Lisaftoclax-d8
Lisaftoclax-d8 is the deuterated-labeled Lisaftoclax (HY-129179). 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.
For research use only. We do not sell to patients.
- Formula: C45H40D8ClN7O8S
- Molecular Weight:890.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
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Bcl-2 |
Bcl-xL |
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled CAS 2180923-05-9
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Molecular Weight 890.47
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Formula C45H40D8ClN7O8S
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SMILES
O=C(NS(=O)(C1=CC=C(NC[C@@H]2OCCOC2)C([N+]([O-])=O)=C1)=O)C3=CC=C(N4C([2H])([2H])C([2H])([2H])N(CC(CC5)=C(C6=CC=C(Cl)C=C6)CC75CCC7)C([2H])([2H])C4([2H])[2H])C=C3OC8=CN=C(NC=C9)C9=C8
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Synonyms
APG-2575-d8; Bcl-2/Bcl-xl inhibitor 1-d8
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)