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

ARS-853 

Cat. No.: HY-19706 Purity: 98.39%
COA Handling Instructions

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  
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This product is a controlled substance and not for sale in your territory.

Customer Review

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

Appearance

Solid

Formula

C22H29ClN4O3
CAS No.
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)

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
10 mM 0.2310 mL 1.1549 mL 2.3098 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

  • 4.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2 mg/mL (4.62 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
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
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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.

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Keywords:

ARS-8531629268-00-3ARS853ARS 853RasApoptosisselective,covalentKRASG12CmutantinactivestatecancerInhibitorinhibitorinhibit

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