Art. -Nr.: HY-U00418

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ARS-1620

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

ARS-1620 is an atropisomeric selective KRAS^G12C inhibitor with desirable pharmacokinetics.

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Reinheit: 99.59%
CAS. Nr.: 1698055-85-4
Formel: C₂₁H₁₇ClF₂N₄O₂
Molecular Weight:430.84

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ARS-1620 Chemical Structure

CAS. Nr.: 1698055-85-4

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

ARS-1620 is an atropisomeric selective KRAS^G12C inhibitor with desirable pharmacokinetics.

IC₅₀ & Target^[1]

KRAS(G12C)

Alle Ras Isoform-spezifische Produkte anzeigen :

In Vitro

ARS-1620 is an atropisomeric selective KRAS^G12C 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.

In Vivo

Following a single oral dose or 5 consecutive daily doses, ARS-1620 yields average peak tumor concentrations of 1.5 μM (50 mg/kg) and 5.5 μM (200 mg/kg), respectively, that enables significant KRAS^G12C target occupancy (>=70% G12C-TE at 200 mg/kg) for >24 hr. In MIAPaCa2 xenografts (p.G12C), ARS-1620 significantly inhibits tumor growth (p<0.001) in a dose-dependent manner with marked regression at a dose of 200 mg/kg, given once daily. Across all tumor models employed, ARS-1620 is well tolerated over the entire 3-week treatment period. Moreover, there are no observed clinical signs or toxicity of ARS-1620 in CD-1 mice even at oral doses up to 1,000 mg/kg administered daily over a 7-day period.

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

Chemical Information

CAS. Nr. 1698055-85-4
Appearance Solid
Molecular Weight 430.84
Formel C₂₁H₁₇ClF₂N₄O₂
Color Off-white to light yellow
SMILES

C=CC(N1CCN(C2=C3C=C(Cl)[C@]([C@]4=C(O)C=CC=C4F)=C(F)C3=NC=N2)CC1)=O.[S]
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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

Cell Type-specific Adaptive Signaling Responses to KRASG12C Inhibition. [Abstract]

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

Systematic cysteine scanning identifies a druggable pocket in oncogenic KRAS. [Abstract]

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.
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

Stability-Based Proteomic Methods Add Value to Activity-Based Protein Profiling Studies. [Abstract]

2026 Jun 11. PMID: 42275002
Patent

US20240219403A1.
bioRxiv

2023 Oct 6.
Virginia Commonwealth University

2019 May.

Lösungsmittel & Löslichkeit

In Vitro:

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)

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

2.3210 mL

11.6052 mL

23.2105 mL

5 mM

0.4642 mL

2.3210 mL

4.6421 mL

10 mM

0.2321 mL

1.1605 mL

2.3210 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, 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.

Molaritätsrechner

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

Mass

Konzentration

Volumen

Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)}

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: ≥ 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.

Protocol 2

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.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (4.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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)
g
Dosing Volume (Per Animal)
μL
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

Protokoll

Cell Assay^[1]

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.

Animal Administration^[1]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
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)

Verweise

[1]. Janes MR, et al. Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor. Cell. 2018 Jan 25;172(3):578-589.e17. [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, 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.

Keywords

ARS-1620

13 Cited Publications

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ARS-1620

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

KRAS Targeted Compound Library

Publications Citing Use of MedChemExpress (MCE) ARS-1620

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ARS-1620 Related Classifications

Art. -Nr.: HY-U00418