PARP1/2-IN-3
PARP1/2-IN-3 (Compound 29) is an orally active inhibitor for PARP 1 and PARP 2 with IC50 of 0.2235 nM and <0.001 nM. PARP1/2-IN-3 inhibits the proliferation of Capan-1 wildtype, AZD2281 or BMN673 resistant cells with IC50 of 1.82-9.98 nM. PARP1/2-IN-3 exhibits antitumor efficacy in mice.
For research use only. We do not sell to patients.
- CAS No.: 3032451-58-1
- Formula: C26H21FN6O3
- Molecular Weight:484.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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PARP-1 0.2235 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CAPAN-1 | IC50 |
1.82 nM
Compound: 2
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Antiproliferative activity against human CAPAN-1 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay
Antiproliferative activity against human CAPAN-1 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay
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[PMID: 37605459] |
| CAPAN-1 | IC50 |
8.28 nM
Compound: 2
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Antiproliferative activity against human Olaparib-resistant CAPAN-1 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay
Antiproliferative activity against human Olaparib-resistant CAPAN-1 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay
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[PMID: 37605459] |
| CAPAN-1 | IC50 |
9.98 nM
Compound: 2
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Antiproliferative activity against human Talazoparib-resistant CAPAN-1 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay
Antiproliferative activity against human Talazoparib-resistant CAPAN-1 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay
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[PMID: 37605459] |
Chemical Information
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CAS No. 3032451-58-1
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Molecular Weight 484.48
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Formula C26H21FN6O3
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SMILES
CC1=CC=C(O1)C2=NN=C3CN(CCN32)C(C4=CC(CC5=NNC(C6=C5C=CC=C6)=O)=CC=C4F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PARP1/2-IN-3 Related Classifications
HY-163817 Related Classifications
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