Art. -Nr.: HY-U00416

ARS-1323

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ARS-1323 is a KRAS G12C inhibitor. ARS-1323 specifically binds to the cysteine residue on the mutant K-Ras protein, locks it in the GDP-bound conformation, thereby blocking K-Ras activation and downstream signaling pathways. ARS-1323 can be used to investigate the signal transduction mechanisms and growth characteristics of tumor cells driven by K-Ras G12C.

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Reinheit: 99.67%
CAS. Nr.: 1698024-73-5
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-1323 Chemical Structure

CAS. Nr.: 1698024-73-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

KRas G12C

Alle Ras Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CT26	IC₅₀	>20 μM Compound: ARS-1620	Antiproliferative activity against mouse CT26 cells harboring KRAS G12D mutant assessed as inhibition of cell viability after 24 hrs by MTT assay Antiproliferative activity against mouse CT26 cells harboring KRAS G12D mutant assessed as inhibition of cell viability after 24 hrs by MTT assay	[PMID: 35276423]
HCT-116	IC₅₀	>20 μM Compound: ARS-1620	Antiproliferative activity against human HCT-116 cells harboring KRAS G13D mutant assessed as inhibition of cell viability after 24 hrs by MTT assay Antiproliferative activity against human HCT-116 cells harboring KRAS G13D mutant assessed as inhibition of cell viability after 24 hrs by MTT assay	[PMID: 35276423]
HeLa	IC₅₀	>20 μM Compound: ARS-1620	Antiproliferative activity against human HeLa cells harboring wild type KRAS assessed as inhibition of cell viability after 24 hrs by MTT assay Antiproliferative activity against human HeLa cells harboring wild type KRAS assessed as inhibition of cell viability after 24 hrs by MTT assay	[PMID: 35276423]
HUVEC	IC₅₀	0.7 μM Compound: ARS-1620	Cytotoxicity against HUVEC cells immortalized with TERT assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against HUVEC cells immortalized with TERT assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36842271]
LCLC-103H cell line	IC₅₀	20.2 μM Compound: ARS-1620	Antiproliferative activity against human LCLC-103H cells harboring wild type KRAS assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human LCLC-103H cells harboring wild type KRAS assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36842271]
MIA PaCa-2	IC₅₀	0.12 μM Compound: 1	Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as reduction in cell viability Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as reduction in cell viability	[PMID: 29937982]
MIA PaCa-2	IC₅₀	0.5 μM Compound: ARS-1620	Antiproliferative activity against human MIA PaCa-2 cells harboring homozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MIA PaCa-2 cells harboring homozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36842271]
MIA PaCa-2	IC₅₀	1.06 μM Compound: 1; ARS1620	Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 33309163]
NCI-H1792	IC₅₀	10.9 μM Compound: ARS-1620	Antiproliferative activity against human NCI-H1792 cells harboring heterozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1792 cells harboring heterozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36842271]
NCI-H2030	IC₅₀	0.16 μM Compound: 1	Antiproliferative activity against human NCI-H2030 cells harboring KRAS G12C mutant assessed as reduction in cell viability Antiproliferative activity against human NCI-H2030 cells harboring KRAS G12C mutant assessed as reduction in cell viability	[PMID: 29937982]
NCI-H23	IC₅₀	0.7 μM Compound: 1	Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant assessed as reduction in cell viability Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant assessed as reduction in cell viability	[PMID: 29937982]
NCI-H23	IC₅₀	1.06 μM Compound: ARS-1620	Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant assessed as inhibition of cell growth incubated for 24 hrs by MTT assay Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant assessed as inhibition of cell growth incubated for 24 hrs by MTT assay	[PMID: 35987104]
NCI-H358	IC₅₀	0.2 μM Compound: ARS-1620	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell viability after 24 hrs by MTT assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell viability after 24 hrs by MTT assay	[PMID: 35276423]
NCI-H358	IC₅₀	0.3 μM Compound: ARS-1620	Antiproliferative activity against human NCI-H358 cells harboring heterozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H358 cells harboring heterozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36842271]
NCI-H358	IC₅₀	0.64 μM Compound: 1	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as reduction in cell viability Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as reduction in cell viability	[PMID: 29937982]
NCI-H358	IC₅₀	1.59 μM Compound: ARS-1620	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell growth incubated for 24 hrs by MTT assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell growth incubated for 24 hrs by MTT assay	[PMID: 35987104]
PANC-1	IC₅₀	>20 μM Compound: ARS-1620	Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant assessed as inhibition of cell viability after 24 hrs by MTT assay Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant assessed as inhibition of cell viability after 24 hrs by MTT assay	[PMID: 35276423]
SW1990	IC₅₀	>20 μM Compound: ARS-1620	Antiproliferative activity against human SW1990 cells harboring KRAS G12D mutant assessed as inhibition of cell viability after 24 hrs by MTT assay Antiproliferative activity against human SW1990 cells harboring KRAS G12D mutant assessed as inhibition of cell viability after 24 hrs by MTT assay	[PMID: 35276423]

In Vitro

ARS-1323 blocks the specific binding of [¹⁸F]PFPMD to purified GDP-bound KRAS^G12C oncoprotein^[3].
ARS-1323 (0-120 min) significantly reduces the uptake of [¹⁸F]PFPMD by KRAS^G12C-mutant H358 NSCLC cells after 60 min of incubation^[3].

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

Chemical Information

CAS. Nr. 1698024-73-5
Appearance Solid
Molecular Weight 430.84
Formel C₂₁H₁₇ClF₂N₄O₂
Color White to off-white
SMILES

O=C(C=C)N1CCN(C2=NC=NC3=C2C=C(Cl)C(C4=C(O)C=CC=C4F)=C3F)CC1
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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (232.10 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

2.3210 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

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

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(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: ≥ 2.5 mg/mL (5.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Liansheng Li, et al. Inhibitors of kras g12c. WO2015054572A1. 2016-04-10.

[2]. Li X, et al. First-in-Humans PET Imaging of KRASG12C Mutation Status in Non-Small Cell Lung and Colorectal Cancer Patients Using [¹⁸F]PFPMD. J Nucl Med. 2023;64(12):1880-1888. Published 2023 Dec 1. [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
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
	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

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ARS-1323

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

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cysteine Targeted Covalent 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

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ARS-1323

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

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cysteine Targeted Covalent 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

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ARS-1323 Related Classifications

HY-U00416 Related Classifications