2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. Pan KRas-IN-1

Pan KRas-IN-1 is a pan KRas inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors.

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

Pan KRas-IN-1 Chemical Structure

Pan KRas-IN-1 Chemical Structure

CAS No. : 2791263-84-6

Size Price Stock Quantity
1 mg USD 280 In-stock
5 mg USD 820 In-stock
10 mg USD 1320 In-stock
50 mg   Get quote  
100 mg   Get quote  

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

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Based on 1 publication(s) in Google Scholar

Pan KRas-IN-1 Related Antibodies

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K-Ras H-Ras Ras

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Pan KRas-IN-1 is a pan KRas inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors[1].

IC50 & Target

KRas G12D

9 nM (IC50)

KRas G12S

11 nM (IC50)

KRas G12C

6 nM (IC50)

KRas Q61H

12 mM (IC50)

KRas G12V

29 mM (IC50)

K-Ras WT

32 nM (IC50)

K-Ras G12R

681 nM (IC50)

K-Ras G13D

23 nM (IC50)

In Vitro

Pan KRas-IN-1 (example 5) shows high binding capacity to KRas, with IC50s of <2 nM among different KRas isform, including G12D, G12V, G12R, G12A, G12S, G13D, Q61H, and WT[1].
Pan KRas-IN-1 inhibits the phosphorylation of ERK downstream of KRas in different cells; AsPC-1 (G12D, IC50=9 nM), A549 (G12S, IC50=11 nM), HCT116 (G13D, IC50=23 nM), NCI-H358 (G12C, IC50=6 nM), NCI-H460 (Q61H, IC50=12 nM), NCI-H727 (G12V, IC50=29 nM), MKN1 (WT, IC50=32 nM), PSN-1 (G12R, IC50=681 nM)[1].
Pan KRas-IN-1 (0-3000 nM; 5 d) exhibits anti-proliferative activity against mutation of reststance to Adagrasib (HY-130149, MRTX849) in mouse 3T3 fibroblasts, with IC50s of 32 nM (G12A), 28.1 nM (G12C), 20.25 nM (G12D), 1742 nM (G12R), 94 nM (G12V), 50 nM (G12W), 610 nM (G13D), 58 nM (Q61H)[1].

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

Pan KRas-IN-1 Related Antibodies
Molecular Weight

607.67

Formula

C33H36F3N5O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

FC1=C(C2=CC(O)=CC3=C2C(CC)=C(F)C=C3)N=CC4=C1N=C(N=C4N5C[C@](O)(CCC5)C)OC[C@@]67N(CCC7)C[C@@H](C6)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (164.56 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 1.6456 mL 8.2282 mL 16.4563 mL
5 mM 0.3291 mL 1.6456 mL 3.2913 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 (sealed storage, away from moisture and light). 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.11 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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 (sealed storage, away from moisture and light). 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 1.6456 mL 8.2282 mL 16.4563 mL 41.1408 mL
5 mM 0.3291 mL 1.6456 mL 3.2913 mL 8.2282 mL
10 mM 0.1646 mL 0.8228 mL 1.6456 mL 4.1141 mL
15 mM 0.1097 mL 0.5485 mL 1.0971 mL 2.7427 mL
20 mM 0.0823 mL 0.4114 mL 0.8228 mL 2.0570 mL
25 mM 0.0658 mL 0.3291 mL 0.6583 mL 1.6456 mL
30 mM 0.0549 mL 0.2743 mL 0.5485 mL 1.3714 mL
40 mM 0.0411 mL 0.2057 mL 0.4114 mL 1.0285 mL
50 mM 0.0329 mL 0.1646 mL 0.3291 mL 0.8228 mL
60 mM 0.0274 mL 0.1371 mL 0.2743 mL 0.6857 mL
80 mM 0.0206 mL 0.1029 mL 0.2057 mL 0.5143 mL
100 mM 0.0165 mL 0.0823 mL 0.1646 mL 0.4114 mL
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Pan KRas-IN-1 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:

Pan KRas-IN-12791263-84-6RasazaquinazolinepreparationERKphosphorylationAsPC-1A549HCT116NCI-H358NCI-H460NCI-H727MKN1PSN-1mouse 3T3 fibroblastsInhibitorinhibitorinhibit

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