2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. ATM/ATR
  4. ATM Inhibitor-8

ATM Inhibitor-8 (Compound 10r) is a highly potent, selective and orally active ATM inhibitor,with an IC50 of 1.15 nM. ATM Inhibitor-8 exhibits anti-tumor activity.

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ATM Inhibitor-8

ATM Inhibitor-8 構造式

CAS 番号 : 2956666-60-5

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ATM Inhibitor-8 関連抗体

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製品説明

ATM Inhibitor-8 (Compound 10r) is a highly potent, selective and orally active ATM inhibitor,with an IC50 of 1.15 nM. ATM Inhibitor-8 exhibits anti-tumor activity[1].

IC50 & Target

IC50:1.15 nM (ATM)[1]
Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
>9 μM
Compound: 10r
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 6 days by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 6 days by MTT assay
[PMID: 37438997]
HCT-116 IC50
1.69 nM
Compound: 10r
Inhibition of colony formation in human HCT-116 cells preincubated for 1 hr followed by exposure to 2 Gy gamma irradiation and measured after 1 week by crystal violet staining based chemiluminescence assay
Inhibition of colony formation in human HCT-116 cells preincubated for 1 hr followed by exposure to 2 Gy gamma irradiation and measured after 1 week by crystal violet staining based chemiluminescence assay
[PMID: 37438997]
MCF7 IC50
>9 μM
Compound: 10r
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 6 days by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 6 days by MTT assay
[PMID: 37438997]
MCF7 IC50
0.04 μM
Compound: 10r
Synergistic antiproliferative activity against human MCF7 cells assessed as Etoposide IC50 at 200 nM measured after 6 days by MTT assay
Synergistic antiproliferative activity against human MCF7 cells assessed as Etoposide IC50 at 200 nM measured after 6 days by MTT assay
[PMID: 37438997]
MCF7 IC50
0.06 μM
Compound: 10r
Antiproliferative activity against human MCF7 cells assessed as irinotecan IC50 at 200 nM measured after 6 days by MTT assay
Antiproliferative activity against human MCF7 cells assessed as irinotecan IC50 at 200 nM measured after 6 days by MTT assay
[PMID: 37438997]
MCF7 IC50
0.06 μM
Compound: 10r
Synergistic antiproliferative activity against human MCF7 cells assessed as irinotecan IC50 at 100 nM measured after 6 days by MTT assay
Synergistic antiproliferative activity against human MCF7 cells assessed as irinotecan IC50 at 100 nM measured after 6 days by MTT assay
[PMID: 37438997]
MCF7 IC50
0.08 μM
Compound: 10r
Synergistic antiproliferative activity against human MCF7 cells assessed as Etoposide IC50 at 100 nM measured after 6 days by MTT assay
Synergistic antiproliferative activity against human MCF7 cells assessed as Etoposide IC50 at 100 nM measured after 6 days by MTT assay
[PMID: 37438997]
SW-620 IC50
>9 μM
Compound: 10r
Antiproliferative activity against human SW620 cells assessed as reduction in cell viability incubated for 6 days by MTT assay
Antiproliferative activity against human SW620 cells assessed as reduction in cell viability incubated for 6 days by MTT assay
[PMID: 37438997]
SW-620 IC50
0.02 μM
Compound: 10r
Synergistic inhibition of colony formation in human SW620 cells assessed as irinotecan IC50 at 200 nM preincubated for 1 hr followed by irinotecan addition and measured after 1 week by crystal violet staining based chemiluminescence assay
Synergistic inhibition of colony formation in human SW620 cells assessed as irinotecan IC50 at 200 nM preincubated for 1 hr followed by irinotecan addition and measured after 1 week by crystal violet staining based chemiluminescence assay
[PMID: 37438997]
SW-620 IC50
0.22 μM
Compound: 10r
Synergistic antiproliferative activity against human SW620 cells assessed as irinotecan IC50 at 200 nM measured after 6 days by MTT assay
Synergistic antiproliferative activity against human SW620 cells assessed as irinotecan IC50 at 200 nM measured after 6 days by MTT assay
[PMID: 37438997]
SW-620 IC50
0.35 μM
Compound: 10r
Synergistic antiproliferative activity against human SW620 cells assessed as irinotecan IC50 at 100 nM measured after 6 days by MTT assay
Synergistic antiproliferative activity against human SW620 cells assessed as irinotecan IC50 at 100 nM measured after 6 days by MTT assay
[PMID: 37438997]
体外実験

ATM Inhibitor-8 inhibits the proliferation of colorectal cancer cells (HCT116, SW620) and breast cancer cells (MCF-7) [1].
ATM Inhibitor-8(200 nM) inhibits the viability of MCF-7 cell combined with 4.22 μM Etposide (HY-13629) and 0.036 μM Irinotecan (HY-16562)[1].
ATM Inhibitor-8 (200 nM) inhibits the viability of SW620 cell with 0.22 μM Irinotecan (HY-16562) and inhibits cell colony with 0.02 μM[1].

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

ATM Inhibitor-8 関連抗体

Western Blot Analysis

Cell Line: HCT116 cell[1]
Concentration: 200 nM
Incubation Time: 4 h
Result: :Inhibted ATM pathway obviously combined with 25 μM Irinotecan.

Cell Cycle Analysis

Cell Line: HCT116 cell[1]
Concentration: 200 nM
Incubation Time: 48 h
Result: Decreased G0/G1 phase cells and increased G0/G1 phase cells with the concentration increase.
体内実験

ATM Inhibitor-8 inhibits the growth of tumor combined with 40 mg/kg Irinotecan in SW620 mice model [1].
ATM Inhibitor-8(10 mg/kg, i.v.) has a good value of PK in Balb/c mice which means a lower plasma clearance , higher plasma exposure as well as excellent oral bioavailability. [1].

ATM Inhibitor-8 Pharmacokinetic Analysis in Balb/c Mice[1]

Route Dose (mg/kg) Cmax (ng/mL) Tmax (h) t1/2 (h) Clobs (L·h/kg) Vss_obs (L/kg) AUCINF_obs (ng·h/mL) F (%)
i.v. 10 6793.55 0.88 5.29 0.78 5.93 13027.01 /
p.o. 10 10216.65 0.33 3.37 0.73 3.52 13952.23 107.10

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

Animal Model: Mouse xenograft model of human colon cancer[1].
Dosage: 40 mg/kg combined with Irinotecan(40 mg/kg)
Administration: ATM Inhibitor-8, 20 or 40 mg/kg, p.o. once daily for 3 days every week starting 24 h post-irinotecan dosing (40 mg/kg, i.p. once weekly).
Result: Inhibited tumor growth significantly.
分子量

462.59

分子式

C26H34N6O2
CAS 番号
SMILES

CN(C1=NC2=CC(C3=CN=C(C=C3)OCCCN4CCCCC4)=CC=C2N=C1)C(NC(C)C)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
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ATM Inhibitor-8 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:

ATM Inhibitor-82956666-60-5ATM Inhibitor8ATM Inhibitor 8ATM/ATRAtaxia telangiectasia mutatedATM and RAD3 relatedATM InhibitorSW620 xenograft modelsMCF-7 cellHCT116 cellInhibitorinhibitorinhibit

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