1. Neuronal Signaling JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR TGF-beta/Smad Stem Cell/Wnt
  2. Monoamine Oxidase EGFR Akt TGF-beta/Smad
  3. CCT365623 hydrochloride

CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties.

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

CCT365623 hydrochloride Chemical Structure

CCT365623 hydrochloride Chemical Structure

CAS No. : 2126136-98-7

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Based on 1 publication(s) in Google Scholar

Other Forms of CCT365623 hydrochloride:

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties[1].

IC50 & Target

IC50: 0.89 μM (LOX)[1].

In Vitro

CCT365623 inhibits LOX at ~5 μM in the biosensor system[1].
CCT365623 (0-40 μM) concentration-dependently decreases the protein levels of surface EGFR[1].
CCT365623 (5 μM) decreases the protein levels of pY1068 EGFR, pAKT and MATN2, and increases the protein levels of pSMAD2[1].
CCT365623 disrupts HTRA1 multimerization, activates TGFβ1 signalling, suppresses MATN2 expression, suppresses EGFR surface retention, and suppresses EGFR signalling[1].

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

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells.
Concentration: 0-40 μM.
Incubation Time: 24 hours
Result: Significantly decreased the protein levels of surface EGFR, pY1068 EGFR, pAKT and MATN2.
Increased the protein levels of pSMAD2.
In Vivo

CCT365623 displays good stability in mouse liver microsomes and does not inhibit the cardiac potassium channel hERG[1].
CCT365623 (70 mg/kg, oral gavage per day) significantly delays the development of the primary tumors and also suppresses metastatic lung burden in the animals. CCT365623 disrupts EGFR cell surface retention and delays the growth of primary and metastatic tumor cell[1].
CCT365623 exhibits a T1/2PO of 0.6 h and F% (oral bioavailability) of 45%[1].

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

Animal Model: Mouse model of spontaneous breast cancer that metastasizes to the lungs (70 days old)[1].
Dosage: 70 mg/kg.
Administration: Oral gavage per day for about 3 weeks.
Result: Significantly reduced MATN2 protein levels in both the primary and metastatic lung tumors and this is accompanied by the loss of EGFR from the plasma membranes of the cells in both the primary and metastatic tumors.
Molecular Weight

443.99

Formula

C18H18ClNO4S3

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

NCC1=CC=C(S(=O)(C2=CC(C3=CC=CC=C3)=CC(S(=O)(C)=O)=C2)=O)S1.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (563.08 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 2.2523 mL 11.2615 mL 22.5230 mL
5 mM 0.4505 mL 2.2523 mL 4.5046 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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: ≥ 2.08 mg/mL (4.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 98.07%

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2523 mL 11.2615 mL 22.5230 mL 56.3076 mL
5 mM 0.4505 mL 2.2523 mL 4.5046 mL 11.2615 mL
10 mM 0.2252 mL 1.1262 mL 2.2523 mL 5.6308 mL
15 mM 0.1502 mL 0.7508 mL 1.5015 mL 3.7538 mL
20 mM 0.1126 mL 0.5631 mL 1.1262 mL 2.8154 mL
25 mM 0.0901 mL 0.4505 mL 0.9009 mL 2.2523 mL
30 mM 0.0751 mL 0.3754 mL 0.7508 mL 1.8769 mL
40 mM 0.0563 mL 0.2815 mL 0.5631 mL 1.4077 mL
50 mM 0.0450 mL 0.2252 mL 0.4505 mL 1.1262 mL
60 mM 0.0375 mL 0.1877 mL 0.3754 mL 0.9385 mL
80 mM 0.0282 mL 0.1408 mL 0.2815 mL 0.7038 mL
100 mM 0.0225 mL 0.1126 mL 0.2252 mL 0.5631 mL
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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.

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CCT365623 hydrochloride
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HY-124674A
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