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Cat. No.: HY-155090

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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.

For research use only. We do not sell to patients.

CAS No.: 2956666-60-5
Formula: C₂₆H₃₄N₆O₂
Molecular Weight:462.59

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

ATM Inhibitor-8 Chemical Structure

CAS No.: 2956666-60-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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]

All ATM/ATR Isoforms :

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]

In Vitro

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. Further protocols information, click here.

Western Blot Analysis

View Protocol

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

View Protocol

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.

In Vivo

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)	C_max (ng/mL)	T_max (h)	t_1/2 (h)	Cl_obs (L·h/kg)	V_{ss_obs} (L/kg)	AUC_{INF_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.

Chemical Information

CAS No. 2956666-60-5
Molecular Weight 462.59
Formula C₂₆H₃₄N₆O₂
SMILES

CN(C1=NC2=CC(C3=CN=C(C=C3)OCCCN4CCCCC4)=CC=C2N=C1)C(NC(C)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. D Deng, et al. Discovery and Evaluation of 3-Quinoxalin Urea Derivatives as Potent, Selective, and Orally Available ATM Inhibitors Combined with Chemotherapy for the Treatment of Cancer via Goal-Oriented Molecule Generation and Virtual Screening. J Med Chem. 2023 Jul 27， [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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