2. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  3. Ras Apoptosis
  4. ARS-853

ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.

For research use only. We do not sell to patients.

ARS-853 Chemical Structure

ARS-853 Chemical Structure

CAS No. : 1629268-00-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 461 In-stock
Solution
10 mM * 1 mL in DMSO USD 461 In-stock
Solid
1 mg USD 187 In-stock
5 mg USD 484 In-stock
10 mg USD 704 In-stock
25 mg USD 1408 In-stock
50 mg USD 2365 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Based on 2 publication(s) in Google Scholar

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K-Ras H-Ras Ras

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation[1][2].

IC50 & Target[1]

KRAS(G12C)

2.5 μM (IC50)

In Vitro

ARS853 is designed to bind KRASG12C with high affinity. Treatment of KRASG12C-mutant lung cancer cells with ARS853 reduces the level of GTP-bound KRAS by more than 95% (10 μM). ARS853 inhibits proliferation with an inhibitory concentration 50% (IC50) of 2.5 μM, which is similar to its IC50 for target inhibition. ARS853 (10 μM) inhibits effector signaling and cell proliferation to varying degrees in six KRASG12C mutant lung cancer cell lines, but not in non-KRASG12C models. Similarly, it completely suppresses the effects of exogenous KRASG12C expression on KRAS-GTP levels, KRAS-BRAF interaction, and ERK signaling. ARS-853 treatment also induces apoptosis in four KRASG12C mutant cell lines. ARS853 selectively reduces KRAS-GTP levels and RAS-effector signaling in KRASG12C-mutant cells, while inhibiting their proliferation and inducing cell death[1]. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation[2].

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

ARS-853 Related Antibodies
Molecular Weight

432.94

Formula

C22H29ClN4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(C2(C)CC2)C=C(NCC(N3CCN(C4CN(C(C=C)=O)C4)CC3)=O)C(O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (57.74 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 2.3098 mL 11.5489 mL 23.0979 mL
5 mM 0.4620 mL 2.3098 mL 4.6196 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (5.77 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 (5.77 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.
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.
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.
Purity & Documentation

Purity: 98.39%

COA (246 KB) HNMR (199 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Purified KRAS (1 μM) is incubated EDTA (10 mM) and GDP (1 mM) or GTPγS (1 mM) at room temperature for 1 h followed by addition of MgCl2 (1 mM) to terminate the reaction. ARS853 (1 μM) is then added and the mixture is incubated for another hour at room temperature. HEK293 cells expressing various KRAS mutants are treated with ARS853. Proteins are extracted using a buffer containing 9M urea, 10 mM DTT and 50 mM ammonium bicarbonate, pH 8, heated to 65°C for 15 min and alkylated using 50 mM iodoacetamide at 37°C for 30 min. The samples are desalted by gel filtration in Zeba spin desalting plates followed by addition of sequencing-grade trypsin to a concentration of 10 μg/ml, and incubation for one hour at 37°C. Heavy isotopic standards (25 fmol) of the KRASG12C target peptide and KRAS normalization peptide are added to the samples followed by desalting in Strata-X polymeric reverse phase plates. LC-MS/MS analysis is performed in a Q Exactive quadrupole orbitrap mass spectrometer under standard condition. The amount of KRASG12C bound by the drug is determined by the ratio of the modified G12C peptide to that of the heavy isotopic standards[1].

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

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 2.3098 mL 11.5489 mL 23.0979 mL 57.7447 mL
5 mM 0.4620 mL 2.3098 mL 4.6196 mL 11.5489 mL
10 mM 0.2310 mL 1.1549 mL 2.3098 mL 5.7745 mL
15 mM 0.1540 mL 0.7699 mL 1.5399 mL 3.8496 mL
20 mM 0.1155 mL 0.5774 mL 1.1549 mL 2.8872 mL
25 mM 0.0924 mL 0.4620 mL 0.9239 mL 2.3098 mL
30 mM 0.0770 mL 0.3850 mL 0.7699 mL 1.9248 mL
40 mM 0.0577 mL 0.2887 mL 0.5774 mL 1.4436 mL
50 mM 0.0462 mL 0.2310 mL 0.4620 mL 1.1549 mL
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ARS-853 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-8531629268-00-3ARS853ARS 853RasApoptosisselective,covalentKRASG12CmutantinactivestatecancerInhibitorinhibitorinhibit

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