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

CCT365623 hydrochloride 

Cat. No.: HY-124674A Purity: >98.0%
Handling Instructions

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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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].

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].

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.

2126136-98-7

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
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >98.0%

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Keywords:

CCT365623CCT 365623CCT-365623Monoamine OxidaseEGFRAktTGF-beta/SmadMAOEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BTransforming growth factor betabreastcancerU87metastasisInhibitorinhibitorinhibit

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CCT365623 hydrochloride
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HY-124674A
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