2. GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt Apoptosis
  3. Ras ERK Apoptosis
  4. RMC-6291

RMC-6291 is an orally active and covalent inhibitor of KRASG12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA). Thus, RMC-6291 prevents KRASG12C(ON) from signaling via steric blockade of RAS effector binding. RMC-6291 inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. RMC-6291 also inhibits the proliferation of KRASG12C mutant cells with a median IC50 of 0.11 nM.

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

RMC-6291 Chemical Structure

RMC-6291 Chemical Structure

CAS No. : 2641998-63-0

Size Price Stock Quantity
1 mg USD 430 In-stock
5 mg USD 1050 In-stock
10 mg USD 1700 In-stock
25 mg USD 3400 In-stock
50 mg USD 5400 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

RMC-6291 Related Antibodies

Top Publications Citing Use of Products

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K-Ras H-Ras Ras

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ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

RMC-6291 is an orally active and covalent inhibitor of KRASG12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA). Thus, RMC-6291 prevents KRASG12C(ON) from signaling via steric blockade of RAS effector binding. RMC-6291 inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. RMC-6291 also inhibits the proliferation of KRASG12C mutant cells with a median IC50 of 0.11 nM[1][2].

IC50 & Target[1]

KRAS(G12C)

 

In Vivo

RMC-6291 (200mg/kg, p.o., qd for 60 d) significantly inhibits tumor growth and induce immunological memory in murine tumor models[3].

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

1012.26

Formula

C55H78FN9O8
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H](OC)C(N=CC=C1)=[C@@]1[C@](N2CC)=C(CC(C)(C)COC([C@H]3NN(C([C@@H](NC([C@H](C(C)C)N(C(C4(F)CCN(C(C#CC(N(C)C)(C)C)=O)CC4)=O)C)=O)C[C@H]5CN6CCO5)=O)CCC3)=O)C7=C2C=CC6=C7
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (98.79 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 0.9879 mL 4.9394 mL 9.8789 mL
5 mM 0.1976 mL 0.9879 mL 1.9758 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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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 (2.47 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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 (2.47 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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: 99.65%

COA (257 KB) HNMR (362 KB) LCMS (100 KB)

Handling Instructions (2659 KB)
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. 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 0.9879 mL 4.9394 mL 9.8789 mL 24.6972 mL
5 mM 0.1976 mL 0.9879 mL 1.9758 mL 4.9394 mL
10 mM 0.0988 mL 0.4939 mL 0.9879 mL 2.4697 mL
15 mM 0.0659 mL 0.3293 mL 0.6586 mL 1.6465 mL
20 mM 0.0494 mL 0.2470 mL 0.4939 mL 1.2349 mL
25 mM 0.0395 mL 0.1976 mL 0.3952 mL 0.9879 mL
30 mM 0.0329 mL 0.1646 mL 0.3293 mL 0.8232 mL
40 mM 0.0247 mL 0.1235 mL 0.2470 mL 0.6174 mL
50 mM 0.0198 mL 0.0988 mL 0.1976 mL 0.4939 mL
60 mM 0.0165 mL 0.0823 mL 0.1646 mL 0.4116 mL
80 mM 0.0123 mL 0.0617 mL 0.1235 mL 0.3087 mL
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RMC-6291 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-62912641998-63-0RMC6291RMC 6291RasERKApoptosisExtracellular signal regulated kinasesKRASG12C (ON)cyclophilin AInhibitorinhibitorinhibit

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