1. Apoptosis
    Autophagy
  2. Bcl-2 Family
    Autophagy
    Mitophagy

ABT-737 

Cat. No.: HY-50907 Purity: 99.59%
Handling Instructions

ABT-737 is a selective and BH3 mimetic Bcl-xLBcl-2 and Bcl-w inhibitor with EC50s of 78.7 nM, 30.3 nM and 197.8 nM, respectively.

For research use only. We do not sell to patients.

ABT-737 Chemical Structure

ABT-737 Chemical Structure

CAS No. : 852808-04-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 91 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 102 In-stock
Estimated Time of Arrival: December 31
50 mg USD 336 In-stock
Estimated Time of Arrival: December 31
100 mg USD 480 In-stock
Estimated Time of Arrival: December 31
200 mg USD 816 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

ABT-737 is a selective and BH3 mimetic Bcl-xLBcl-2 and Bcl-w inhibitor with EC50s of 78.7 nM, 30.3 nM and 197.8 nM, respectively.

IC50 & Target[3]

Bcl-2

30.3 nM (EC50)

Bcl-xL

78.7 nM (EC50)

Bcl-W

197.8 nM (EC50)

Bcl-B

1820 nM (EC50)

Autophagy

 

Mitophagy

 

In Vitro

ABT-737 and ATO inhibits proliferation and induces apoptosis in SGC-7901 and MGC-803 cells in concentration- and time-dependent manner, and shows a synergistic effect. ABT-737 disturbs the binding of B cell lymphoma (Bcl)-2 homologous antagonist killer and Bcl-extra large[1]. ABT-737 induces a BAX/BAK-dependent impairment of maximal O2 consumption rate in sensitive cells. Stable BCL-2 overexpression in MCF10A cells induces an ABT-737-sensitive primed for death state. ABT-737 induces dose-dependent impairment of maximal O2 consumption rate in B-cell lymphoma cells[2]. ABT-737 induces apoptosis and synergizes with chemotherapy,and disrups BCL-2/BAX heterodimerization and induces BAX conformational change in AML cells[3].

In Vivo

ABT-737 (50 mg/kg, i.p.) and ATO significantly suppress SGC-7901 xenograft growth, synergistically inhibit tumour growth and induce apoptosis in vivo[1]. ABT-737 suppresses the leukemia burden by 48% and 53% at the 20 and 30 mg/kg dose levels, respectively[3].

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (61.47 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2294 mL 6.1468 mL 12.2936 mL
5 mM 0.2459 mL 1.2294 mL 2.4587 mL
10 mM 0.1229 mL 0.6147 mL 1.2294 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (3.07 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.07 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (3.07 mM); Suspended solution; Need ultrasonic

References
Kinase Assay
[3]

To determine the binding affinity of GST-BCL-2 family proteins to the FITC-conjugated BH3 domain of BIM (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR), FPAs are performed as follows. Briefly, 100 nM of GST-BCL-2 family fusion proteins are incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-BIM BH3 peptide (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is added. Fluorescence polarization is measured using an Analyst TM AD Assay Detection System after 10 min using the 96-well black plate. IC50s are determined using GraphPad Prism software.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

Cells are treated with ABT-737, ABT-263, or vehicle (DMSO) for 4 h in XF24 assay medium (6×104 MCF10A cells, see medium composition below) or RPMI 1640 medium (1×106 B-cell lymphoma cells) and apoptosis is analyzed by Annexin-V-binding/PI exclusion or by sub-diploid nuclei determination. FACS analysis is performed on Becton Dickinson FACScan or FACScalibur instruments. Data analysis is performed with CellQuest software.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

For intraperitoneal (i.p.) administration, 1 g/mL stock solution of ABT-737 in DMSO is added to a mixture of 30% propylene glycol, 5% Tween 80, 65% D5W (5% dextrose in water) (pH 4−5; final concentration of DMSO ≤ 1%). Mice injected with FD/ΔRaf-1:ER cells are treated with either ABT-737 (20 and 30 mg/kg/mouse every day i.p. for 21 days starting on day 1 post-cell injection (n=9-10 mice per group) or vehicle or left untreated (control); mice injected with human KG-1 cells are treated with 30 mg/kg ABT-737 starting on day 18 post-cell injection. For noninvasive imaging of FD/ΔRaf-1:ER-luc cells, anesthetized mice are injected with 150 mg/kg of D-luciferin and placed for imaging in the In Vivo Imaging System with total imaging time of 2 min.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

813.43

Formula

C₄₂H₄₅ClN₆O₅S₂

CAS No.

852808-04-9

SMILES

CN(CC[[email protected]@H](NC1=CC=C(C=C1[N+]([O-])=O)S(NC(C2=CC=C(C=C2)N3CCN(CC3)CC4=CC=CC=C4C5=CC=C(C=C5)Cl)=O)(=O)=O)CSC6=CC=CC=C6)C

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
ABT-737
Cat. No.:
HY-50907
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ABT-737

Cat. No.: HY-50907