2. Epigenetics
  3. Histone Demethylase
  4. QC6352

QC6352 est un inhibiteur de KDM4C qui est oralement disponible, sélectif et puissant avec un IC50 de 35 nM.

QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B).

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

QC6352 Chemical Structure

QC6352 Chemical Structure

CAS No. : 1851373-36-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 460 In-stock
Solution
10 mM * 1 mL in DMSO USD 460 In-stock
Solid
1 mg USD 180 In-stock
5 mg USD 540 In-stock
10 mg USD 730 In-stock
25 mg USD 1250 In-stock
50 mg USD 1740 In-stock
100 mg USD 2500 In-stock
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500 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

QC6352 Related Antibodies

Top Publications Citing Use of Products

View All Histone Demethylase Isoform Specific Products:

View All Isoforms
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B)[1][2].

IC50 & Target[2]

KDM4

 

KDM5B

750 nM (IC50)

KDM4A

104 nM (IC50)

KDM4B

56 nM (IC50)

KDM4C

35 nM (IC50)

KDM4D

104 nM (IC50)

In Vitro

QC6352 is a potent KDM4C inhibitor with an IC50 of 35±8 nM[1]. In a concentration-dependent manner QC6352 dramatically reduces the sphere-forming capacity of BCSC1 and BCSC2. QC6352 blocks proliferation and self-renewal of BCSCs. As shown by western blot analysis the protein levels of (Epidermal growth factor receptor) EGFR are reduced in both BCSC1 and BCSC2 upon treatment with QC6352[2].

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

QC6352 Related Antibodies
In Vivo

QC6352 strongly affects tumor growth and final tumor weight of both BCSC1 and BCSC2 xenografts. Treatment with QC6352 is well tolerated and does not affect body weight of the mice. Results demonstrate that treatment with the KDM4 inhibitor QC6352 blocks BCSC xenograft tumor growth[2].

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

387.47

Formula

C24H25N3O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(NC[C@@H]2CCCC3=C2C=CC(N(C)C4=CC=CC=C4)=C3)C=NC=C1)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (43.02 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 2.5808 mL 12.9042 mL 25.8084 mL
5 mM 0.5162 mL 2.5808 mL 5.1617 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 (protect from light). 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 1.67 mg/mL (4.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 1.67 mg/mL (4.31 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 10 mg/mL (25.81 mM); Suspended solution; Need ultrasonic

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).

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

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

Purity: 99.48%

COA (254 KB) HNMR (297 KB) LCMS (90 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[2]

Cells are detached by Accutase and counted. 1×103 single BCSC1 and BCSC2 cells are seeded as triplicates in 50% Matrigel into individual wells of 24-well ultra-low attachment plates in serum-free MSC medium. After 7 days, spheres over 50 μm diameter are counted for QC6352- and QC6688-treated and control cells and spheres over 20 μm diameter are counted for paclitaxel-treated and control cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice: When tumors reach a palpable size of 3 mm3, mice are treated with vehicle (control) or QC6352. The inhibitor is administered daily to mice via oral gavage at 10 mg/kg. Control animals receive vehicle only. Animals are monitored twice weekly for weight and tumor growth[2].

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 (protect from light). 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 2.5808 mL 12.9042 mL 25.8084 mL 64.5211 mL
5 mM 0.5162 mL 2.5808 mL 5.1617 mL 12.9042 mL
10 mM 0.2581 mL 1.2904 mL 2.5808 mL 6.4521 mL
15 mM 0.1721 mL 0.8603 mL 1.7206 mL 4.3014 mL
20 mM 0.1290 mL 0.6452 mL 1.2904 mL 3.2261 mL
25 mM 0.1032 mL 0.5162 mL 1.0323 mL 2.5808 mL
30 mM 0.0860 mL 0.4301 mL 0.8603 mL 2.1507 mL
40 mM 0.0645 mL 0.3226 mL 0.6452 mL 1.6130 mL
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QC6352 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:

QC63521851373-36-8QC 6352QC-6352Histone DemethylaseInhibitorinhibitorinhibit

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