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Navitoclax
Catalog No. T2101 CAS 923564-51-6
Synonyms: ABT-263
Navitoclax (ABT-263) is a Bcl-2 inhibitor that binds to Bcl-xL, Bcl-2, and Bcl-w proteins (Ki<1 nM) with potent and oral activity. Navitoclax has antitumor activity and induces apoptosis.
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Navitoclax, CAS 923564-51-6
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5 mg
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1 mL * 10 mM (in DMSO)
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Purity: 100%
Purity: 99.67%
Purity: 99.43%
Purity: 99.22%
Purity: 99%
Purity: 98.88%
Purity: 98.88%
Purity: 98.65%
Purity: 98.46%
Purity: 98.13%
Purity: 98%
Purity: 95.82%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description
Navitoclax (ABT-263) is a Bcl-2 inhibitor that binds to Bcl-xL, Bcl-2, and Bcl-w proteins (Ki<1 nM) with potent and oral activity. Navitoclax has antitumor activity and induces apoptosis.
METHODS: Mouse primary B lymphocytes FL5.12/Bcl-xL and FL5.12/Bcl-2 were treated with Navitoclax (0.001-1000 nmol/L) for 48 h. Cell viability was measured using the CellTiter Glo. RESULTS: Navitoclax reversed the protection afforded by overexpression of Bcl-2 or Bcl-xL (EC50 of 60 and 20 nmol/L, respectively). In the presence of IL-3, Navitoclax was ineffective in inducing cell death in the absence of pro-apoptotic stimuli in FL5.12 cells. [1] METHODS: HCC cells PLC/PRF/5, Hep3B, HepG2, and Huh7 were treated with Navitoclax (5 μM) for 18 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: After treatment with Navitoclax, Mcl-1 levels were significantly increased in all HCC cell lines, but Bcl-2 and B cl-xL levels did not change significantly. [2]
In vivo
METHODS: To detect anti-tumor activity in vivo, Navitoclax (100 mg/kg in 10% ethanol+30% polyethylene glycol 400+60% Phosal 50 PG) was administered orally to scid mice bearing human SCLC and ALL xenografts once a day for twenty-one days. RESULTS: Oral administration of Navitoclax resulted in tumor regression of SCLC and ALL xenografts in vivo. [1] METHODS: To assay antitumor activity in vivo, Navitoclax (50-100 mg/kg in 10% ethanol+30% polyethylene glycol 400+60% Phosal 50 PG) was administered orally as a single dose to scid mice bearing human SCLC tumor H146. RESULTS: Single-dose Navitoclax-treated H146 tumors showed a high number of dead and dying cells, including a well-vascularized tumor periphery. [3]
Kinase Assay
ABT-737 and ABT-263 were synthesized as previously described. The enantiomer and BH3-only peptides were synthesized at Abbott. Binding affinities (Ki or IC50) were determined with competitive fluorescence polarization assays. The following peptide probe/protein pairs were used: f-bad (1 nmol/L) and Bcl-xL (6 nmol/L), f-Bax (1 nmol/L) and Bcl-2 (10 nmol/L), f-Bax (1 nmol/L) and Bcl-w (40 nmol/L), f-Noxa (2 nmol/L) and Mcl-1 (40 nmol/L), and f-Bax (1 nmol/L) and Bcl-2-A1 (15 nmol/L). Binding affinities for Bcl-xL were also determined using a time-resolved fluorescence resonance energy transfer assay. Bcl-xL (1 nmol/L, His tagged) was mixed with 200 nmol/L f-Bak, 1 nmol/L Tb-labeled anti-His antibody, and compound at room temperature for 30 min. Fluorescence was measured on an Envision plate reader using a 340/35 nm excitation filter and 520/525 (f-Bak) and 495/510 nm (Tb-labeled anti-His antibody) emission filters. Dissociation constants (Ki) were determined using Wang's equation [1].
