2. MAPK/ERK Pathway Stem Cell/Wnt
  3. MEK ERK
  4. IK-595

IK-595 is a MEK1/MEK2 inhibitor with high affinity (7.39 nM).IK-595 blocks EGF-induced ERK1/2 phosphorylation in AsPC-1 cells with IC50 value of 0.1 nM. IK-595 has oral activity and blood-brain barrier penetration. IK-595 can be used for the research of Ras/MAPK pathway-altered cancers.

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IK-595

IK-595 Chemical Structure

CAS No. : 3018909-73-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

IK-595 Related Antibodies

Top Publications Citing Use of Products

View All MEK Isoform Specific Products:

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MEK1 MEK2 MEK5 MEK MAP2K4/MEK4

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ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

IK-595 is a MEK1/MEK2 inhibitor with high affinity (7.39 nM).IK-595 blocks EGF-induced ERK1/2 phosphorylation in AsPC-1 cells with IC50 value of 0.1 nM. IK-595 has oral activity and blood-brain barrier penetration. IK-595 can be used for the research of Ras/MAPK pathway-altered cancers[1].

In Vitro

IK-595 (3 nM; 4 h) increases MEK-CRAF interaction in HCT-116 cells and promotes MEK interactions with BRAFV600E, class II, and class III mutants in HT-29, NCI-H1755, and NCI-H1666 cells [1].
IK-595 (25 nM; long-term monitoring) in combination with sotorasib (62.5 nM) maintains cell viability inhibition for over 30 days in NCI-H358 cells[1].
IK-595 (3 nM; 120 h) combined with sotorasib (1000 nM) induces more apoptosis in NCI-H358 cells than other MEK inhibitor combinations. IK-595 (10 nM; 120 h) in combination with RMC-7977 (1 nM) increases apoptosis in NCI-H358 cells[1].
IK-595 (3 nM; long-term monitoring) in combination with sotorasib (250 nM) blocks growth of sotorasib-resistant NCI-H358-R cells. IK-595 inhibits ERK1/2 phosphorylation in sotorasib-resistant NCI-H358-R cells[1].

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

IK-595 Related Antibodies

Western Blot Analysis[1]

Cell Line: NCI-H2122, AsPC-1, 5637
Concentration: 10 nM
Incubation Time: up to 96 h
Result: Inhibited ERK1/2 phosphorylation for as long as 96 h in NCI-H2122 and AsPC-1 cells; recovery occurred after 48 h in 5637 cells, delayed relative to reference compounds.
In Vivo

IK-595 (6 mg/kg; p.o.; QOD) exhibits antitumor efficacy in xenograft mice[1].
IK-595 (6 mg/kg; p.o.; single dose) exhibits superior brain pharmacodynamic activity in A549 intracranial and subcutaneous tumor-bearing mice[1].

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

Animal Model: BALB/c nude (female)[1]
Dosage: 6 mg/kg
Administration: p.o.; single dose
Result: Significantly reduced DUSP6 mRNA expression in intracranial tumors compared to trametinib, avutometinib, and selumetinib; Reduced DUSP6 mRNA expression in subcutaneous tumors compared to avutometinib and selumetinib.
Animal Model: Rag2/Il2rg-knockout (female) [1]
Dosage: 0.3 mg/kg
Administration: p.o.; QOD
Result: Demonstrated superior antitumor activity (TGI = 89.27%) compared to trametinib; Maintained more substantial inhibition of tumor ERK1/2 phosphorylation at 4 and 24 hours post-treatment and stronger inhibition of tumor DUSP6 mRNA expression compared to trametinib.
Molecular Weight

675.90

Formula

C24H24ClFIN5O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CNS(=O)(NC1=C(C(OC2=C(C(N(C(NC3=C(C=C(I)C=C3)F)=C2C(NC4CC4)=O)C)=O)C)=CC=C1)Cl)=O
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 : 100 mg/mL (147.95 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 1.4795 mL 7.3975 mL 14.7951 mL
5 mM 0.2959 mL 1.4795 mL 2.9590 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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: ≥ 5 mg/mL (7.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (7.40 mM); Suspended solution

    This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
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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 1.4795 mL 7.3975 mL 14.7951 mL 36.9877 mL
5 mM 0.2959 mL 1.4795 mL 2.9590 mL 7.3975 mL
10 mM 0.1480 mL 0.7398 mL 1.4795 mL 3.6988 mL
15 mM 0.0986 mL 0.4932 mL 0.9863 mL 2.4658 mL
20 mM 0.0740 mL 0.3699 mL 0.7398 mL 1.8494 mL
25 mM 0.0592 mL 0.2959 mL 0.5918 mL 1.4795 mL
30 mM 0.0493 mL 0.2466 mL 0.4932 mL 1.2329 mL
40 mM 0.0370 mL 0.1849 mL 0.3699 mL 0.9247 mL
50 mM 0.0296 mL 0.1480 mL 0.2959 mL 0.7398 mL
60 mM 0.0247 mL 0.1233 mL 0.2466 mL 0.6165 mL
80 mM 0.0185 mL 0.0925 mL 0.1849 mL 0.4623 mL
100 mM 0.0148 mL 0.0740 mL 0.1480 mL 0.3699 mL
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IK-595 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:

IK-5953018909-73-1IK595IK 595MEKERKMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesCRAFERK1/2MEK1pancreatic ductal adenocarcinomaARAFKRAS-G12CMEK2non-small cell lung cancerMAPK pathwayBRAFInhibitorinhibitorinhibit

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