Cat. No.: HY-157941

ART0380

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ART0380 is a potent, selective and orally active ATR kinase inhibitor. ART0380 potently inhibits human ATR-ATRIP complex with an IC₅₀ of 51.7 nM. ART0380 binds the ATP pocket of the ATR-ATRIP complex, blocks ATR-dependent Chk1 serine 345 phosphorylation, and induces cell cycle disorder and DNA damage. ART0380 demonstrates potent and selective antitumor activity in preclinical models with varying types of ataxia-telangiectasia mutated (ATM) gene aberrancy. ART0380 can be used for the research of cancer, such as colorectal cancer and prostate cancer.

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Pureté: 99.90%
CAS No.: 2267316-76-5
Formule: C₁₈H₂₄N₆O₂S
Masse moléculaire:388.49

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ART0380 Chemical Structure

CAS No.: 2267316-76-5

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

Chk1

Voir tous les produits spécifiques à Isoform ATM/ATR :

Voir tous les produits spécifiques à Isoform Checkpoint Kinase (Chk) :

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	7.9 μM Compound: ART0380	Antiproliferative activity against HEK293 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Antiproliferative activity against HEK293 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 38955347]

In Vitro

ART0380 potently inhibits the catalytic activity of the purified human ATR-ATRIP complex with an IC₅₀ of 51.7 nM^[1].
ART0380 potently inhibits ATR-dependent pChk1 (Ser345) phosphorylation in HT-29 colorectal adenocarcinoma cells with an EC₅₀ of 0.022 μM^[1].
ART0380 exhibits minimal inhibition of mTOR pathway-mediated pRPS6 (Ser235/236) phosphorylation in HT-29 colorectal adenocarcinoma cells, with an EC₅₀ range of 6.0 μM, indicating high selectivity for ATR over mTOR^[1].
ART0380 (7 days) potently inhibits proliferation in ATM loss-of-function cancer cell lines (NCI-H23, Granta-519) and replication stress-prone LoVo cells, with weaker activity in normal CCD-18Co colon fibroblasts, showing EC₅₀ values of 0.13, 0.44, 1.0, and 6.4 μM, respectively^[1].
ART0380 (0.001 to 1 μM; 7-10 days) exhibits preferential antiproliferative activity in ATM knockout isogenic cell lines (NCI-H460, Calu-6, PC-3) compared to their ATM-proficient parental counterparts, with EC₅₀ values ranging from 0.045-0.213 μmol/L in ATM KO cells and 0.170-1.215 μM in parental cells^[1].
ART0380 (0.3-1 μM; 24-48 h) induces cell cycle disorder and increases DNA damage (measured via γH2AX foci) in ATM knockout NCI-H460 cells^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

NCI-H460 ATM KO and parental wild-type cells
Concentration:

0.3, 1 μM
Incubation Time:

48 h (continuous); 24 h on/24 h off (intermittent)
Result:

Induced G1-phase accumulation in ATM KO cells with continuous 48-hour treatment.
Caused arrested S-phase accumulation and increased gH2AX foci in geminin-positive cells in ATM KO cells with intermittent 24-hour on/24-hour off schedule, indicating elevated DNA damage.

In Vivo

ART0380 (30-50 mg/kg; p.o. ; once daily) produces significant tumor growth inhibition in ATM-aberrant Granta-519 mantle cell lymphoma xenografts in NSG mice^[1].
ART0380 (100 mg/kg; p.o.; once daily or b.i.d., 3 days on/4 days off.) induces tumor regression in an ATM loss-of-function lung adenocarcinoma PDX model in NSG mice^[1].
ART0380 (10-100 mg/kg; p.o.; daily) produces dose-dependent tumor growth inhibition in LoVo colorectal adenocarcinoma xenografts in CD-1 nude mice^[1].
ART0380 (100 mg/kg; p.o.; twice daily for 3 days followed by 4 days off) produces significant tumor growth inhibition in ATM-aberrant colorectal cancer PDX models with varying degrees of ATM protein loss, but not in wild-type ATM PDX models, in NSG mice^[1].

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

Animal Model:

oVo colorectal adenocarcinoma xenografts CD-1 nude (female, 6-12 weeks old)^[1]
Dosage:

10 mg/kg; 30 mg/kg; 50 mg/kg; 100 mg/kg
Administration:

P.o.; daily
Result:

Induced dose-dependent tumor growth inhibition, with 50 mg/kg and 100 mg/kg producing 84% and 96% tumor growth inhibition, respectively.
Reduced pChk1 Ser345 levels in tumor xenografts after treatment combined with gemcitabine-induced DNA damage.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2267316-76-5
Appearance Solid
Masse moléculaire 388.49
Formule C₁₈H₂₄N₆O₂S
Color White to off-white
SMILES

C[C@@H]1COCCN1C2=NC(C3=CC=NC(N)=C3)=NC(N=[S@](C)(C4CC4)=O)=C2
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (257.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5741 mL

12.8703 mL

25.7407 mL

5 mM

0.5148 mL

2.5741 mL

5.1481 mL

10 mM

0.2574 mL

1.2870 mL

2.5741 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (12.87 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (12.87 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (12.87 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)
Instruction de manipulation (2659 KB)

Références

[1]. Pilié PG, et al. Ataxia-Telangiectasia Mutated Loss-of-Function Displays Variant and Tissue-Specific Differences across Tumor Types. Clin Cancer Res. 2024;30(10):2121-2139. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5741 mL	12.8703 mL	25.7407 mL	64.3517 mL
	5 mM	0.5148 mL	2.5741 mL	5.1481 mL	12.8703 mL
	10 mM	0.2574 mL	1.2870 mL	2.5741 mL	6.4352 mL
	15 mM	0.1716 mL	0.8580 mL	1.7160 mL	4.2901 mL
	20 mM	0.1287 mL	0.6435 mL	1.2870 mL	3.2176 mL
	25 mM	0.1030 mL	0.5148 mL	1.0296 mL	2.5741 mL
	30 mM	0.0858 mL	0.4290 mL	0.8580 mL	2.1451 mL
	40 mM	0.0644 mL	0.3218 mL	0.6435 mL	1.6088 mL
	50 mM	0.0515 mL	0.2574 mL	0.5148 mL	1.2870 mL
	60 mM	0.0429 mL	0.2145 mL	0.4290 mL	1.0725 mL
	80 mM	0.0322 mL	0.1609 mL	0.3218 mL	0.8044 mL
	100 mM	0.0257 mL	0.1287 mL	0.2574 mL	0.6435 mL

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ART0380

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

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Anti-Cancer Metabolism Compound Library

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Glucose Metabolism Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

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Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Voir tous les produits spécifiques à Isoform ATM/ATR

Voir tous les produits spécifiques à Isoform Checkpoint Kinase (Chk)

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

ART0380 Related Classifications

HY-157941 Related Classifications