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Formula | C20H16ClN3O2 |
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Molecular Weight | 365.81 | CAS No. | 1380087-89-7 | |
Solubility (25°C)* | In vitro | DMSO | 73 mg/mL (199.55 mM) | |
Ethanol | 9 mg/mL (24.6 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.) |
Description | Pelabresib (CPI-0610) is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with an IC50 of 39 nM for BRD4-BD1 in TR-FRET assay and currently undergoing human clinical trials for hematological malignancies. CPI-0610 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. | ||||
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In vitro | CPI-0610 inhibits MM(multiple myeloma) cell growth in the presence of cytokines and when co-cultured with bone marrow stromal cells. CPI-0610 induces apoptosis and G1 cell cycle arrest associated with MYC downregulation. However, protein levels of BCL2, NF-κB and MCL1 remain unchanged in MM cells upon BET inhibition. CPI-0610 suppresses Ikaros and IRF4 expression at the levels of both transcription and protein in MM cells[2]. |
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In vivo | In a mouse xenograft model using MV-4-11 acute myeloid leukemia cells, MYC mRNA levels of CPI-0610-treated mice were substantially reduced at 4 h compared to the vehicle control and recovered toward the control level at the later time points, which corresponded with decreasing free concentrations of compound in plasma. BET bromodomain inhibition by CPI-01610 resulted in substantial suppression of tumor growth over the time period examined (41%, 80%, and 74% tumor growth inhibition, respectively), without any significant body weight loss in the animals. On the basis of an acceptable toxicity profile in rat and dog, A common set of toxicities was observed in both species: lymphoid depletion; hypocellularity of the bone marrow with associated anemia and thrombocytopenia; GI mucosal atrophy, erosion, and ulceration; degeneration of the testicular seminiferous epithelium; and mild to moderate hyperglycemia. These toxicities is reversible[1]. |
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Animal Study: |
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Targeting of mutant-p53 and MYC as a novel strategy to inhibit oncogenic SPAG5 activity in triple negative breast cancer [ Cell Death Dis, 2024, 15(8):603] | PubMed: 39164278 |
Ex Vivo Culture Models of Hidradenitis Suppurativa for Defining Molecular Pathogenesis and Treatment Efficacy of Novel Drugs [ Inflammation, 2022, 45(3):1388-1401] | PubMed: 35301634 |
Ex Vivo Culture Models of Hidradenitis Suppurativa for Defining Molecular Pathogenesis and Treatment Efficacy of Novel Drugs [ Inflammation, 2022, 45(3):1388-1401] | PubMed: 35301634 |
Targeting BET Proteins BRD2 and BRD3 in Combination with PI3K-AKT Inhibition as a Therapeutic Strategy for Ovarian Clear Cell Carcinoma [ Mol Cancer Ther, 2021, 20(4):691-703] | PubMed: 33509905 |
Targeting BET proteins BRD2 and BRD3 in combination with PI3K-AKT inhibition as a therapeutic strategy for ovarian clear cell carcinoma [ Mol Cancer Ther, 2021, molcanther.0809.2020] | PubMed: 33509905 |
Ex Vivo Culture Models of Hidradenitis Suppurativa for defining molecular pathogenesis and treatment efficacy of novel drugs [ bioRxiv, 2021, 10.1101/2021.10.11.464007] | PubMed: N/A |
Loss of CHD1 Promotes Heterogeneous Mechanisms of Resistance to AR-Targeted Therapy via Chromatin Dysregulation [ Cancer Cell, 2020, 37(4):584-598.e11] | PubMed: 32220301 |
RETURN POLICY
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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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.