2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. ATM/ATR Checkpoint Kinase (Chk) DNA/RNA Synthesis
  4. ART0380

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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ART0380

ART0380 構造式

CAS 番号 : 2267316-76-5

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 209 在庫あり
Solution
10 mM * 1 mL in DMSO USD 209 在庫あり
Solid
5 mg $190 在庫あり
10 mg $270 在庫あり
25 mg $480 在庫あり
50 mg $680 在庫あり
100 mg $950 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 0 publication(s) in Google Scholar

ART0380 関連抗体

Top Publications Citing Use of Products

ATM/ATR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
ATM ATR TRRAP

Checkpoint Kinase (Chk) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Chk1 Chk2 BUBR1

DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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  • 純度とドキュメンテーション

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製品説明

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[1].

IC50 & Target[1]

Chk1

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
7.9 3
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]
体外実験

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.

ART0380 関連抗体

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.
体内実験

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.
臨床実験
分子量

388.49

分子式

C18H24N6O2S
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

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

一般には略語で表示されます：C1V1 = C2V2

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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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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.
純度とドキュメンテーション

純度: 99.90%

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

取扱説明書 (2659 KB)
参考文献

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.

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 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

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

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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

ART03802267316-76-5ART 0380ART-0380ATM/ATRCheckpoint Kinase (Chk)DNA/RNA SynthesisAtaxia telangiectasia mutatedATM and RAD3 relatedCD-1 nude miceDNA damage responseATRChk1Chk1 serine 345 phosphorylationHT-29colorectal adenocarcinoma cellsNSG miceInhibitorinhibitorinhibit

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