2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  3. ATM/ATR Apoptosis
  4. A011

A011 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. A011 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). A011 combines with CPT-11 shows antitumor activity.

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A011 Chemical Structure

A011 Chemical Structure

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Description

A011 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. A011 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). A011 combines with CPT-11 shows antitumor activity[1].

IC50 & Target[1]

ATM

1.0 nM (IC50)

In Vitro

A011 (compound 8d) (10, 30, 100 nM; 5 days) increases the sensitivity of SW620 and HCT116 cells to CPT-11 (HY-16562) (100 nM)[1].
A011 (0-100 nM; 24, 72 h) induces apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11[1].
A011 (3, 9, 27, 83, 250 nM) decreases the expression of p-ATM and p-Chk2 in a dose-dependent manner under 1.5 or 3 Gy irradiation conditions in SW620 cells[1].

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

A011 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: SW620, HCT116 cells
Concentration: 10, 30, 100 nM
Incubation Time: 5 days
Result: Increased the sensitivity of SW620 and HCT116 cells to CPT-11 (100 nM).

Cell Cycle Analysis[1]

Cell Line: SW620, HCT116 cells
Concentration: 0-100 nM
Incubation Time: 24 h
Result: Dose-dependent increased in G2/M arrest was noted when A011 was combined with CPT-11 in SW620 and HCT116 cells.

Apoptosis Analysis[1]

Cell Line: SW620, HCT116 cells
Concentration: 0-100 nM
Incubation Time: 72 h
Result: Significantly increased the apoptotic cell populations when combined with CPT-11.

Western Blot Analysis[1]

Cell Line: SW620, HCT116 cells
Concentration: 3, 10, 30 nM
Incubation Time: 24 h
Result: Reduced the expression of p-Chk2 when combined with CPT-11.
In Vivo

A011 (5 mg/kg; i.p.; once daily for 23 days) combines with CPT-11 (5 mg/kg, i.p.; once a week) shows antitumor activity in mice[1].

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

Animal Model: Female nude mice (SW620 tumor xenograft model)[1]
Dosage: 5 mg/kg; CPT-11 (5 mg/kg, i.p.; once a week)
Administration: I.p.; once daily for 23 days
Result: Increased the antitumor activity of CPT-11.
Molecular Weight

452.55

Formula

C27H28N6O
SMILES

CN(C)CCCOC1=NC=C(C2=CC=C(N=CC3=C4N([C@H](C)C5=CC=CC=C5)N=N3)C4=C2)C=C1
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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A011 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:

A011A 011A-011ATM/ATRApoptosisAtaxia telangiectasia mutatedATM and RAD3 relatedantiproliferativeantitumorapoptosisG2/MSW620HCT116 cellsInhibitorinhibitorinhibit

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