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ABT-737

Catalog No. T2099 CAS 852808-04-9

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w (EC50s: 78.7/30.3/197.8 nM).

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ABT-737, CAS 852808-04-9

Pack Size	Availability	Price/USD
5 mg	In stock	$ 64.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 139.00
50 mg	In stock	$ 247.00
100 mg	In stock	$ 433.00
200 mg	In stock	$ 638.00
1 mL * 10 mM (in DMSO)	In stock	$ 71.00

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Purity: 100%

Purity: 99.73%

Purity: 99.3%

Purity: 98.69%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w (EC50s: 78.7/30.3/197.8 nM).
Targets&IC50	BCL-B:1820 nM(EC50, cell free), BCL-W:197.8 nM(EC50, cell free), BCL-XL:78.7 nM(EC50, cell free), BCL2:30.3 nM(EC50, cell free)
In vitro	ABT-737 induced the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. In cells with phosphorylated BCL-2 or increased MCL-1, ABT-737 was inactive. Inhibition of BCL-2 phosphorylation and reduction of MCL-1 expression restored sensitivity to ABT-737 [1]. ABT-737 inhibited proliferation and induced apoptosis in SGC-7901 and MGC-803 cells in concentration- and time-dependent manners. ABT-737 disturbed the binding of B cell lymphoma (Bcl)-2 homologous antagonist killer and Bcl-extra large [2]. ABT-737 does not directly initiate the apoptotic process, but enhances the effects of death signals, displaying synergistic cytotoxicity with chemotherapeutics and radiation. ABT-737 exhibits single-agent-mechanism-based killing of cells from lymphoma and small-cell lung carcinoma lines, as well as primary patient-derived cells [3].
In vivo	ABT-737 and ATO significantly suppressed SGC-7901 xenograft growth, synergistically inhibited tumour growth and induced apoptosis in vivo [2]. H146 tumours were treated with a single dose of ABT-737. A significant increase in caspase-3-positive cells was noted as early as 2 h after treatment, with a 12-fold increase achieved within 16 h. Examination of liver, heart, and intestine revealed no increase in caspase-3 activation in these normal tissues [3]. Treatment with either ABT-737 (100 mg/kg/day) was initiated on the day following inoculation. On day 21 post-treatment, the mean tumor volume, weight, and serum level of sIL-2Ra were significantly lower than those of vehicle-treated mice [4].
Kinase Assay	To determine the binding affinity of GST-BCL-2 family proteins to the FITCconjugated BH3 domain of BIM, FPAs were performed as described. Briefly, 100 nM of GST-BCL-2 family fusion proteins were incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-BIM BH3 peptide was added. Fluorescence polarization was measured using a Detection System after 10 min using the 96-well black plate. IC50s were determined [1].
Cell Research	Cells were seeded into 96-well plates (5 × 10^3 cells/well) and cultured for 12 h at 37 °C, as described above. Then, the medium was replaced with RPMI 1640 containing various concentrations of ATO (1, 2, 4 and 8 nM), ABT-737 (2.5, 5, 10 and 20 μM) or combinations of ATO and ABT-737, and cells were cultured for a further for 24, 48 or 72 h at 37 °C. Cells cultured in RPMI 1640 containing an equal volume of 0.01 M phosphate-buffered saline (PBS, pH 7.4; vehicle) served as controls. Cell viability was measured using Cell Counting Kit-8, according to the manufacturer's instructions. The cell proliferation rate was calculated according to the formula: experimental optical density (OD) value/control OD value × 100%. Experiments were repeated in triplicate [2].
Animal Research	Mice were housed under standard conditions and had free access to water and food, under a 12-h light/12-h dark cycle in a room maintained at 18 – 22 °C and 50 – 65% humidity. SGC7901 cells (5 × 10^6) were subcutaneously inoculated into the right flank of BALB/c mice (H-2b). Tumour volume was measured using callipers and estimated according to the formula: π ? 6 × a2 × b, where a was the short axis, and b was the long axis. After 10 days, when the tumours had reached about 0.2 cm in diameter, the mice were randomly assigned to four groups (n = 8 per group), using a randomization schedule generated by the SAS software package. The groups were: control; ABT-737; ATO; ABT737 + ATO. They received, respectively: vehicle (1% DMSO, 99% 0.01 M PBS; pH 7.4); ABT-737 (50 mg/kg); ATO (2.5 mg/kg); ABT737 (50 mg/kg) + ATO (2.5 mg/kg) intraperitoneally (i.p.) every 2 days. Drugs were dissolved in the vehicle solution. To standardize the experiments, each mouse received a similar volume of solution. After 15 days, the mice were euthanized and the solid SGC-7901 tumours were harvested, fixed with 4% paraformaldehyde, frozen in optimal cutting temperature compound and stored at –80 °C [2].

Molecular Weight	813.43
Formula	C42H45ClN6O5S2
CAS No.	852808-04-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (114.3 mM)

References and Literature

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. 2. Sun XP, et al. ABT-737 Synergizes with Arsenic Trioxide to Induce Apoptosis of Gastric Carcinoma Cells In Vitro and In Vivo.J Int Med Res. 2012;40(4):1251-64. 3. Oltersdorf T, et al. An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature. 2005 Jun 2;435(7042):677-81. 4. Ishitsuka K, et al. Targeting Bcl-2 family proteins in adult T-cell leukemia/lymphoma: in vitro and in vivo effects of the novel Bcl-2 family inhibitor ABT-737. Cancer Lett. 2012 Apr 28;317(2):218-25. 5. Sui B, Wang R, Chen C, et al. Apoptotic Extracellular Vesicles (ApoEVs) Safeguard Liver Homeostasis and Regeneration via Assembling an ApoEV-Golgi Organelle[J]. bioRxiv. 2021

Citations

1. Zhang W, Li X, Jiang M, et al.SOCS3 deficiency-dependent autophagy repression promote the survival of early-stage myeloid-derived suppressor cells in breast cancer by activating the Wnt/mTOR pathway.Journal of Leukocyte Biology.2023: qiad020.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Mitochondria-Targeted Compound Library Cuproptosis Compound Library Anti-Aging Compound Library PPI Inhibitor Library ReFRAME Related Library Anti-COVID-19 Compound Library Hematonosis Compound Library Human Metabolite Library

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Keywords

ABT-737 852808-04-9 Apoptosis Autophagy BCL Mitophagy inhibit mimetic HCT116 BIM ABT 737 BH3 AML HL-60 Bcl-2 Family Mitochondrial Autophagy BCL-2/BAX ABT737 Inhibitor inhibitor

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