Cell Research
Human tumor cell lines were maintained at 37°C containing 5% CO2. SCLC cell lines were cultured in RPMI 1640 with 10% fetal bovine serum (FBS), 1% sodium pyruvate, 25 mmol/L HEPES, 4.5 g/L glucose, and 1% penicillin/streptomycin. Leukemia and lymphoma cell lines were cultured in RPMI 1640 supplemented with 10% FBS and 1% penicillin/streptomycin. Cells (1 × 10^4–5 × 10^4) were treated for 48 h in 96-well culture plates in a final volume of 100 μL and cytotoxicity was assessed with the CellTiter Glo assay [1].
Animal Research
C.B.-17 scid-bg or C.B.-17 scid mice were implanted with 5 × 10^6 (1 × 10^6 for DoHH2) cells in 0.2 mL 50% Matrigel s.c. into the right flank. Tumor-bearing mice were size matched (~235 mm3; day 0) into treatment and control groups, ear tagged, and monitored individually. Tumor volume was measured two to three times weekly by electronic calipers (volume = length × width2 / 2). Tumor growth inhibition was calculated based on the difference in mean tumor volumes between treated and appropriate vehicle control groups. Partial response (PR) is defined as ≥50% tumor growth inhibition, and complete response (CR) is defined as nonpalpable tumor. All studies used 8 to 10 mice per group. ABT-263 was formulated in 10% ethanol, 30% polyethylene glycol 400, and 60% Phosal 50 PG and administered p.o. The other agents used [rituximab, doxorubicin, cyclophosphamide, vincristine, bortezomib, and prednisone] were administered i.p., p.o., or i.v. and formulated according to the manufacturers' recommendations. For combination studies, ABT-263 was given ~2 h before the other agents, except bortezomib, which was given ~4 h before ABT-263 [1].
Synonyms
ABT-263
Molecular Weight
974.61
Formula
C47H55ClF3N5O6S3
CAS No.
923564-51-6
Storage
store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 50 mg/mL (51.3 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
References and Literature
1. Tse C, et al. ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer Res. 2008 May 1;68(9):3421-8. 2. Wang B, et al. The Bcl-2/xL inhibitor ABT-263 increases the stability of Mcl-1 mRNA and protein in hepatocellular carcinoma cells. Mol Cancer. 2014 Apr 30;13:98. 3. Shoemaker AR, et al. Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models. Clin Cancer Res. 2008 Jun 1;14(11):3268-77. 4. Torres P, Anerillas C, Encinas M, et al. The Motor Neuron Disease Mouse Model hSOD1-G93A Presents a Non-canonical Profile of Senescence Biomarkers in The Spinal Cord[J]. 2020
Citations
1. Wang S, Wang Z, Wang X, et al. Humanized cerebral organoids-based ischemic stroke model for discovering of potential anti-stroke agents. Acta Pharmacologica Sinica. 2022: 1-11. 2. Torres P, Anerillas C, Ramírez-Núñez O, et al. The motor neuron disease mouse model hSOD1-G93A shows a non-canonical profile of senescence biomarkers. Disease Models & Mechanisms. 2022 3. Torres P, Anerillas C, Ramírez-Núñez O, et al. A motor neuron disease mouse model reveals a non-canonical profile of senescence biomarkers. Disease models & mechanisms. 2022, 15(8): dmm049059. 4. Bhatt H N, Diwan R, Borrego E A, et al.A photothermal driven chemotherapy for the treatment of metastatic melanoma.Journal of Controlled Release.2023, 361: 314-333. 5. Bhatt H N, Diwan R, Estevao I L, et al.Cadherin-11 targeted cell-specific liposomes enabled skin fibrosis treatment by inducing apoptosis.Journal of Controlled Release.2024, 370: 110-123.
Related compound libraries
This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Inhibitor Library Anti-COVID-19 Compound Library Fluorochemical Library Anti-Aging Compound Library Orally Active Compound Library ReFRAME Related Library
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL),
Method for preparing in vivo formulation:Take μL DMSO master liquid, next add μL PEG300, mix and clarify, next add μL Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL DMSO master liquid, next add μL Corn oil,mix and clarify.
Note:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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