IK-595 |
カタログ番号GC79482
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 3018909-73-1
Sample solution is provided at 25 µL, 10mM.
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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].
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].
References:
[1]. Haines E, et al. The MEK-RAF molecular glue IK-595 has potent antitumor activity across RAS/MAPK pathway-altered cancers. Nat Cancer. 2026;7(1):116-130.
| Cas No. | 3018909-73-1 | SDF | |
| Formula | C24H24ClFIN5O5S | M.Wt | 675.9 |
| 溶解度 | DMSO: 100 mg/mL (147.95 mM; Need ultrasonic) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4795 mL | 7.3975 mL | 14.7951 mL |
| 5 mM | 295.9 μL | 1.4795 mL | 2.959 mL |
| 10 mM | 148 μL | 739.8 μL | 1.4795 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)