purity of fractions is examined by analysing the expression of nuclear PARP and cytoplasmic α-tubulin in non-crosslinked fractions. One of three similar experiments is shown[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Nude mice (BALB/c, 4-5-week old) are injected subcutaneously with 100 μL of cells (2×106). For drug treatment, mice (n=6) are treated intraperitoneally after 7 days of transplantation with Corn oil, Sulindac (60 mg/kg), or K-80003 (60 mg/kg) once every other day (six injections). Body weight and tumor sizes are measured every 4 days.

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9727 mL 14.8633 mL 29.7265 mL 74.3163 mL
5 mM 0.5945 mL 2.9727 mL 5.9453 mL 14.8633 mL
10 mM 0.2973 mL 1.4863 mL 2.9727 mL 7.4316 mL
15 mM 0.1982 mL 0.9909 mL 1.9818 mL 4.9544 mL
20 mM 0.1486 mL 0.7432 mL 1.4863 mL 3.7158 mL
25 mM 0.1189 mL 0.5945 mL 1.1891 mL 2.9727 mL
30 mM 0.0991 mL 0.4954 mL 0.9909 mL 2.4772 mL
40 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8579 mL
50 mM 0.0595 mL 0.2973 mL 0.5945 mL 1.4863 mL
60 mM 0.0495 mL 0.2477 mL 0.4954 mL 1.2386 mL
80 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9290 mL
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K-80003 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

K-800031292821-90-9TX-803K80003K 80003TX803TX 803AktPKBProtein kinase BInhibitorinhibitorinhibit

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