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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

4.5 *For Research Use Only! Not for Human Use. We Do Not Sell to Patients.

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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
English Name :8-(Isoindolin-2-ylmethyl)-1,2-dihydro-3H-pyridazino[3,4,5-de]quinazolin-3-one
MDL No. :MFCD28167842
InChI Key :JLFSBHQQXIAQEC-UHFFFAOYSA-N
Pubchem ID :135565981

Safety of Stenoparib

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
DLD-1 cells 10 μmol/L 24 h To evaluate the effect of E7449 on Wnt signaling, results showed increased axin2 protein levels. Oncotarget. 2015 Dec 1;6(38):41307-23.
SW480 cells 10 μmol/L 24 h To evaluate the effect of E7449 on Wnt signaling, results showed increased axin2 protein levels and decreased β-catenin levels. Oncotarget. 2015 Dec 1;6(38):41307-23.
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. Oncotarget. 2015 Dec 1;6(38):41307-23.
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 mBio. 2021 Jan 19;12(1):e03495-20.
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%) mBio. 2021 Jan 19;12(1):e03495-20.
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 mBio. 2021 Jan 19;12(1):e03495-20.
A549 cells 10 mol/L 48 hours E7449 significantly downregulated TNKS expression, inhibited proliferation, migration, and invasion of A549 cells, and induced early apoptosis. J Cell Mol Med. 2024 Jun;28(12):e18467.
A549L6 cells 5.753 µM (IC50) 96 hours Evaluate the inhibitory effect of E7449 on proliferation and migration of A549L6 cells Cancers (Basel). 2025 Feb 6;17(3):559.

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. Oncotarget. 2015 Dec 1;6(38):41307-23.
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. J Cell Mol Med. 2024 Jun;28(12):e18467.
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 Cancers (Basel). 2025 Feb 6;17(3):559.

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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