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In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Reference
Matthew S. Davids and Anthony Letai. ABT-199: a new hope for selective BCL-2 inhibition. Cancer Cell 2013; 23(2): 139-141
Cell lines
normal human B cells, as well as CD4+ and CD8+ T cells
Preparation method
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.
Reaction Conditions
24 h; 4 μM
Applications
We first determined the in vitro sensitivity to ABT-199 of normal human B cells, as well as CD4+ and CD8+ T cells in peripheral blood sampled from healthy donors (n=9). Significantly, normal peripheral B cells were intrinsically more sensitive (~1000 fold) to ABT-199 than either T cell subset (mean ABT-199 LC50±s.e.m. for B cells, CD4 T cells and CD8 T cells were 3.0±0.9 nM, 2.5±0.6 μM and 1.3±0.7 μM , respectively; B versus CD4 T cells: P=0.008; and B versus CD8 T cells: P=0.004). The result shown that normal human peripheral blood B cells are highly sensitive to ABT-199, unlike T cells and myeloid cells.
Animal models
Eμ-Myc mice
Dosage form
100 mg/kg; Oral taken
We examined the effect of short-term treatment with ABT-199 (used at 100 mg/kg) on the lymphoid subpopulations in vivo to assess this and to model probable changes during therapy of patients. ABT-199 was administered orally, Consistent with our in vitro observations with murine and human cells, the drug substantially reduced peripheral B cells to a similar extent. These data suggested that because of intrinsic insensitivity to selective Bcl-2 inhibition of key B- and T-precursor cells, longer-term administration of ABT-199 may have an impact on normal lymphopoiesis to a lesser degree.
Other notes
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References:
[1] Khaw S L, Mérino D, Anderson M A, et al. Both leukaemic and normal peripheral B lymphoid cells are highly sensitive to the selective pharmacological inhibition of prosurvival Bcl-2 with ABT-199[J]. Leukemia, 2014, 28(6): 1207-1215.
