KZ-02 |
Katalog-Nr.GC79477
One-Click Copy Product Info
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KZ-02 is an orally active dual MEK1 / Pim-1 kinase inhibitor, with an IC50 of 1.07 nM against MEK1 and an IC50 of 1.34 μM against Pim-1.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1801756-14-8
Sample solution is provided at 25 µL, 10mM.
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In Vivo, KZ-02 (1 mg/kg; p.o.; once daily; 20 days) inhibits Colo205 colorectal cancer xenograft growth by 56.6% when administered orally at 1 mg/kg once daily for 20 days, with no detectable body weight loss[1].
In Vitro, KZ-02 (0.01-1000 nmol/L; 24-72 h) potently inhibits Colo205 human colorectal cancer cell proliferation with an IC50 of 0.015 nmol/L at 48 h, which is 1033-fold more potent than AZD6244[1]. KZ-02 (1-1000 nmol/L; 2 h, unspecified) inhibits MEK and Pim-1 activity in Colo205 and HT29 human colorectal cancer cells by decreasing ERK and Cdc25C phosphorylation, reducing Pim-1 protein levels, and inhibiting phosphorylation of Pim-1 downstream targets P21Cip1/Waf1, P27Kip1, and Bad[1]. KZ-02 (10 nmol/L; 2 h) increases Pim-1 mRNA levels in Colo205 and HT29 human colorectal cancer cells following 2 h of treatment at 10 nmol/L[1]. KZ-02 (10 nmol/L; 2 h) decreases Pim-1 protein levels in Colo205 and HT29 human colorectal cancer cells by promoting proteasome-dependent degradation[1].
References:
[1]. Li Y, et al. A New Compound with Increased Antitumor Activity by Cotargeting MEK and Pim-1. iScience. 2020;23(7):101254.
| Cas No. | 1801756-14-8 | SDF | |
| Formula | C15H11F2IN4O3S | M.Wt | 492.24 |
| Löslichkeit | Storage | Store at -20°C, sealed storage, away from moisture and light | |
| 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 | 2.0315 mL | 10.1576 mL | 20.3153 mL |
| 5 mM | 406.3 μL | 2.0315 mL | 4.0631 mL |
| 10 mM | 203.2 μL | 1.0158 mL | 2.0315 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: >98.00% 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.)