1820889-23-3
Chemical Structure
Ertabresib
Synonym(s): INCB-057643
- CAS No.: 1820889-23-3
- Formula:C20H21N3O5S
- Molecular Weight:415.46
IUPAC Name: 2,2,4-trimethyl-8-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-6-(methylsulfonyl)-2H-benzo[b][1,4]oxazin-3(4H)-one
InChIKey: VZSAMEOETVNDQH-UHFFFAOYSA-N
SMILES: O=C1C(C)(C)OC2=C(C3=CN(C)C(C4=C3C=CN4)=O)C=C(S(=O)(C)=O)C=C2N1C
Biological Activity: Ertabresib (INCB-057643) is an orally active BET protein inhibitor. Ertabresib blocks gene transcription by targeting the BET protein family, induces cell cycle arrest and apoptosis by downregulating proto-oncogenes such as c-MYC, and additionally reduces the expression of FOXP3 and PD-L1 to improve the immune microenvironment. It also exerts synergistic effects and overcomes drug resistance when combined with chemotherapy and XPO1 inhibitors. Ertabresib can be used in research related to high-grade B-cell lymphoma with MYC and BCL2 rearrangements, pancreatic cancer, pancreatitis, and metastatic castration-resistant prostate cancer[1][2][3].
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Ertabresib | 98.34% | Ertabresib (INCB-057643) is an orally active BET protein inhibitor. Ertabresib blocks gene transcription by targeting the BET protein family, induces cell cycle arrest and apoptosis by downregulating proto-oncogenes such as c-MYC, and additionally reduces the expression of FOXP3 and PD-L1 to improve the immune microenvironment. It also exerts synergistic effects and overcomes drug resistance when combined with chemotherapy and XPO1 inhibitors. Ertabresib can be used in research related to high-grade B-cell lymphoma with MYC and BCL2 rearrangements, pancreatic cancer, pancreatitis, and metastatic castration-resistant prostate cancer. | ||||||||||||||||||||
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Ertabresib (Standard) | ≥98% | Ertabresib (Standard) (INCB-057643 (Standard)) is the analytical standard of Ertabresib (HY-111485). This product is intended for research and analytical applications. Ertabresib (INCB-057643) is an orally active BET protein inhibitor. Ertabresib blocks gene transcription by targeting the BET protein family, induces cell cycle arrest and apoptosis by downregulating proto-oncogenes such as c-MYC, and additionally reduces the expression of FOXP3 and PD-L1 to improve the immune microenvironment. It also exerts synergistic effects and overcomes drug resistance when combined with chemotherapy and XPO1 inhibitors. Ertabresib can be used in research related to high-grade B-cell lymphoma with MYC and BCL2 rearrangements, pancreatic cancer, pancreatitis, and metastatic castration-resistant prostate cancer. | ||||||||||||||||||||
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- [1]. Vázquez R, et al. Efficacy of Novel Bromodomain and Extraterminal Inhibitors in Combination with Chemotherapy for Castration-Resistant Prostate Cancer. European urology oncology. 2021 Jun;4(3):437-446.
- [2]. Deng M, et al. The synergy of the XPO1 inhibitors combined with the BET inhibitor INCB057643 in high-grade B-cell lymphoma via downregulation of MYC expression. Scientific reports. 2023 Oct 29;13(1):18554.
- [3]. Leal AS, et al. The Bromodomain Inhibitor, INCB057643, Targets Both Cancer Cells and the Tumor Microenvironment in Two Preclinical Models of Pancreatic Cancer. Cancers. 2020 Dec 30;13(1):96. [Content Brief]
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