ABT-737

Name: ABT-737
Brand: MedChemExpress
SKU: HY-50907
Rating: 5.0 (46 reviews)

Cat. No.: HY-50907 Purity: 99.96%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-x_L and Bcl-w inhibitor with EC₅₀s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research.

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

ABT-737 Chemical Structure

CAS No. : 852808-04-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 89	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 89	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 83	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 330	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 583	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 968	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Customer Review

Based on 46 publication(s) in Google Scholar

Other Forms of ABT-737:

ABT-737-d₈ Get quote

45 Publications Citing Use of MCE ABT-737

: ABT-737 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2019 Oct 1;461:102-111. [Abstract]; Expression of active (cleaved) PARP and active (cleaved) Caspase-3 after 48h of treatment with AGS, 1 μM ABT-737 or 1 μM ABT-737 added to AGS as determined by Western blot. Floating cells are included in lysate.

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Bcl-2

30.3 nM (EC₅₀)

Bcl-xL

78.7 nM (EC₅₀)

Bcl-W

197.8 nM (EC₅₀)

Bcl-B

1820 nM (EC₅₀)

Bfl-1

>10 μM (EC₅₀)

Mcl-1

>10 μM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	IC₅₀	0.74 μM Compound: 1, ABT-737	Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay	[PMID: 22582991]
DU-145	IC₅₀	27.6 μM Compound: 7, ABT-737	Cytotoxicity against human DU145 cells after 48 hrs by cell titer-blue assay Cytotoxicity against human DU145 cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
FL5.12	EC₅₀	30 nM Compound: 1, ABT-737	Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum	[PMID: 18841882]
FL5.12	EC₅₀	7.7 nM Compound: 1, ABT-737	Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum	[PMID: 18841882]
HCT-116	IC₅₀	4.06 μM Compound: 7, ABT-737	Cytotoxicity against human HCT116 cells after 48 hrs by cell titer-blue assay Cytotoxicity against human HCT116 cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
HCT-116	IC₅₀	47.7 μM Compound: ABT-737	Cytotoxicity against human HCT116 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay	[PMID: 22172701]
HL-60	IC₅₀	0.76 μM Compound: 1, ABT-737	Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay	[PMID: 22582991]
HL-60	IC₅₀	0.97 μM Compound: ABT-737	Growth inhibition of human HL60 cells after 72 hrs by MTT assay Growth inhibition of human HL60 cells after 72 hrs by MTT assay	[PMID: 27712939]
Jurkat	IC₅₀	1.38 μM Compound: 7, ABT-737	Cytotoxicity against human Jurkat cells after 48 hrs by cell titer-blue assay Cytotoxicity against human Jurkat cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
K562	IC₅₀	16.4 μM Compound: ABT-737	Induction of apoptosis in Mcl1 dependent human K562 cells after 48 hrs by Annexin V staining based flow cytometry Induction of apoptosis in Mcl1 dependent human K562 cells after 48 hrs by Annexin V staining based flow cytometry	[PMID: 23314054]
K562	IC₅₀	34.7 μM Compound: 1, ABT-737	Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay	[PMID: 22582991]
Leukemia cell	IC₅₀	> 1 μM Compound: 1, ABT-737	Binding affinity to human/mouse chimeric Mcl-1 by luminescence proximity assay Binding affinity to human/mouse chimeric Mcl-1 by luminescence proximity assay	[PMID: 23767404]
Leukemia cell	IC₅₀	> 10 μM Compound: 1, ABT-737	Binding affinity to human/mouse chimeric Mcl-1 by surface plasmon resonance assay Binding affinity to human/mouse chimeric Mcl-1 by surface plasmon resonance assay	[PMID: 23767404]
MCF7	IC₅₀	21.26 μM Compound: 7, ABT-737	Cytotoxicity against human MCF7 cells after 48 hrs by cell titer-blue assay Cytotoxicity against human MCF7 cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
MCF7	IC₅₀	25.33 μM Compound: ABT-737	Growth inhibition of human MCF7 cells after 72 hrs by MTT assay Growth inhibition of human MCF7 cells after 72 hrs by MTT assay	[PMID: 27712939]
MCF7	EC₅₀	4.39 μM Compound: ABT-737	Antiproliferative activity against cisplatin-resistant human MCF7-CR cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against cisplatin-resistant human MCF7-CR cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 35421577]
MDA-MB-435	IC₅₀	> 122.94 μM Compound: ABT-737	Cytotoxicity against human MDA-MB-435 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-435 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay	[PMID: 22172701]
MEF	EC₅₀	> 10000 nM Compound: 1, ABT-737	Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 1% serum Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 1% serum	[PMID: 21366295]
MEF	EC₅₀	> 10000 nM Compound: 1, ABT-737	Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 10% serum Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 10% serum	[PMID: 21366295]
