Name: Sabutoclax
Price: 299.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Sabutoclax is an inhibitor of pan-Bcl-2 family with IC50 values of 0.32, 0.31, 0.20 and 0.62 μM for Bcl-2, Bcl-xL, Mcl-1 and Bfl-1, respectively [1].
    Sabutoclax is a derivative of apogossypolone. It showed a high binding affinity to Bcl-xL both in NMR binding assay and in ITC assay, with a Kd value of 0.11μM. Sabutoclax also showed better cell membrane permeability than other apogossypolone derivatives. In PC3 cells, sabutoclax inhibited cell growth with EC50 value of 0.13 μM. In human BP3 cell line, sabutoclax induced cell apoptosis with IC50 value of 0.049 μM. In mice bearing M2182 cancer xenografts, administration of sabutoclax significantly reduced the tumor size. At dose of 5 mg/kg, sabutoclax induced near complete tumor growth suppression [1].
    
    [1] Wei J, Stebbins J L, Kitada S, et al. BI-97C1, an optically pure Apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. Journal of medicinal chemistry, 2010, 53(10): 4166-4176.
- Properties
  - Alternative Name
    
    2,3,5-trihydroxy-7-methyl-N-[(2R)-2-phenylpropyl]-6-[1,6,7-trihydroxy-3-methyl-5-[[(2R)-2-phenylpropyl]carbamoyl]naphthalen-2-yl]naphthalene-1-carboxamide
    
    CAS Number
    
    1228108-65-3
    
    Molecular Formula
    
    C42H40N2O8
    
    Molecular Weight
    
    700.78
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥205.6 mg/mL in DMSO; ≥98.2 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Minieri V, De Dominici M, et al. "Targeting STAT5 or STAT5-Regulated Pathways Suppresses Leukemogenesis of Ph+ Acute Lymphoblastic Leukemia." Cancer Res. 2018 Oct 15;78(20):5793-5807. PMID:30154155
    2. Mishra P J, Mishra P J, Merlino G. "Integrated Genomics Identifies miR-32/MCL-1 Pathway as a Critical Driver of Melanomagenesis: Implications for miR-Replacement and Combination Therapy[J]." PloS one, 2016, 11(11): e0165102. PMID:27846237

Sabutoclax

Sabutoclax

Background

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