ARS-1323
Based on 1 Customer Validation
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.67%
- CAS No.: 1698024-73-5
- Formule: C21H17ClF2N4O2
- Masse moléculaire:430.84
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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KRas G12C |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CT26 | IC50 |
>20 μM
Compound: ARS-1620
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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
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[PMID: 35276423] |
| HCT-116 | IC50 |
>20 μM
Compound: ARS-1620
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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
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[PMID: 35276423] |
| HeLa | IC50 |
>20 μM
Compound: ARS-1620
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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
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[PMID: 35276423] |
| HUVEC | IC50 |
0.7 μM
Compound: ARS-1620
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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
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[PMID: 36842271] |
| LCLC-103H cell line | IC50 |
20.2 μM
Compound: ARS-1620
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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
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[PMID: 36842271] |
| MIA PaCa-2 | IC50 |
0.12 μM
Compound: 1
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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
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[PMID: 29937982] |
| MIA PaCa-2 | IC50 |
0.5 μM
Compound: ARS-1620
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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
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[PMID: 36842271] |
| MIA PaCa-2 | IC50 |
1.06 μM
Compound: 1; ARS1620
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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
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[PMID: 33309163] |
| NCI-H1792 | IC50 |
10.9 μM
Compound: ARS-1620
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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
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[PMID: 36842271] |
| NCI-H2030 | IC50 |
0.16 μM
Compound: 1
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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
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[PMID: 29937982] |
| NCI-H23 | IC50 |
0.7 μM
Compound: 1
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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
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[PMID: 29937982] |
| NCI-H23 | IC50 |
1.06 μM
Compound: ARS-1620
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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
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[PMID: 35987104] |
| NCI-H358 | IC50 |
0.2 μM
Compound: ARS-1620
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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
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[PMID: 35276423] |
| NCI-H358 | IC50 |
0.3 μM
Compound: ARS-1620
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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
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[PMID: 36842271] |
| NCI-H358 | IC50 |
0.64 μM
Compound: 1
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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
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[PMID: 29937982] |
| NCI-H358 | IC50 |
1.59 μM
Compound: ARS-1620
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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
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[PMID: 35987104] |
| PANC-1 | IC50 |
>20 μM
Compound: ARS-1620
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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
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[PMID: 35276423] |
| SW1990 | IC50 |
>20 μM
Compound: ARS-1620
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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
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[PMID: 35276423] |
ARS-1323 blocks the specific binding of [18F]PFPMD to purified GDP-bound KRASG12C oncoprotein[3].
ARS-1323 (0-120 min) significantly reduces the uptake of [18F]PFPMD by KRASG12C-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
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CAS No. 1698024-73-5
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Appearance Solid
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Masse moléculaire 430.84
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Formule C21H17ClF2N4O2
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Color White to off-white
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SMILES
O=C(C=C)N1CCN(C2=NC=NC3=C2C=C(Cl)C(C4=C(O)C=CC=C4F)=C3F)CC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 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.
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: ≥ 2.5 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.
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.
Pureté et documentation
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Fiche technique (275 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
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 |
|---|---|---|---|---|---|
| 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 |
ARS-1323 Related Classifications
HY-U00416 Related Classifications
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