2. Cell Cycle/DNA Damage Epigenetics PI3K/Akt/mTOR Apoptosis
  3. PARP ATM/ATR Apoptosis
  4. 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.

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ATR/PARP1-IN-1 Chemical Structure

ATR/PARP1-IN-1 Chemical Structure

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ATR/PARP1-IN-1 Related Antibodies

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ATM ATR

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Description

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[1].

IC50 & Target[1]

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)

In Vitro

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.

ATR/PARP1-IN-1 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells and MDA-MB-468 cells
Concentration: 0.5, 1 μM
Incubation Time: 48 h
Result: Induced G2/M cell cycle arrest in MDA-MB-231 cells and MDA-MB-468 cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells and MDA-MB-468 cells
Concentration: 0.5, 1 μM
Incubation Time: 72 h
Result: Induced apoptosis in MDA-MB-231 cells and MDA-MB-468 cells.

Immunofluorescence[1]

Cell Line: MDA-MB-231 cells and MDA-MB-468 cells
Concentration: 0.5, 1 μM
Incubation Time: 48 h
Result: Increased tail intensity more markedly than AZD6738, Olaparib, and their combination treatment.
Increased the formation of γH2AX.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 1, 2 μM
Incubation Time: 48 h
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.
In Vivo

ATR/PARP1-IN-1 (25-50 mg/kg, i.p., bis in die for 28 days) exerts good antitumor efficacy and possesses a favorable safety profile in MDA-MB-468 xenografted mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice were subcutaneously with MDA-MB-468 cells (1 x107)[1]
Dosage: 25, 50 mg/kg
Administration: i.p. daily for 28 days
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.
Molecular Weight

820.87

Formula

C45H41FN10O5
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ATR/PARP1-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ATR/PARP1-IN-1PARPATM/ATRApoptosispoly ADP ribose polymerase Ataxia telangiectasia mutatedATM and RAD3 relatedATRPARP1MDA-MB-468MDA-MB-231cancerInhibitorinhibitorinhibit

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