[CAS NO. 1802175-06-9] CPI-360
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PRODUCTS SPECIFICATIONS [1802175-06-9]
Catalog
SLK-S7656
Brand
Selleck
CAS
1802175-06-9
DESCRIPTION [1802175-06-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 437.53 |
| Molecular Formula | C25H31N3O4 |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2856 mL | 11.4278 mL | 22.8556 mL |
| 5 mM | 0.4571 mL | 2.2856 mL | 4.5711 mL |
| 10 mM | 0.2286 mL | 1.1428 mL | 2.2856 mL |
| 50 mM | - | - | - |
Description
CPI-360 is a potent, selective,and SAM-competitive inhibitor with of 102.3 nM, >100-fold selectivity over other methyltransferases.
Targets
| EZH1 [1] |
| 102.3 nM |
In vitro
In KARPAS-422 cells, CPI-360 potently reduces global H3K27me3 and H3K27me2 levels with EC50 of 56 nM and 65 nM, respectively. CPI-360 also causes time-dependent transcriptional changes, and affects the viability of Y641N mutant EZH2-containing KARPAS-422 cells. In addition, CPI-360 gradually arrests KARPAS-422 cells in the G1 cell cycle stage followed by the induction of apoptosis.
In vivo
In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%.
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