ABT-263

SKU: orb1306480

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Description

Navitoclax (ABT-263) is an orally bioavailable small molecule that potently inhibits Bcl-2, Bcl-xL, and Bcl-w (Ki<1 nM), inducing apoptosis. It is widely used in cancer research, demonstrating antitumor activity in both in vitro cellular assays and in vivo xenograft models for studying programmed cell death mechanisms.

Research Area

Cell Biology, Neuroscience, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	923564-51-6
MW	974.6
Purity	>98%
Formula	C₄₇H₅₅ClF₃N₅O₆S₃
SMILES	C(C1=C(CCC(C)(C)C1)C2=CC=C(Cl)C=C2)N3CCN(CC3)C4=CC=C(C(NS(=O)(=O)C5=CC(S(C(F)(F)F)(=O)=O)=C(N[C@H](CCN6CCOCC6)CSC7=CC=CC=C7)C=C5)=O)C=C4
Target	Bcl-2
Solubility	Soluble in DMSO (up to 25 mg/ml)

Bioactivity

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Target IC50	BCL-W:< 1 nM (Ki, cell free)\|Bcl-2:< 1 nM (Ki, cell free)\|BCL-XL:0.4 nM (Ki, cell free)
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. 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. Read more...
In Vitro	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. 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. Read more...
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 . Read more...
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 . Read more...

Storage & Handling

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

Alternative Names

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Navitoclax

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Compound Identifiers

PubChem CID

24978538 ↗

Key Properties

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No computed properties available.

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CAS Number:	1217620-38-6
MW:	982.66
Formula:	C₄₇H₅₅ClF₃N₅O₆S₃

Purity:	99.87% (May vary between batches)
CAS Number:	2365172-82-1
MW:	918.55
Formula:	C₄₄H₅₁ClF₃N₅O₅S₃

Purity:	99.82% (May vary between batches)
CAS Number:	2143096-93-7
MW:	973.63
Formula:	C₄₇H₅₆ClF₃N₆O₅S₃

Purity:	>98% (HPLC)
CAS Number:	923564-51-6
MW:	974.6127
Formula:	C₄₇H₅₅ClF₃N₅O₆S₃

ABT-263

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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