MEF	EC₅₀	0.013 μM Compound: 1; ABT-737	Cytotoxicity against MCL deficient mouse embryonic fibroblast cells assessed as reduction in cell viability in presence of 1 % fetal calf serum measured after 24 hrs by propidium iodide staining based flow cytometric analysis Cytotoxicity against MCL deficient mouse embryonic fibroblast cells assessed as reduction in cell viability in presence of 1 % fetal calf serum measured after 24 hrs by propidium iodide staining based flow cytometric analysis	[PMID: 33904752]
MEF	EC₅₀	2.03 nM Compound: 1, ABT-737	Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 1% serum Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 1% serum	[PMID: 21366295]
MEF	EC₅₀	51 nM Compound: 1, ABT-737	Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum	[PMID: 21366295]
MEF	EC₅₀	51 nM Compound: 1, ABT-737	Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% serum Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% serum	[PMID: 21366295]
MOLT-4	IC₅₀	227 nM Compound: ABT-263	Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 32145645]
NCI-H1417	IC₅₀	0.13 μM Compound: 1, ABT-737	Growth inhibition of human NCI-H1417 cells after 4 days by WST8 assay Growth inhibition of human NCI-H1417 cells after 4 days by WST8 assay	[PMID: 22448988]
NCI-H1417	IC₅₀	173.4 nM Compound: 1, ABT-737	Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay	[PMID: 23448298]
NCI-H1417	IC₅₀	412 nM Compound: 1, ABT-737	Antiproliferative activity against human NCI-H1417 cells after 4 days by WST8 assay Antiproliferative activity against human NCI-H1417 cells after 4 days by WST8 assay	[PMID: 22747598]
NCI-H146	EC₅₀	0.087 μM Compound: 1, ABT-737	Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum	[PMID: 18841882]
NCI-H146	IC₅₀	0.097 μM Compound: 1, ABT-737	Growth inhibition of human NCI-H146 cells after 4 days by WST8 assay Growth inhibition of human NCI-H146 cells after 4 days by WST8 assay	[PMID: 22448988]
NCI-H146	IC₅₀	37 nM Compound: 1, ABT-737	Antiproliferative activity against human NCI-H146 cells after 4 days by WST8 assay Antiproliferative activity against human NCI-H146 cells after 4 days by WST8 assay	[PMID: 22747598]
NCI-H146	IC₅₀	43.8 nM Compound: ABT-263	Antiproliferative activity against human NCI-H146 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Antiproliferative activity against human NCI-H146 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 32145645]
NCI-H187	IC₅₀	137.7 nM Compound: 1, ABT-737	Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay	[PMID: 23448298]
NCI-H1963	IC₅₀	54 nM Compound: 1, ABT-737	Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay	[PMID: 23448298]
NCI-H1963	IC₅₀	59 nM Compound: 1, ABT-737	Antiproliferative activity against human NCI-H1963 cells after 4 days by WST8 assay Antiproliferative activity against human NCI-H1963 cells after 4 days by WST8 assay	[PMID: 22747598]
NCI-H23	IC₅₀	71.16 μM Compound: ABT-737	Growth inhibition of human NCI-H23 cells after 72 hrs by MTT assay Growth inhibition of human NCI-H23 cells after 72 hrs by MTT assay	[PMID: 27712939]
NCI-H460	IC₅₀	8.03 μM Compound: 7, ABT-737	Cytotoxicity against human H460 cells after 48 hrs by cell titer-blue assay Cytotoxicity against human H460 cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
Platelet	IC₅₀	242 nM Compound: ABT-263	Toxicity in human platelet assessed as reduction in cell viability measured after 48 hrs by MTS assay Toxicity in human platelet assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 32145645]
Raji	IC₅₀	93.49 μM Compound: ABT-737	Cytotoxicity against human Raji cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay Cytotoxicity against human Raji cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay	[PMID: 22172701]
RS4-11	IC₅₀	0.27 μM Compound: ABT-737	Induction of apoptosis in Bcl2 dependent human RS4:11 cells after 48 hrs by Annexin V staining based flow cytometry Induction of apoptosis in Bcl2 dependent human RS4:11 cells after 48 hrs by Annexin V staining based flow cytometry	[PMID: 23314054]
RS4-11	IC₅₀	0.33 μM Compound: ABT-737	Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 29453135]
RS4-11	IC₅₀	49 nM Compound: ABT-263	Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 32145645]
SK-OV-3	IC₅₀	46.59 μM Compound: ABT-737	Growth inhibition of human SKOV3 cells after 72 hrs by MTT assay Growth inhibition of human SKOV3 cells after 72 hrs by MTT assay	[PMID: 27712939]
SU.86.86	IC₅₀	4.24 μM Compound: 7, ABT-737	Cytotoxicity against human SU-8686 cells after 48 hrs by cell titer-blue assay Cytotoxicity against human SU-8686 cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
U-266	IC₅₀	27.35 μM Compound: ABT-737	Growth inhibition of human U266 cells after 72 hrs by MTT assay Growth inhibition of human U266 cells after 72 hrs by MTT assay	[PMID: 27712939]

