ABT-737

SKU: orb1306485

Description

ABT-737

Research Area

Cell Biology, Neuroscience

Key Properties

• CAS Number: 852808-04-9
• MW: 813.4
• Purity: >98%
• Formula: C₄₂H₄₅ClN₆O₅S₂
• SMILES: CN(C)CCC(CSc1ccccc1)Nc1ccc(cc1[N+]([O-])=O)S(=O)(=O)NC(=O)c1ccc(cc1)N1CCN(Cc2ccccc2-c2ccc(Cl)cc2)CC1
• Target: Bcl-2
• Solubility: Soluble in DMSO (up to 5 mg/ml)

Bioactivity

• Target IC50:
  Bfl-1:>10 μM (EC50)|Bcl-2:30.3 nM(EC50, cell free)|BCL-XL:78.7 nM(EC50, cell free)|MCL1:>10 μM (EC50)|BCL-B:1820 nM(EC50, cell free)|BCL-W:197.8 nM(EC50, cell free)
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• In Vivo:
  METHODS: 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. 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.
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• In Vitro:
  METHODS: 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. 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%).
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• 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 .
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• 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 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, AML, Apoptosis, Bcl-B, Bcl-w, BCL-2/BAX, Bcl-2, Bcl-2 Family, BH3, Bcl-xL, BIM, ABT 737, ABT737, ABT-737, Inhibitor, HCT116, HL-60, inhibit, Mitochondrial Autophagy, mimetic, Mitophagy

Compound Identifiers

PubChem CID

46228957