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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Apoptosis>Bcl-2 inhibitors>ABT-737
ABT-737
  • ABT-737

ABT-737 NEW

Price $64 $77 $139
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: ABT-737 CAS No.: 852808-04-9
Purity: 99.73% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameABT-737
DescriptionABT-737 is a BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w (EC50=30.3 nM/78.7 nM/197.8 nM). ABT-737 exhibits antitumor activity and anti-aging activity.
Cell ResearchCells 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].
Kinase AssayTo 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].
Animal ResearchMice 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].
In vitroMETHODS: AML cell line HL-60 was treated with ABT-737 (10-250 nM) for 24-72 h. Cell growth was detected by live cell counting. RESULTS: HL-60 cells showed high sensitivity to ABT-737 with IC50=50 nM.[1] METHODS: Thyroid cancer cells were treated with ABT-737 (1 μM) for 24 h and cell cycle was detected by flow cytometer. RESULTS: In all five cell lines analyzed, there was a significant increase in cells at the subG1 level, suggesting that ABT-737 induced cell death and DNA breaks.The highest percentage of cells at the subG1 peak was found in ABT-737-treated papillary BHT101 and mesenchymal SW1736 cells (54.8% and 39.9%). [2]
In vivoMETHODS: To test the antitumor activity in vivo, Insulin (0.035 mg per mouse) and anti-PD1 (0.25 mg per mouse) were intraperitoneally injected into C57BL/6 mice bearing mouse colorectal carcinoma tumor MC38 every two days for five administrations. RESULTS: anti-PD1 significantly inhibited the growth of MC38 tumors, while Insulin promoted the growth of MC38 tumors. The therapeutic effect of the combination of Insulin and anti-PD1 on MC38 tumor suppression was attenuated compared to anti-PD1 treatment alone. anti-PD1 significantly increased the number of infiltrating CD8+ T cells, whereas Insulin significantly decreased the number of tumor-infiltrating CD8+ T cells. [4] METHODS: To study virus-induced insulin-dependent diabetes mellitus (IDDM), Insulin (1 mg) was administered orally to RIP-LCMV tg mice twice a week for two months. RESULTS: Insulin treatment was effective in preventing the progression of islet infiltration to overt IDDM in pre-diabetic tg mice. Oral administration of Insulin did not affect the production of LCMV-NP-specific anti auto-cytotoxic T lymphocytes or the infiltration of lymphocytes into the pancreas. [5]
Storagekeep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationH2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (61.47 mM)
KeywordsMitophagy | inhibit | mimetic | HCT116 | Apoptosis | BIM | ABT 737 | BH3 | Autophagy | AML | HL-60 | Bcl-2 Family | Mitochondrial Autophagy | BCL-2/BAX | ABT737 | Inhibitor | ABT-737
Inhibitors RelatedStavudine | Xylitol | Myricetin | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib
Related Compound LibrariesApoptosis Compound Library | Bioactive Compound Library | ReFRAME Related Library | Autophagy Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-COVID-19 Compound Library | Anti-Cancer Active Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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