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Chemical Structure| 1429639-50-8 Chemical Structure| 1429639-50-8

Structure of CZ415
CAS No.: 1429639-50-8

Chemical Structure| 1429639-50-8

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CZ415 is a potent and highly selective ATP-competitive mTOR inhibitor with pKdapp value of 8.2.

Synonyms: CZ415

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Product Details of CZ415

CAS No. :1429639-50-8
Formula : C22H29N5O4S
M.W : 459.56
SMILES Code : O=C(NCC)NC1=CC=C(C2=NC(N3[C@@H](C)COCC3)=C4C(C(C)(C)S(C4)(=O)=O)=N2)C=C1
Synonyms :
CZ415
MDL No. :MFCD30533321
InChI Key :IZLPVLBNRGPOHA-AWEZNQCLSA-N
Pubchem ID :71547699

Safety of CZ415

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of CZ415

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • mTOR

    mTOR, pIC50:8.07

In Vitro:

Cell Line
Concentration Treated Time Description References
U2OS cells 25-1000 nM 72 hours CZ415 concentration-dependently inhibited survival of U2OS cells PMC5669867
Primary human OS cells (primary OS2) 25/100 nM CZ415 inhibited survival of primary human OS cells (primary OS2) PMC5669867
Primary human OS cells (primary OS1) 25/100 nM CZ415 inhibited survival of primary human OS cells (primary OS1) PMC5669867
SaOs2 cells 25-1000 nM 72 hours CZ415 concentration-dependently inhibited survival of SaOs2 cells PMC5669867
Human whole blood cells 226 nM IC50 18 hours Inhibition of IFNγ release PMC4983736
HEK293T cells 14.5 nM IC50 2 hours Inhibition of S6RP phosphorylation PMC4983736
MG-63 cells 25-1000 nM 72 hours CZ415 concentration-dependently inhibited survival of MG-63 cells PMC5669867

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Anti-CD3 mouse model Oral 1, 3, and 10 mg/kg 1 hour before stimulus Inhibition of mTOR downstream signaling PMC4983736
SCID mice U2OS tumor xenograft model Oral 25 mg/kg Daily for 21 days CZ415 oral administration efficiently inhibited U2OS tumor growth in mice, and its activity was further potentiated with co-administration of MEK162 PMC5669867

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.88mL

2.18mL

1.09mL

21.76mL

4.35mL

2.18mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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