PARP-1-IN-1
PARP-1-IN-1 is a high selective and orally active PARP-1 inhibitor (IC50=0.96 nM). PARP-1-IN-1 has well tolerance and remarkable single dose activity in the MDA-MB-436 xenotransplantation model.
For research use only. We do not sell to patients.
- CAS No.: 2763840-83-9
- Formula: C23H25FN4O
- Molecular Weight:392.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
106.3 μM
Compound: Y49
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Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
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[PMID: 34656898] |
| MCF7 | IC50 |
123.5 μM
Compound: Y49
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
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[PMID: 34656898] |
| MX1 | IC50 |
9.46 μM
Compound: Y49
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Antiproliferative activity against human BRCA mutant MX1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human BRCA mutant MX1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
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[PMID: 34656898] |
PARP-1-IN-1 (compound Y49) (48 hours) has effective inhibition on different cancer cells (IC50s of 9.64, 123.5 106.3 μM for MX-1, MCF7 and A548 cells, respectively)[1].
PARP-1-IN-1 (2.5-10 μM, 48 hours) successfully inhibits the activity of PARP-1 and reduces the production of PAR in A549 cells, which is dose-dependent to some extent[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:2.5 μM, 5 μM and 10 μM
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Incubation Time:48h
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Result:Inhibited the activity of PARP-1 successfully and reduced the production of PAR in cancer cells. PARP-1-IN-1 was dose-dependent to some extent.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic BALB/c nude mice (inoculated MDA-MB-436 cells)[1]
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Dosage:50 mg/kg
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Administration:p.o., daily for 18 days
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Result:Inhibited the growth of MDA-MB-436 tumor significantly, and no significant change in the body weight of PARP-1-IN-1 treated mice.
Chemical Information
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CAS No. 2763840-83-9
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Molecular Weight 392.47
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Formula C23H25FN4O
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SMILES
NC1CCN(CC1)CC2=CC(C3=C4CCNC(C5=C4C(N3)=CC(F)=C5)=O)=CC=C2
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PARP-1-IN-1 Related Classifications
HY-144642 Related Classifications
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