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Technical Data
| Formula | C27H33F3N4O3 |
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| 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 | |||
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* <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. | ||||
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| In vitro | Treatment with EZH2 inhibitor CPI-1205 cause apoptosis in multiple myeloma and plasmacytoma cell models[2]. |
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| 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: |
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Selleck's Lirametostat (CPI-1205) has been cited by 9 publications
| 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 |
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.