[CAS NO. 784211-09-2] RGB-286147
PRODUCTS SPECIFICATIONS [784211-09-2]
DESCRIPTION [784211-09-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 473.35 |
| Molecular Formula | C23H22Cl2N4O3 |
| SMILES | O=C1C2=C(N(C3=C(Cl)C=CC=C3Cl)N=C2C(C)C)N=C(CC4=CC=C(OCCO)C=C4)N1 |
Summary
IC50 & Target
|
CDK1/cyclinB 48 nM (IC 50 ) |
CDK2/E 15 nM (IC 50 ) |
CDK4/D1 839 nM (IC 50 ) |
cdk6/cyclin D3 232 nM (IC 50 ) |
In Vitro
RGB-286147 (50-100 nM; 24-48 hr) induces cell cycle arrest in the G1 phase, causes a marked inhibition of DNA replication, and induces apoptosis in HCT116 cells
[1]
.
RGB-286147 (100 nM; 48 hr) results in proteolytic cleavage of PARP in HCT116 cells
[1]
.
RGB-286147 (24-72 hr) shows potent and irreversible cell killing activity in HCT116 cells. The IC
50
value for inhibition of colony formation by RGB-286147 is 57 nM
[1]
.
RGB-286147 (48 hr) exhibits broad anti-tumor activity with an average GI
50
value of <10 nM for 60 tumorigenic cell lines. And also inhibits growth of non-cycling HCT116 cells with an IC
50
value of 40 nM
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cycle Analysis [1]
| Cell Line: | HCT116 cells |
| Concentration: | 50 nM and 100 nM |
| Incubation Time: | 24 or 48 hr |
| Result: | Caused a marked inhibition of DNA replication and induced cell cycle arrest. |
Western Blot Analysis [1]
| Cell Line: | HCT116 cells |
| Concentration: | 100 nM |
| Incubation Time: | 48 hr |
| Result: | Resulted in proteolytic cleavage of PARP. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.