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Chemical Structure| 1140964-99-3 Chemical Structure| 1140964-99-3

Structure of Stenoparib
CAS No.: 1140964-99-3

Chemical Structure| 1140964-99-3

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E7449 is an orally bioavailable, potent, small molecule inhibitor of PARP1 and PARP2 and enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors.

Synonyms: E7449; 2X-121; MGI25036

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Product Details of Stenoparib

CAS No. :1140964-99-3
Formula : C18H15N5O
M.W : 317.34
SMILES Code : O=C1NNC2=C3C1=CC=CC3=NC(CN4CC5=C(C=CC=C5)C4)=N2
Synonyms :
E7449; 2X-121; MGI25036
MDL No. :MFCD28167842
InChI Key :JLFSBHQQXIAQEC-UHFFFAOYSA-N
Pubchem ID :135565981

Safety of Stenoparib

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H302-H319-H372-H410
Precautionary Statements:P501-P273-P260-P270-P264-P280-P391-P314-P337+P313-P305+P351+P338-P301+P312+P330
Class:9
UN#:3077
Packing Group:

Related Pathways of Stenoparib

epigenetics
DNA

Isoform Comparison

Biological Activity

Target
  • PARP1

    PARP1, IC50:1 nM

  • PARP2

    PARP2, IC50:1.2 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
LLC-MK2 rhesus macaque kidney cells 30 μM 120 hours Evaluate the inhibitory effect of Stenoparib on HCoV-NL63, showing a 69.3% reduction in plaquing efficiency and 95.8% reduction in viral copy number PMC7845641
Calu-3 human lung adenocarcinoma cells 60 μM 120 hours Evaluate the inhibitory effect of Stenoparib on SARS-CoV-2, showing nearly complete inhibition of plaque formation (94.0%) PMC7845641
Vero E6 monkey kidney cells 30 μM 48 hours Evaluate the inhibitory effect of Stenoparib on SARS-CoV-2, showing a significant 63.2% reduction in viral load PMC7845641
DLD-1 cells 10 μmol/L 24 h To evaluate the effect of E7449 on Wnt signaling, results showed increased axin2 protein levels. PMC4747407
SW480 cells 10 μmol/L 24 h To investigate the activation of PEPT1 transcription by DAC, results showed DAC activated PEPT1 transcription in a dose-dependent manner. PMC4747407
DT40 cells 0.1-10 μmol/L 30 min To evaluate the role of E7449 in DNA damage repair, results showed increased PARP1 binding to chromatin. PMC4747407
A549 cells 10 mol/L 48 hours Inhibited RSK4 activation, resulting in decreased cellular cIAP1 and cIAP2 expression PMC11186742
A549L6 cells 5.753 µM (IC50) 96 hours Evaluate the inhibitory effect of E7449 on proliferation and migration of A549L6 cells PMC11816722
Vero E6 cells 714μM To evaluate the effect of ACBI1 on SARS-CoV-2 infection, results showed that ACBI1 significantly inhibited viral replication. PMC9473406

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice B16-F10 isograft model Orally 10, 30, 100 mg/kg Once daily for 7 days To evaluate the antitumor effect of E7449 in combination with TMZ, results showed significantly enhanced tumor growth inhibition. PMC4747407
BALB/c nude mice Subcutaneous xenograft model with A549 cells Gavage 100 mg/kg Once daily for 14 days E7449 significantly inhibited the growth of subcutaneous lung adenocarcinoma tumors and induced apoptosis by attenuating the Wnt signaling pathway. PMC11186742
BALB/c nude mice LUAD bone metastasis model Oral 40 mg/kg Once daily for 21 days Evaluate the inhibitory effect of E7449 on bone metastasis PMC11816722
Mice SARS-CoV-2 infection model Oral 50 mg/kg Once daily for 5 days Evaluated the in vivo antiviral efficacy of Stenoparib, showing significant reduction in viral load. PMC9473406

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.15mL

0.63mL

0.32mL

15.76mL

3.15mL

1.58mL

31.51mL

6.30mL

3.15mL

References

 

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