[CAS NO. 1200126-26-6] GNE-900
PRODUCTS SPECIFICATIONS [1200126-26-6]
DESCRIPTION [1200126-26-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 367.45 |
| Molecular Formula | C23H21N5 |
| SMILES | N#CC1=NC=C2C(C3=CC(C4=CC=C(CN5CCCCC5)C=C4)=CN=C3N2)=C1 |
Summary
GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC 50 s of 0.0011, 1.5 µM for ChKl, ChK2 , respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis . gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity [1] .
IC50 & Target
|
Chk1 0.0011 μM (IC 50 ) |
Chk2 1.5 μM (IC 50 ) |
In Vitro
GNE-900 (1 µM; 1-48 h) induces apoptosis with increases in the expression of cleaved PARP when combined with gemcitabine (50 nM) in HT-29 cells [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis [1]
| Cell Line: | HT-29 cells |
| Concentration: | 1 µM |
| Incubation Time: | 1-48 h |
| Result: | Inducesd apoptosis with increased the expression of cleaved PARP when combination with gemcitabine (50 nM). |
In Vivo
GNE-900 (2.5-40 mg/kg; p.o.; once) decreases the tumor volume and increases DNA damage, γ-H2AX levels when combinated with gemcitabine (HY-17026) in rats [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Sprague-Dawley rats (HT-29 tumor xenografts) [1] |
| Dosage: | 2.5-40 mg/kg (received a dose of gemcitabine 120 mg/kg) |
| Administration: | P.o.; once |
| Result: | Decreased the tumor volume and resulted in significant enhancement of DNA damage, increased γ-H2AX levels. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.