ATR/PARP1-IN-1
ATR/PARP1-IN-1 is a potent ATR and PARP1 dual inhibitor with IC50s of 17.3 nM and 0.38 nM, respectively. ATR/PARP1-IN-1 effectively reduces cell viability, induces apoptosis and DNA damage. ATR/PARP1-IN-1 significantly impairs triple-negative breast cancer (TNBC) colony formation, migration, and invasion. ATR/PARP1-IN-1 suppresses tumor growth effectively in MDA-MB-468 xenografted mice, with no significant body weight change.
For research use only. We do not sell to patients.
- Formula: C45H41FN10O5
- Molecular Weight:820.87
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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
|
PARP1 0.38 nM (IC50) |
PARP2 5.1 nM (IC50) |
TNKS1 116 nM (IC50) |
TNKS2 740.5 nM (IC50) |
PARP7 28.5 nM (IC50) |
ATM ＞5000 nM (IC50) |
ATR 17.3 nM (IC50) |
PI3Kα ＞2500 nM (IC50) |
DNA-PK ＞5000 nM (IC50) |
ATR/PARP1-IN-1 (Compound B8) shows anti-proliferation activity in TNBC cells with IC50s of 1.89 μM (MDA-MB-231), 0.32 μM (MDA-MB-468), 0.009 μM (MDA-MB-436)[1].
ATR/PARP1-IN-1 (0.5-1 μM, 48 h) induces G2/M cell cycle arrest in MDA-MB-231 cells and MDA-MB-468 cells, with a significantly stronger effect than the combination of Ceralasertib (AZD6738) (HY-19323) and Olaparib (HY-10162)[1].
ATR/PARP1-IN-1 (0.5-1 μM, 72 h) demonstrates a markedly stronger capacity to induce apoptosis than the combination of AZD6738 and Olaparib in MDA-MB-231 and MDA-MB-468 cells as determined by Annexin V/PI staining assay[1].
ATR/PARP1-IN-1 (0.5-1 μM, 10 days) exhibits a significantly greater inhibitory effect on the colony formation rate, migration, and invasion in both MDA-MB-231 and MDA-MB-468 cells compared to either treatment of AZD6738 or Olaparib administered alone, or their combination[1].
ATR/PARP1-IN-1 (1-2 μM, 48 h) interferes with the Epithelial-mesenchymal transition (EMT) of MDA-MB-468 cells[1].
ATR/PARP1-IN-1 (0.5-1 μM, 48 h) induces significant DNA damage in MDA-MB-231 cells and MDA-MB-468 cells[1].
ATR/PARP1-IN-1 (1-2 μM, 48 h) suppresses CHK1 phosphorylation through ATR inhibition in MDA-MB-468 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells and MDA-MB-468 cells
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Concentration:0.5, 1 μM
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Incubation Time:48 h
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Result:Induced G2/M cell cycle arrest in MDA-MB-231 cells and MDA-MB-468 cells.
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Cell Line:MDA-MB-231 cells and MDA-MB-468 cells
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Concentration:0.5, 1 μM
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Incubation Time:72 h
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Result:Induced apoptosis in MDA-MB-231 cells and MDA-MB-468 cells.
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Cell Line:MDA-MB-231 cells and MDA-MB-468 cells
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Concentration:0.5, 1 μM
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Incubation Time:48 h
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Result:Increased tail intensity more markedly than AZD6738, Olaparib, and their combination treatment.
Increased the formation of γH2AX.
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Cell Line:MDA-MB-468 cells
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Concentration:1, 2 μM
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Incubation Time:48 h
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Result:Decreased the protein expression of BCL-2.
Induced more BAX and cleaved-caspase-3 protein expression compared to the combination of AZD6738 and Olaparib.
Increased the expression of the epithelial cell marker E-cadherin.
Decreased the expression of the mesenchymal cell marker Vimentin.
Reduced the protein levels of both ATR and PARP1.
Increased the DSB marker γH2AX.
Decreased CHK1Ser345 phosphorylation.
Enhanced CDK1 Tyr15 phosphorylation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice were subcutaneously with MDA-MB-468 cells (1 x107)[1]
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Dosage:25, 50 mg/kg
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Administration:i.p. daily for 28 days
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Result:Suppressed the growth of MDA-MB-468 xenografted mice.
Decreased Ki67 expression and increased γH2AX and cleaved-caspase-3 expression.
Showed no significant effect on body weight.
Did not cause significant changes in organ structure or cellular morphology of heart, liver, spleen, lungs, and kidneys.
Chemical Information
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Molecular Weight 820.87
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Formula C45H41FN10O5
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SMILES
O=C(NCC1=NC(C2=C3C(NC=C3)=NC=C2)=NC(N4[C@H](C)COCC4)=C1)C5=CC=C(C(N6CCN(C(C7=CC(CC8=NNC(C9=C8C=CC=C9)=O)=CC=C7F)=O)CC6)=O)C=C5
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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)
ATR/PARP1-IN-1 Related Classifications
HY-174828 Related Classifications
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