ART0380

Name: ART0380
Brand: MedChemExpress
SKU: HY-157941
Rating: 4.5 (1 reviews)

Cat. No.: HY-157941 Purity: 99.90%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

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

ART0380 Chemical Structure

CAS No. : 2267316-76-5

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Chk1

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.

Clinical Trial

Molecular Weight

388.49

Formula

C₁₈H₂₄N₆O₂S

CAS No.

2267316-76-5

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (280 KB) SDS (254 KB)

COA (252 KB) HNMR (137 KB) RP-HPLC (168 KB) LCMS (232 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

ART0380 Related Classifications

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.

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ART0380

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ART0380 Related Antibodies

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View All DNA/RNA Synthesis Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

ART0380 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

ART0380 Related Classifications

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