2180923-05-9
Chemical Structure
Lisaftoclax
Synonym(s): APG-2575; Bcl-2/Bcl-xl inhibitor 1
- CAS No.: 2180923-05-9
- Formula:C45H48ClN7O8S
- Molecular Weight:882.42
IUPAC Name: (S)-N-((4-(((1,4-dioxan-2-yl)methyl)amino)-3-nitrophenyl)sulfonyl)-2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((6-(4-chlorophenyl)spiro[3.5]non-6-en-7-yl)methyl)piperazin-1-yl)benzamide
InChIKey: FNBXDBIYRAPDPI-BHVANESWSA-N
SMILES: O=C(NS(=O)(C1=CC=C(NC[C@@H]2OCCOC2)C([N+]([O-])=O)=C1)=O)C3=CC=C(N4CCN(CC(CC5)=C(C6=CC=C(Cl)C=C6)CC75CCC7)CC4)C=C3OC8=CN=C(NC=C9)C9=C8
Biological Activity: Lisaftoclax is an orally active, selective BCL-2 inhibitor with a Ki of < 0.1 nM against human BCL-2. Lisaftoclax selectively binds to BCL-2, disrupts the BCL-2:BIM complex, and antagonizes the antiapoptotic function of BCL-2. Lisaftoclax induces BAX/BAK-dependent, caspase-mediated apoptosis, upregulates the pro-death proteins BIM and Noxa, and downregulates mitochondrial respiratory function and ATP production. Lisaftoclax can be used in the research of hematological malignancies including chronic lymphocytic leukemia, multiple myeloma, and diffuse large B-cell lymphoma[1][2][3][4][5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Lisaftoclax | 99.78% | Lisaftoclax is an orally active, selective BCL-2 inhibitor with a Ki of < 0.1 nM against human BCL-2. Lisaftoclax selectively binds to BCL-2, disrupts the BCL-2:BIM complex, and antagonizes the antiapoptotic function of BCL-2. Lisaftoclax induces BAX/BAK-dependent, caspase-mediated apoptosis, upregulates the pro-death proteins BIM and Noxa, and downregulates mitochondrial respiratory function and ATP production. Lisaftoclax can be used in the research of hematological malignancies including chronic lymphocytic leukemia, multiple myeloma, and diffuse large B-cell lymphoma. | ||||||||||||||||||||
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- [1]. Ailawadhi S, et al. Novel BCL-2 Inhibitor Lisaftoclax in Relapsed or Refractory Chronic Lymphocytic Leukemia and Other Hematologic Malignancies: First-in-Human Open-Label Trial. Clinical cancer research : an official journal of the American Association for Cancer Research. 2023 Jul 05;29(13):2385-2393.
- [2]. Deng J, et al. Lisaftoclax (APG-2575) Is a Novel BCL-2 Inhibitor with Robust Antitumor Activity in Preclinical Models of Hematologic Malignancy. Clinical cancer research : an official journal of the American Association for Cancer Research. 2022 Dec 15;28(24):5455-5468.
- [3]. Davids MS, et al. Lisaftoclax (APG-2575) demonstrates activity and safety when given with accelerated ramp-up and then combined with acalabrutinib or rituximab in patients (pts) with chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), including those with prior exposure to venetoclax. Blood. 2024;144(Suppl 1):4614.
- [4]. Ailawadhi S, et al. Lisaftoclax (APG-2575) Combined with Novel Therapeutic Regimens in Patients (pts) with Relapsed or Refractory Multiple Myeloma (R/R MM) or Immunoglobulin Light-Chain (AL) Amyloidosis. Blood. 2024;144(Suppl 1):1022.
- [5]. Wang CW, Chen J. N-(phenylsulfonyl)benzamides and related compounds as bcl-2 inhibitors. WO2018027097 A1. 2018 Feb 8.
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