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CPI-360

Catalog No. T6810   CAS 1802175-06-9
Synonyms: Synonym 2, CPI 360, CPI360

CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.

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CPI-360 Chemical Structure
CPI-360, CAS 1802175-06-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 76.00
5 mg In stock $ 175.00
10 mg In stock $ 285.00
25 mg In stock $ 478.00
50 mg In stock $ 687.00
100 mg In stock $ 998.00
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Purity: 99.52%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.
Targets&IC50 EZH1:102.3 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. [1]
In vivo In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%. [1]
Synonyms Synonym 2, CPI 360, CPI360
Molecular Weight 437.53
Formula C25H31N3O4
CAS No. 1802175-06-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 22.5 mg/mL (51.4 mM)

H2O: <1 mg/mL

DMF: 9.0 mg/mL (20.6 mM)

Ethanol: 27.0 mg/mL (61.7 mM)

TargetMolReferences and Literature

1. Vatolin S, et al. Novel Protein Disulfide Isomerase Inhibitor with Anticancer Activity in Multiple Myeloma. Cancer Res. 2016 Jun 1;76(11):3340-50. 2. Felder ChB, et al. Ultrasonic atomization and subsequent polymer desolvation for peptide and protein microencapsulation into biodegradable polyesters. J Microencapsul. 2003;20(5):553-567. 3. Arora S, et al. EZH2 inhibitors are broadly efficacious in multiple myeloma as single agent and in combination with standard of care therapeutics. 2016. 4. Lang S, et al. Transport and metabolic pathway of thymocartin (TP4) in excised bovine nasal mucosa. J Pharm Pharmacol. 1996;48(11):1190-1196.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Histone Modification Compound Library

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TD52 (±)-α-Bisabolol DB1976 dihydrochloride AZD5582 Ecdysone BS-181 SCR7 EPZ004777 hydrochloride

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Keywords

CPI-360 1802175-06-9 Apoptosis Chromatin/Epigenetic Histone Methyltransferase Synonym 2 CPI 360 CPI360 inhibitor inhibit

 

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