Search Site
Related Products
ABT-199Bcl-2 inhibitor,potent and selective

ABT-199

Catalog No. A8194
Size Price Stock Qty
10mM (in 1mL DMSO) $320.00 In stock
Evaluation Sample $28.00 In stock
1mg $70.00 In stock
5mg $190.00 In stock
50mg $680.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Winter PS, et al. "RAS signaling promotes resistance to JAK inhibitors by suppressing BAD-mediated apoptosis." Sci Signal. 2014 Dec 23. PMID:25538080
2. 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

Quality Control

Chemical structure

ABT-199

Related Biological Data

ABT-199

Related Biological Data

ABT-199

Related Biological Data

ABT-199

Biological Activity

ABT-199 (GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1.
Targets Bcl-2          
IC50 < 0.010 nM (Ki)          

Protocol

Cell experiment [1]:

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

24h ;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 experiment [1]:

Animal models

Eμ-Myc mice

Dosage form

100 mg/kg ; Oral taken

Applications

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.

ABT-199 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

ABT-199 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 1257044-40-8 SDF Download SDF
Synonyms ABT199, ABT 199, GDC0199, GDC-0199
Chemical Name 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
Canonical SMILES CC1(CCC(=C(C1)C2=CC=C(C=C2)Cl)CN3CCN(CC3)C4=CC(=C(C=C4)C(=O)NS(=O)(=O)C5=CC(=C(C=C5)NCC6CCOCC6)[N+](=O)[O-])OC7=CN=C8C(=C7)C=CN8)C
Formula C45H50ClN7O7S M.Wt 868.44
Solubility >43.4mg/mL in DMSO Storage Store at -20°C
General tips No
Shipping Condition No

View Related Products By Research Topics

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.

Reference

Matthew S. Davids and Anthony Letai. ABT-199: a new hope for selective BCL-2 inhibition. Cancer Cell 2013; 23(2): 139-141