2. GPCR/G Protein MAPK/ERK Pathway PI3K/Akt/mTOR Stem Cell/Wnt Apoptosis
  3. Ras PI3K ERK mTOR Apoptosis
  4. RMC-4998

RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRASG12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRASG12C mutant, with an IC50 value of 28 nM. RMC-4998 can inhibit ERK signaling in KRASG12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research.

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RMC-4998 Chemical Structure

RMC-4998 Chemical Structure

CAS No. : 2642037-07-6

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Based on 1 publication(s) in Google Scholar

Other Forms of RMC-4998:

RMC-4998 Related Antibodies

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ERK ERK1 ERK2 ERK5 ERK8

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mTOR mTORC1 mTORC2

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Description

RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRASG12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRASG12C mutant, with an IC50 value of 28 nM. RMC-4998 can inhibit ERK signaling in KRASG12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research[1][2].
IC50 & Target

KRASG12C[1].
In Vitro

RMC-4998 (100 nM, 120 h) disrupts oncogenic signaling in KRASG12C mutant cells by recruiting cyclophilin A (CYPA) to the active state of mutant KRAS[1].
RMC-4998 can inhibit the expression of ERK signaling related proteins and cell proliferation in KRASG12C mutant cancer cells[1].
RMC-4998 (0-1000 nM, 72 h) inhibits lung cancer cell viability by suppressing the PI3K/mTOR and ERK signaling pathways[2].
RMC-4998 (30 nM, 96 h) can inhibit ERK protein phosphorylation and suppress LU65 cell viability[3].

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

RMC-4998 Related Antibodies

Cell Proliferation Assay[1].

Cell Line: KRASG12C mutant cancer cell LU65 and H358 models
Concentration: 100 nM
Incubation Time: 120 h
Result: Inhibited cell proliferation, with an IC50 value of 0.28 nM.

Western Blot Analysis[1].

Cell Line: KRASG12C mutant cancer cell models (H358, H23, H2030, SW873, MIA PaCa-2)
Concentration: 0-10000 nM
Incubation Time: 2 h
Result: Inhibited phosphorylation of ERK signaling related proteins, including PSK, ERK, and CRAF proteins.

Cell Viability Assay[2].

Cell Line: H358, LU65, H2122, LU99A, SW1573 cells
Concentration: 0-1000 nM
Incubation Time: 72 h
Result: Had the strongest inhibitory effect on H358, LU65, and H2122 cells, but its effect was weaker in cell lines that are most resistant to inactive KRASG12C inhibitors such as LU99A and SW1573.
In Vivo

RMC-4998 (10-200 mg/kg; once daily; 28 days; p.o.) inhibits ERK phosphorylation in tumors and exhibits anti-tumor activity in mice carrying NCI-H358 xenografts[1].
RMC-4998 (80 mg/kg; once daily; 4 weeks; p.o.) can promote tumor regression in non-small cell lung cancer mice and has anti-tumor activity[2].
RMC-4998 (100 mg/kg; once daily; p.o.) induces tumor regression and inhibits ERK phosphorylation expression in sotorasib-R LU65 xenograft mice[3].

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

Animal Model: Mice model bearing H358 CDX tumors[1].
Dosage: 10-200 mg/kg
Administration: Oral gavage (p.o.); once daily; 28 days
Result: Inhibited ERK phosphorylation in tumors for about 24 hours and induced cell apoptosis, leading to tumor regression.
Animal Model: The cell-line derived H2122 KRASG12C lung adenocarcinoma xenograft model (CDX)[2].
Dosage: 80 mg/kg
Administration: Oral gavage (p.o.); once daily; 4 weeks
Result: Inhibited tumor growth for 30-35 days.
Animal Model: Sotorasib-R LU65 mice xenograft model[3].
Dosage: 100 mg/kg
Administration: Oral gavage (p.o.); once dailys
Result: Reduced tumor volume and lowered the expression of pERK protein in the tumor.
Molecular Weight

983.25

Formula

C57H74N8O7
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N1CCC[C@@H](C2=O)N1)[C@@H](NC([C@H](C(C)C)N3C([C@@]4(CCN(C(C#CC(C)(C)N(C)C)=O)C4)CC3)=O)=O)CC5=CC(C6=CC(C(CC(C)(C)CO2)=[C@@]([C@@]7=C([C@H](C)OC)N=CC=C7)N8CC)=C8C=C6)=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (101.70 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 1.0170 mL 5.0852 mL 10.1704 mL
5 mM 0.2034 mL 1.0170 mL 2.0341 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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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 (2.54 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.54 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:

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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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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0170 mL 5.0852 mL 10.1704 mL 25.4259 mL
5 mM 0.2034 mL 1.0170 mL 2.0341 mL 5.0852 mL
10 mM 0.1017 mL 0.5085 mL 1.0170 mL 2.5426 mL
15 mM 0.0678 mL 0.3390 mL 0.6780 mL 1.6951 mL
20 mM 0.0509 mL 0.2543 mL 0.5085 mL 1.2713 mL
25 mM 0.0407 mL 0.2034 mL 0.4068 mL 1.0170 mL
30 mM 0.0339 mL 0.1695 mL 0.3390 mL 0.8475 mL
40 mM 0.0254 mL 0.1271 mL 0.2543 mL 0.6356 mL
50 mM 0.0203 mL 0.1017 mL 0.2034 mL 0.5085 mL
60 mM 0.0170 mL 0.0848 mL 0.1695 mL 0.4238 mL
80 mM 0.0127 mL 0.0636 mL 0.1271 mL 0.3178 mL
100 mM 0.0102 mL 0.0509 mL 0.1017 mL 0.2543 mL
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RMC-4998 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:

RMC-49982642037-07-6RMC4998RMC 4998RasPI3KERKmTORApoptosisPhosphoinositide 3-kinaseExtracellular signal regulated kinasesMammalian target of RapamycinKRAS mutationLU65 cellNSCLCanti-tumor activityInhibitorinhibitorinhibit

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