|
Toll Free: (877) 796-6397 -- USA and Canada only -- |
Fax: +1-832-582-8590 Orders: +1-832-582-8158 |
Tech Support: +1-832-582-8158 Ext:3 Please provide your Order Number in the email. |
Technical Data
| Formula | C25H31N3O4 |
|||
| Molecular Weight | 437.53 | CAS No. | 1802175-06-9 | |
| Solubility (25°C)* | In vitro | DMSO | 20 mg/mL warmed with 50ºC water bath (45.71 mM) | |
| Ethanol | 18 mg/mL warmed with 50ºC water bath (41.14 mM) | |||
| Water | Insoluble | |||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
||||
Preparing Stock Solutions
Biological Activity
| Description | CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases. | ||
|---|---|---|---|
| Targets |
|
||
| 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. [1] | ||
| In vivo | In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%. [1] |
Protocol (from reference)
| Animal Study:[1] |
|
|---|
References
|
Selleck's CPI-360 has been cited by 2 publications
| Dual targeting of EZH1 and EZH2 for the treatment of malignant rhabdoid tumors [ Mol Ther Oncolytics, 2022, 27:14-25] | PubMed: 36212776 |
| Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] | PubMed: 30135193 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.