Lirametostat (CPI-1205)

Catalog No.S8353 Batch:S835301

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Technical Data

Formula

C27H33F3N4O3
Molecular Weight 518.57 CAS No. 1621862-70-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (192.83 mM)
Ethanol 100 mg/mL (192.83 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.)

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Biological Activity

Description Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity.
Targets
EZH2 [1]
(Cell-free assay)		 EZH1 [1]
(Cell-free assay)
2 nM 52 nM
In vitro

Treatment with EZH2 inhibitor CPI-1205 cause apoptosis in multiple myeloma and plasmacytoma cell models[2].
In vivo

CPI-1205 shows excellent oral bioavailability. It was well-tolerated for repeat dosing as demonstrated by the absence of significant body weight loss. CPI-1205 shows relatively high clearance in both rats and dogs (3.19 L/h/kg and 1.41 L/h/kg, respectively) but demonstrates good oral bioavailability in both species(44.6% F in rats and 46.2% F in dogs). CPI-1205 was well-tolerated in the 28-day GLP toxicology studies, and any findings were reversible over the recovery period[1].

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    CB-17 SCID mice

  • Dosages

    160 mg/kg orally twice daily

  • Administration

    p.o

Selleck's Lirametostat (CPI-1205) has been cited by 10 publications

Select EZH2 inhibitors enhance viral mimicry effects of DNMT inhibition through a mechanism involving NFAT:AP-1 signaling [ Sci Adv, 2024, 10(13):eadk4423] PubMed: 38536911
ARID1A-deficient bladder cancer is dependent on PI3K signaling and sensitive to EZH2 and PI3K inhibitors [ JCI Insight, 2022, e155899] PubMed: 35852858
Intrinsic immunogenicity of small cell lung carcinoma revealed by its cellular plasticity [ Cancer Discov, 2021, candisc.0913.2020] PubMed: 33707236
Multi-omics analysis identifies therapeutic vulnerabilities in triple-negative breast cancer subtypes [ Nat Commun, 2021, 12(1):6276] PubMed: 34725325
Druggable epigenetic suppression of interferon-induced chemokine expression linked to MYCN amplification in neuroblastoma [ J Immunother Cancer, 2021, 9(5)e001335] PubMed: 34016720
EZH2 presents a therapeutic target for neuroendocrine tumors of the small intestine [ Sci Rep, 2021, 11(1):22733] PubMed: 34815475
Multiple pharmacological inhibitors targeting the epigenetic suppressor enhancer of Zeste homolog 2 (EZH2) accelerate osteoblast differentiation [ Bone, 2021, S8756-3282(21)00155-1] PubMed: 33940225
Precision Targeting with EZH2 and HDAC Inhibitors in Epigenetically Dysregulated Lymphomas [ Clin Cancer Res, 2019, 10.1158/1078-0432] PubMed: 30979734
Precision Targeting with EZH2 and HDAC Inhibitors in Epigenetically Dysregulated Lymphomas [ Clin Cancer Res, 2019, 25(17):5271-5283] PubMed: 30979734
Precision Targeting with EZH2 and HDAC Inhibitors in Epigenetically Dysregulated Lymphomas [ American Association for Cancer Research, 2019, 10.1158/1078-0432.CCR-18-3989] PubMed: None

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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.

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