In Vitro

ABT-737 binds BCL-2, BCL-X_L, and BCL-W with high affinity (K_i<1 nM) but binds weakly (K_i>460 nM) to other antiapoptotic BCL-2 family members, including MCL-1 and BFL-1. ABT-737 binds the BH3-binding groove of BCL-X_L and BCL-2^[1].
ABT-737 (100 nM; 1-72 hours) induces apoptosis and synergizes with chemotherapy in HL-60 cells^[1].
ABT-737 (5, 7.5, 10 μM; 72 hours) causes approximately 80% HCT116 cell death. The BAX knockout variant is completely resistant to ABT-737^[1].
ABT-737 has no effect on cell cycle distribution. ABT-737 disrupts BCL-2/BAX heterodimerization and induces BAX conformational change in HL-60 leukemic cells^[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^[3].

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

In Vivo

ABT-737 (20, 30 mg/kg/day; i.p.; for 21 days) suppresses the leukemia burden by 48% and 53% at the 20 and 30 mg/kg dose levels, respectively, in four- to six-week-old CB.17 Scid mice with human leukemia KG-1 cells^[1].
ABT-737 significantly extends survival of mice in this aggressive leukemia model^[1].

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

Molecular Weight

813.43

Formula

C₄₂H₄₅ClN₆O₅S₂

CAS No.

852808-04-9

Appearance

Solid

Color

Yellow to orange

SMILES

CN(CC[C@@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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (61.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

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

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 2% DMSO 40% PEG300 5% Tween-80 53% Saline
Solubility: 2 mg/mL (2.46 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (250 KB) HNMR (324 KB) LCMS (256 KB)

Handling Instructions (2659 KB)

References

[1]. Konopleva M, et al. Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia. Cancer Cell. 2006 Nov;10(5):375-88. [Content Brief]

[2]. Ahamed Saleem, et al. Effect of dual inhibition of apoptosis and autophagy in prostate cancer. Prostate. 2012 Sep 1;72(12):1374-81. [Content Brief]

[3]. Clerc P, et al. Polster BM.Rapid Detection of an ABT-737-Sensitive Primed for Death State in Cells Using Microplate-Based Respirometry.PLoS One. 2012;7(8):e42487. Epub 2012 Aug 3. [Content Brief]

Kinase Assay ^[1]	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 ^[3]	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 ^[1]	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	[1]. Konopleva M, et al. Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia. Cancer Cell. 2006 Nov;10(5):375-88. [Content Brief] [2]. Ahamed Saleem, et al. Effect of dual inhibition of apoptosis and autophagy in prostate cancer. Prostate. 2012 Sep 1;72(12):1374-81. [Content Brief] [3]. Clerc P, et al. Polster BM.Rapid Detection of an ABT-737-Sensitive Primed for Death State in Cells Using Microplate-Based Respirometry.PLoS One. 2012;7(8):e42487. Epub 2012 Aug 3. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.2294 mL	6.1468 mL	12.2936 mL	30.7341 mL
	5 mM	0.2459 mL	1.2294 mL	2.4587 mL	6.1468 mL
	10 mM	0.1229 mL	0.6147 mL	1.2294 mL	3.0734 mL
	15 mM	0.0820 mL	0.4098 mL	0.8196 mL	2.0489 mL
	20 mM	0.0615 mL	0.3073 mL	0.6147 mL	1.5367 mL
	25 mM	0.0492 mL	0.2459 mL	0.4917 mL	1.2294 mL
	30 mM	0.0410 mL	0.2049 mL	0.4098 mL	1.0245 mL
	40 mM	0.0307 mL	0.1537 mL	0.3073 mL	0.7684 mL
	50 mM	0.0246 mL	0.1229 mL	0.2459 mL	0.6147 mL
	60 mM	0.0205 mL	0.1024 mL	0.2049 mL	0.5122 mL

ABT-737 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ABT-737852808-04-9ABT737ABT 737Bcl-2 FamilyApoptosisAutophagyMitophagyMitochondrial AutophagyBH3mimeticBCL-2/BAXBIMAMLHL-60HCT116Inhibitorinhibitorinhibit

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ABT-737

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