1217620-38-6
Chemical Structure
Navitoclax-d8
- CAS No.: 1217620-38-6
- Formula:C47H47D8ClF3N5O6S3
- Molecular Weight:982.66
IUPAC Name: (R)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-(morpholino-d8)-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide
InChIKey: JLYAXFNOILIKPP-YSUYZUONSA-N
SMILES: CC(C)(C1)CCC(C2=CC=C(C=C2)Cl)=C1CN3CCN(C4=CC=C(C=C4)C(NS(=O)(C5=CC(S(C(F)(F)F)(=O)=O)=C(C=C5)N[C@@H](CSC6=CC=CC=C6)CCN7C([2H])([2H])C([2H])([2H])OC([2H])([2H])C7([2H])[2H])=O)=O)CC3
Biological Activity: Navitoclax-d8 is the d8-labeled Navitoclax (HY-10087). Navitoclax (ABT-263 ) is an orally active BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w, with a Ki value of <1 nM for each target. Navitoclax triggers endogenous Apoptosis and downregulates the expression of Survivin and TGFβ2. Navitoclax alleviates fibrosis and induces thrombocytopenia. Navitoclax exhibits anticancer activity against a variety of tumors and enhances the efficacy of chemotherapy and radiotherapy. Navitoclax can be used in the research of acute lymphoblastic leukemia, ovarian cancer, and fibrotic diseases[1][2][3][4][5][6].
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Navitoclax-d8 | 99.71% | Navitoclax-d8 is the d8-labeled Navitoclax (HY-10087). Navitoclax (ABT-263 ) is an orally active BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w, with a Ki value of <1 nM for each target. Navitoclax triggers endogenous Apoptosis and downregulates the expression of Survivin and TGFβ2. Navitoclax alleviates fibrosis and induces thrombocytopenia. Navitoclax exhibits anticancer activity against a variety of tumors and enhances the efficacy of chemotherapy and radiotherapy. Navitoclax can be used in the research of acute lymphoblastic leukemia, ovarian cancer, and fibrotic diseases. | ||||||||||||||||||||
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Navitoclax (Standard) | 99.14% | Navitoclax (Standard) (ABT-263 (Standard)) is the analytical standard of Navitoclax (HY-10087). This product is intended for research and analytical applications. Navitoclax (ABT-263 ) is an orally active BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w, with a Ki value of <1 nM for each target. Navitoclax triggers endogenous Apoptosis and downregulates the expression of Survivin and TGFβ2. Navitoclax alleviates fibrosis and induces thrombocytopenia. Navitoclax exhibits anticancer activity against a variety of tumors and enhances the efficacy of chemotherapy and radiotherapy. Navitoclax can be used in the research of acute lymphoblastic leukemia, ovarian cancer, and fibrotic diseases. | ||||||||||||||||||||
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Navitoclax | 99.64% | Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM. | ||||||||||||||||||||
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- [1]. Lock R, et al. Initial testing (stage 1) of the BH3 mimetic ABT-263 by the pediatric preclinical testing program. Pediatric blood & cancer. 2008 Jun;50(6):1181-9. [Content Brief]
- [2]. Chen J, et al. The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo. Mol Cancer Ther. 2011 Dec;10(12):2340-9. [Content Brief]
- [3]. Chen J, et al. The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo. Molecular cancer therapeutics. 2011 Dec;10(12):2340-9. [Content Brief]
- [4]. Mohamad Anuar NN, et al. Clinical Review: Navitoclax as a Pro-Apoptotic and Anti-Fibrotic Agent. Frontiers in pharmacology. 2020;11:564108. [Content Brief]
- [5]. Wilson WH, et al. Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity. The Lancet. Oncology. 2010 Dec;11(12):1149-59. [Content Brief]
- [6]. Wong M, et al. Navitoclax (ABT-263) reduces Bcl-x(L)-mediated chemoresistance in ovarian cancer models. Molecular cancer therapeutics. 2012 Apr;11(4):1026-35. [Content Brief]