ARS-1620
Based on 13 publication(s) in Google Scholar
ARS-1620 is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.59%
- CAS 番号: 1698055-85-4
- 分子式: C21H17ClF2N4O2
- 分子量:430.84
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 ARS-1620
More- Nat Med. 2019 Apr;25(4):628-640. [Abstract]
- Cancer Discov. 2024 May 8. [Abstract]
- Nat Cancer. 2026 Feb 24. [Abstract]
- Clin Cancer Res. 2021 May 1;27(9):2533-2548. [Abstract]
- Clin Cancer Res. 2020 Nov 15;26(22):5962-5973. [Abstract]
- Clin Cancer Res. 2020 Apr 1;26(7):1633-1643. [Abstract]
- Cell Chem Biol. 2026 Feb 11:S2451-9456(26)00027-9. [Abstract]
- Cell Death Discov. 2023 Feb 6;9(1):45. [Abstract]
- Mol Cancer Ther. 2023 Apr 3;22(4):529-538. [Abstract]
- ACS Chem Biol. 2026 Jun 11. [Abstract]
- Patent. US20240219403A1.
- bioRxiv. 2023 Oct 6.
- Virginia Commonwealth University. 2019 May.
Customer Validation & Images
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WB
生物活性
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KRAS(G12C) |
ARS-1620 is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics. ARS-1620 exhibits complete growth suppression of p.G12C cell lines (IC50=150 nM) with relatively benign effects on control cell lines. It is found that ARS-1620 significantly reduces expression of the gene set in p.G12C mutant cells in a time-dependent manner but not in the p.G12S mutant cells. Following a 5-day treatment period, only a minority of G12C mutant cell lines are sensitive to ARS-1620 under monolayer culture conditions, whereas in 3D-spheroid conditions, ARS-1620 elicits a robust response (p=0.0140)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1698055-85-4
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性状 Solid
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分子量 430.84
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分子式 C21H17ClF2N4O2
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Color Off-white to light yellow
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SMILES
C=CC(N1CCN(C2=C3C=C(Cl)[C@]([C@]4=C(O)C=CC=C4F)=C(F)C3=NC=N2)CC1)=O.[S]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Med
Combination of ERK and autophagy inhibition as a treatment approach for pancreatic cancer. [Abstract]2019 Apr;25(4):628-640. PMID: 30833752 -
Cancer Discov
D3S-001, a KRAS G12C inhibitor with rapid target engagement kinetics, overcomes nucleotide cycling and demonstrates robust preclinical and clinical activities. [Abstract]2024 May 8. PMID: 38717075 -
Nat Cancer
The GENEVA platform models tumor mosaicism to reveal variations of responses to KRAS inhibitors and identify improved drug combinations. [Abstract]2026 Feb 24. PMID: 41735640 -
Clin Cancer Res
2021 May 1;27(9):2533-2548. PMID: 33619172 -
Clin Cancer Res
Epithelial-to-Mesenchymal Transition is a Cause of Both Intrinsic and Acquired Resistance to KRAS G12C Inhibitor in KRAS G12C-Mutant Non-Small Cell Lung Cancer. [Abstract]2020 Nov 15;26(22):5962-5973. PMID: 32900796 -
Clin Cancer Res
Vertical Pathway Inhibition Overcomes Adaptive Feedback Resistance to KRASG12C Inhibition. [Abstract]2020 Apr 1;26(7):1633-1643. PMID: 31776128 -
Cell Chem Biol
2026 Feb 11:S2451-9456(26)00027-9. PMID: 41679298 -
Cell Death Discov
Gemcitabine promotes autophagy and lysosomal function through ERK- and TFEB-dependent mechanisms. [Abstract]2023 Feb 6;9(1):45. PMID: 36746928
ARS-1620 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2023 Feb 6;9(1):45. [Abstract]
In MIA PaCa-2 cells, ARS-1620 (10 µM; 48 h) limites Gemcitabine (10 µM)-induced ERK phosphorylation and autophagy flux, thus reinforcing the contribution of the RAS–ERK pathway in Gemcitabine-induced autophagy.
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Mol Cancer Ther
Efficacious Combination Drug Treatment for Colorectal Cancer that Overcomes Resistance to KRAS G12C Inhibitors. [Abstract]2023 Apr 3;22(4):529-538. PMID: 36780229 -
ACS Chem Biol
2026 Jun 11. PMID: 42275002 -
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溶剤 & 溶解度
DMSO : 125 mg/mL (290.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 11 mg/mL (25.53 mM; ultrasonic and adjust pH to 3 with HCl)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
プロトコル
5×104 cells are seeded into 24 well ULA-plates and allowed to rest overnight. Cells are then treated with DMSO or ARS-1620. After 2 days of treatment, apoptosis and cell death is measured by staining with annexinV-APC and prodidium iodide or by 70% ethanol fixation followed by FxCycle Violet staining to measure DNA content (cell cycle) and percentage of sub-diploid events by flow cytometry[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
For pharmacokinetic (PK) studies 6- to 8-week-old male BALB/c mice are used. To determine oral bioavailability, mice are treated with ARS-1620 by a single intravenous (IV) bolus or oral gavage administration at the doses of 2 and 10 mg/kg, respectively. ARS-1620 concentration in plasma is quantified by LC-MS/MS-based methods. Pharmacokinetic parameters are estimated from mean plasma concentration-time profiles. The area under the curve (AUC) is calculated from time versus concentration data using the linear trapezoidal rule. The oral bioavailability is calculated as the ratio of AUC for ARS-1620 from oral and IV dosage. The calculation is normalized by relative doses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (281 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.3210 mL | 11.6052 mL | 23.2105 mL | 58.0262 mL |
| 5 mM | 0.4642 mL | 2.3210 mL | 4.6421 mL | 11.6052 mL | |
| 10 mM | 0.2321 mL | 1.1605 mL | 2.3210 mL | 5.8026 mL | |
| 15 mM | 0.1547 mL | 0.7737 mL | 1.5474 mL | 3.8684 mL | |
| 20 mM | 0.1161 mL | 0.5803 mL | 1.1605 mL | 2.9013 mL | |
| 25 mM | 0.0928 mL | 0.4642 mL | 0.9284 mL | 2.3210 mL | |
| DMSO | 30 mM | 0.0774 mL | 0.3868 mL | 0.7737 mL | 1.9342 mL |
| 40 mM | 0.0580 mL | 0.2901 mL | 0.5803 mL | 1.4507 mL | |
| 50 mM | 0.0464 mL | 0.2321 mL | 0.4642 mL | 1.1605 mL | |
| 60 mM | 0.0387 mL | 0.1934 mL | 0.3868 mL | 0.9671 mL | |
| 80 mM | 0.0290 mL | 0.1451 mL | 0.2901 mL | 0.7253 mL | |
| 100 mM | 0.0232 mL | 0.1161 mL | 0.2321 mL | 0.5803 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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