ARS-1323

Name: ARS-1323
Brand: MedChemExpress
SKU: HY-U00416
Rating: 5.0 (1 reviews)

Cat. No.: HY-U00416 Pureza: 99.67%: Ficha de datos
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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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ARS-1323 Estructura química

No. CAS : 1698024-73-5

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

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Revisión del cliente

Based on 1 publication(s) in Google Scholar

Other Forms of ARS-1323:

ARS-1323-alkyne In-stock
ARS-1630 In-stock
ARS-1620 In-stock

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Ras:

Ver todas las isoformas

K-Ras H-Ras N-Ras Ras

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

IC₅₀ & Target

KRas G12C

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]
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]
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]
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.

Peso molecular

430.84

Fòrmula

C₂₁H₁₇ClF₂N₄O₂

No. CAS

1698024-73-5

Appearance

Solid

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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: ≥ 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.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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.

Pureza y Documentación

Purity: 99.67%

Select Batch:

Ficha de datos (275 KB) SDS (393 KB)

COA (252 KB) HNMR (143 KB) LCMS (94 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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]

Complete Stock Solution Preparation Table

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

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:

ARS-13231698024-73-5ARS1323ARS 1323RasKRAS G12C inhibitorH358 NSCLC cells
Inhibitorinhibitorinhibit

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ARS-1323

Revisión del cliente

Other Forms of ARS-1323:

ARS-1323 Related Antibodies

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Ras:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

ARS-1323 Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

ARS-1323 Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

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