KZ-02
Based on 1 Customer Validation
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. KZ-02 reduces the phosphorylation levels of ERK and Cdc25C, and promotes the proteasomal degradation of Pim-1 protein. KZ-02 inhibits cancer cell growth and exerts anti-tumor effects. KZ-02 can be used in the research of colorectal cancer.
For research use only. We do not sell to patients.
- CAS No.: 1801756-14-8
- Formula: C15H11F2IN4O3S
- Molecular Weight:492.24
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Storage:
-20°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)
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
MEK1 1.07 nM (IC50) |
PIM1 1.34 μM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Colo205 and HT29 human colorectal cancer cells
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Concentration:1, 10, 100 and 1000 nM
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Incubation Time:Pretreatment for 2 hours, then 48 hours
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Result:Decreased Pim-1 protein levels and inhibited phosphorylation of ERK (a MEK substrate) and Cdc25C (a Pim-1 substrate) in both cell lines at 10 nM for 2 h.
Decreased Pim-1 protein levels and phosphorylation of P21Cip1/Waf1 (Thr145), P27Kip1 (Thr198), and Bad (Ser112) in Colo205 cells at 1-1000 nM.
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Cell Line:Colo205 and HT29 human colorectal cancer cells
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Concentration:10 nM
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Incubation Time:Pretreatment for 2 hours, then 48 hours
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Result:Significantly increased Pim-1 mRNA levels in both Colo205 and HT29 cells, similar to the effect of AZD6244.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male, ~20 g, subcutaneously injected with 1×107 Colo205 human colon cancer cells)[1]
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Dosage:1 mg/kg
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Administration:p.o.; once daily; 20 days
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Result:Inhibited Colo205 xenograft growth by 56.6%.
Showed no apparent effect on mouse body weight during treatment.
- Kinase activity and phosphorylation assays
- Western Blot
- Protocol for Cell Counting and Cell Density Analysis
- Somatic Cell Culture
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Kinase activity and phosphorylation assays
- Cell Counting-Based Growth Curve Assay
- MTT Cell Proliferation Assay
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 1801756-14-8
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Appearance Solid
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Molecular Weight 492.24
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Formula C15H11F2IN4O3S
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Color Light yellow to yellow
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SMILES
O=C(C1=CC2=C(C(F)=C1NC3=CC=C(C=C3F)I)N=NS2)NOCCO
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°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)
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KZ-02 Related Classifications
HY-185446 Related Classifications
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