2207569-08-0
Chemical Structure
QCA570
- CAS No.: 2207569-08-0
- Formula:C39H33N7O4S
- Molecular Weight:695.79
IUPAC Name: 3-(4-(5-(4-((3-benzyl-9-methyl-4H,6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,4]oxazepin-2-yl)ethynyl)-1H-pyrazol-1-yl)pent-1-yn-1-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione
InChIKey: RTVTYLRQKKDYMQ-UHFFFAOYSA-N
SMILES: O=C(N(C1CCC(NC1=O)=O)C2)C3=C2C(C#CCCCN4N=CC(C#CC(S5)=C(CC6=CC=CC=C6)C(COC7)=C5N8C7=NN=C8C)=C4)=CC=C3
Biological Activity: QCA570 is a pan-BET-BRD PROTAC degrader. QCA570 degrades BRD2/3/4 and BRDT via cereblon and the ubiquitin-proteasome pathway, inhibits the expression of c-MYC, EZH2 and Mcl-1, induces tumor cell apoptosis, cycle arrest and regression, and exerts a synergistic inhibitory effect on Osimertinib (HY-15772)-resistant EGFR-mutant non-small cell lung cancer. QCA570 can be used in the research of acute myeloid leukemia, acute lymphoblastic leukemia, bladder cancer and non-small cell lung cancer[1][2][3][4][5][6].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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QCA570 | 99.30% | QCA570 is a pan-BET-BRD PROTAC degrader. QCA570 degrades BRD2/3/4 and BRDT via cereblon and the ubiquitin-proteasome pathway, inhibits the expression of c-MYC, EZH2 and Mcl-1, induces tumor cell apoptosis, cycle arrest and regression, and exerts a synergistic inhibitory effect on Osimertinib (HY-15772)-resistant EGFR-mutant non-small cell lung cancer. QCA570 can be used in the research of acute myeloid leukemia, acute lymphoblastic leukemia, bladder cancer and non-small cell lung cancer. | ||||||||||||||||||||
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References
- [1]. Qin C, et al. Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. Journal of medicinal chemistry. 2018 Aug 09;61(15):6685-6704. [Content Brief]
- [2]. Wang Q, et al. Lethal activity of BRD4 PROTAC degrader QCA570 against bladder cancer cells. Frontiers in chemistry. 2023;11:1121724.
- [3]. Liu C, et al. The novel BET degrader, QCA570, is highly active against the growth of human NSCLC cells and synergizes with osimertinib in suppressing osimertinib-resistant EGFR-mutant NSCLC cells. American journal of cancer research. 2022;12(2):779-792. [Content Brief]
- [4]. Malathi Kandarp, et al. Superior Pre-Clinical Efficacy of Novel Protac Based BET Degrader in a Large Acute Myeloid Leukemia Cohort, Blood, Volume 134, Supplement 1, 2019, Page 3936, ISSN 0006-4971.
- [5]. Hu Z, et al. Recent Developments in PROTAC-Mediated Protein Degradation: From Bench to Clinic. Chembiochem : a European journal of chemical biology. 2022 Jan 19;23(2):e202100270. [Content Brief]
- [6]. Zou Y, et al. The PROTAC technology in drug development. Cell biochemistry and function. 2019 Jan;37(1):21-30.
