Name: ABT-199
Price: 310.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    ABT-199, developed through a structure-based reverse engineering process, is a novel and specific inhibitor of B-cell lymphoma/leukemia 2 (BCL-2) maintaining a sub-nanomolar affinity towards BCL-2 and over three orders of magnitude less affinity towards BCL-XL. It kills a diverse array of non-Hodgkin lymphoma (NHL) and acute myelogenous leukemia cell lines as well as BCL-2 dependent but not BCL-XL dependent cells via suppressing mitochondrial pathway of apoptosis, exhibiting potent antitumor activity against a wide variety of hematologic malignancies while sparing platelets. According to previous studies, ABT-199 is capable of suppressing tumor growth in several human hematologic tumor xenograft models.
- Properties
  - Alternative Name
    
    ABT199, ABT 199, GDC0199, GDC-0199; 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[3-nitro-4-(oxan-4-ylmethylamino)phenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide
    
    CAS Number
    
    1257044-40-8
    
    Molecular Formula
    
    C45H50ClN7O7S
    
    Molecular Weight
    
    868.44
    
    Appearance
    
    A solid
    
    Purity
    
    99.81%
    
    Solubility
    
    ≥43.42 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Linlin Gu, Ranu Surolia, et al. "Targeting Cpt1a-Bcl-2 interaction modulates apoptosis resistance and fibrotic remodeling." Cell Death Differ. 2022 Jan;29(1):118-132. PMID:34413485
    2. Kirsteen J. Campbell, Susan M. Mason, et al. "Breast cancer dependence on MCL-1 is due to its canonical anti-apoptotic function." Cell Death Differ. 2021 Sep;28(9):2589-2600. PMID:33785871
    3. Enyuan Shang, Trang T. T. Nguyen, et al. "Epigenetic Targeting of Mcl-1 Is Synthetically Lethal with Bcl-xL/Bcl-2 Inhibition in Model Systems of Glioblastoma." Cancers 2020, 12(8), 2137;1 August 2020. PMID:32752193
    4. Meyer L, Verbist KC, et al. "JAK/STAT pathway inhibition sensitizes CD8 T cells to dexamethasone-induced apoptosis in hyperinflammation." Blood. 2020;blood.2020006075. PMID:32530039
    5. Shahbandi A, Rao SG, et al. "BH3 mimetics selectively eliminate chemotherapy-induced senescent cells and improve response in TP53 wild-type breast cancer." Cell Death Differ. 2020;10.1038/s41418-020-0564-6. PMID:32457483
    6. Meyer LK, Huang BJ, et al. "Glucocorticoids paradoxically facilitate steroid resistance in T-cell acute lymphoblastic leukemias and thymocytes." J Clin Invest. 2019 Nov 5. pii: 130189. PMID:31687977
    7. Thompson PJ, Shah A, et al. "Targeted Elimination of Senescent Beta Cells Prevents Type 1 Diabetes." Cell Metab. 2019 Feb 14. pii: S1550-4131(19)30021-X. PMID:30799288
    8. Minagawa K, Al-Obaidi M, et al. "Generation of Suicide Gene-Modified Chimeric Antigen Receptor-Redirected T-Cells for Cancer Immunotherapy." Methods Mol Biol. 2019;1895:57-73. PMID:30539529
    9. Wu S, Fatkhutdinov N, et al. "SWI/SNF catalytic subunits' switch drives resistance to EZH2 inhibitors in ARID1A-mutated cells." Nat Commun. 2018 Oct 8;9(1):4116. PMID:30297712
    10. Li Q, Deng Q, et al. "Linking prostate cancer cell AR heterogeneity to distinct castration and enzalutamide responses." Nat Commun. 2018 Sep 6;9(1):3600. PMID:30190514
    11. Kim SR, Lewis JM, et al. "BET inhibition in advanced cutaneous T cell lymphoma is synergistically potentiated by BCL2 inhibition or HDAC inhibition." Oncotarget. 2018 Jun 26;9(49):29193-29207. PMID:30018745
    12. Wilson Xuan Mai."Comprehensive Characterization of the Apoptotic Machinery in Glioblastoma Identifies New Therapeutic Strategies." UNIVERSITY OF CALIFORNIA.2018-01-01.
    13. Tuzlak S, Haschka MD, et al."Differential effects of Vav-promoter-driven overexpression of BCLX and BFL1 on lymphocyte survival and B cell lymphomagenesis." FEBS J. 2018 Apr;285(8):1403-1418. PMID:29498802
    14. Trisciuoglio D, Tupone MG, et al. "BCL-X(L) overexpression promotes tumor progression-associated properties." Cell Death Dis. 2017 Dec 13;8(12):3216. PMID:29238043
    15. Nanjappa SG, McDermott AJ, et al. "Antifungal Tc17 cells are durable and stable, persisting as long-lasting vaccine memory without plasticity towards IFNγ cells." PLoS Pathog. 2017 May 22;13(5):e1006356. PMID:28542595
    16. Delgado-Martin C, Meyer LK, et al. "JAK/STAT pathway inhibition overcomes IL7-induced glucocorticoid resistance in a subset of human T-cell acute lymphoblastic leukemias." Leukemia. 2017 Dec;31(12):2568-2576. PMID:28484265
    17. Minagawa K, Jamil MO, et al. "In Vitro Pre-Clinical Validation of Suicide Gene Modified Anti-CD33 Redirected Chimeric Antigen Receptor T-Cells for Acute Myeloid Leukemia." PLoS One. 2016 Dec 1;11(12):e0166891. PMID:27907031
    18. Xiang XY, Kang JS, et al. "SIRT3 participates in glucose metabolism interruption and apoptosis induced by BH3 mimetic S1 in ovarian cancer cells." Int J Oncol. 2016 Aug;49(2):773-84. PMID:27277143
    19. Kris Cameron Wood,Peter Saville Winter. "Compositions and Methods for Treating Cancer with JAK2 Activity." US Patent App. 15/027,216, 2016.
    20. Winter PS, et al. "RAS signaling promotes resistance to JAK inhibitors by suppressing BAD-mediated apoptosis." Sci Signal. 2014 Dec 23. PMID:25538080

ABT-199

ABT-199

Background

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