2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. K-Ras G12C-IN-4

K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRASG12C.

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

K-Ras G12C-IN-4 Chemical Structure

K-Ras G12C-IN-4 Chemical Structure

CAS No. : 2376328-55-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 432 In-stock
Solution
10 mM * 1 mL in DMSO USD 432 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 530 In-stock
25 mg USD 900 In-stock
50 mg USD 1260 In-stock
100 mg USD 1750 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

K-Ras G12C-IN-4 Related Antibodies

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  • Biological Activity

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Description

K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRASG12C[1].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
> 10 μM
Compound: 1
Inhibition of KRAS G12C mutant in human A549 cells assessed as reduction in EGF-induced ERK1/2 phosphorylation incubated for 4 hrs followed by EGF addition by luminescence based assay
Inhibition of KRAS G12C mutant in human A549 cells assessed as reduction in EGF-induced ERK1/2 phosphorylation incubated for 4 hrs followed by EGF addition by luminescence based assay
[PMID: 31531201]
A549 IC50
9.33 μM
Compound: 1
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
[PMID: 31531201]
MIA PaCa-2 IC50
0.067 μM
Compound: 1
Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
[PMID: 31531201]
In Vitro

K-Ras G12C-IN-4 (4 hours) exhibits IC50=0.219 μM for inhibition of MAPK signaling (p-ERK) in MIA PaCa-2 cells[1].
K-Ras G12C-IN-4 (72 hours) translates to a 0.067 μM IC50 for inhibition of cellular viability in a CellTiter-Glo experiment in MIA PaCa-2 cells[1].

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

K-Ras G12C-IN-4 Related Antibodies
Molecular Weight

561.07

Formula

C31H33ClN4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1CN(C(C=C)=O)C1)CN2C(C3CC3)=C(C(N4CC5=C(C(OC)=CC=C5)CC4)=O)C6=C2C(C)=CC(Cl)=C6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (111.39 mM; ultrasonic and warming and heat to 60°C; 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 1.7823 mL 8.9115 mL 17.8231 mL
5 mM 0.3565 mL 1.7823 mL 3.5646 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
=
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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (3.71 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 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 (20.8 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 2

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

    Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 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)

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
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 1.7823 mL 8.9115 mL 17.8231 mL 44.5577 mL
5 mM 0.3565 mL 1.7823 mL 3.5646 mL 8.9115 mL
10 mM 0.1782 mL 0.8912 mL 1.7823 mL 4.4558 mL
15 mM 0.1188 mL 0.5941 mL 1.1882 mL 2.9705 mL
20 mM 0.0891 mL 0.4456 mL 0.8912 mL 2.2279 mL
25 mM 0.0713 mL 0.3565 mL 0.7129 mL 1.7823 mL
30 mM 0.0594 mL 0.2971 mL 0.5941 mL 1.4853 mL
40 mM 0.0446 mL 0.2228 mL 0.4456 mL 1.1139 mL
50 mM 0.0356 mL 0.1782 mL 0.3565 mL 0.8912 mL
60 mM 0.0297 mL 0.1485 mL 0.2971 mL 0.7426 mL
80 mM 0.0223 mL 0.1114 mL 0.2228 mL 0.5570 mL
100 mM 0.0178 mL 0.0891 mL 0.1782 mL 0.4456 mL
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K-Ras G12C-IN-4 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:

K-Ras G12C-IN-42376328-55-9RasInhibitorinhibitorinhibit

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