IK-595
Based on 1 Customer Validation
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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- Purity: 98.55%
- CAS No.: 3018909-73-1
- 화학식: C24H24ClFIN5O5S
- 분자량:675.90
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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.
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Cell Line:NCI-H2122, AsPC-1, 5637
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Concentration:10 nM
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Incubation Time:up to 96 h
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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.
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.
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Animal Model:BALB/c nude (female)[1]
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Dosage:6 mg/kg
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Administration:p.o.; single dose
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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.
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Animal Model:Rag2/Il2rg-knockout (female) [1]
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Dosage:0.3 mg/kg
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Administration:p.o.; QOD
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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.
Chemical Information
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CAS No. 3018909-73-1
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Appearance Solid
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분자량 675.90
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화학식 C24H24ClFIN5O5S
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Color White to off-white
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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 | 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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