Navitoclax (ABT-263) | CAS:923564-51-6

Navitoclax (ABT-263)

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Description:

Navitoclax (ABT-263) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1.

Targets:

Bcl-xL/Bcl-2/Bcl-w

In vitro:

Clin Cancer Res, 2008 Jun 1;14(11):3268-77.

Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models.[Pubmed: 18519752]

The purpose of this study was to characterize the activity of the Bcl-2 protein family inhibitor ABT-263 in a panel of small cell lung cancer (SCLC) xenograft models.
METHODS AND RESULTS:
A panel of 11 SCLC xenograft models was established to evaluate the efficacy of ABT-263. Single agent activity was examined on a continuous dosing schedule in each of these models. The H146 model was used to further evaluate dose and schedule, comparison to standard cytotoxic agents, and induction of apoptosis. ABT-263 exhibited a range of antitumor activity, leading to complete tumor regression in several models. Significant regressions of tumors as large as 1 cc were also observed. The efficacy of ABT-263 was also quite durable; in several cases, minimal tumor regrowth was noted several weeks after the cessation of treatment. Antitumor effects were equal or superior to that of several clinically approved cytotoxic agents. Regression of large established tumors was observed through several cycles of therapy and efficacy was retained in a Pgp-1 overexpressing line. Significant efficacy was observed on several dose and therapeutic schedules and was associated with significant induction of apoptosis.
CONCLUSIONS:
ABT-263 is a potent, orally bioavailable inhibitor of Bcl-2 family proteins that has recently entered clinical trials. The efficacy data reported here suggest that SCLC is a promising area of clinical investigation with this agent.

Navitoclax (ABT-263) Description

Source:
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage:	Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C). Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
After receiving:	The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.

Cell Research:

Cancer Res,2008 May 1;68(9):3421-8.

ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor.[Pubmed: 18451170]

Cell lines:SCLC cell lines
Concentrations: 0-1 μM
Incubation Time: 48 hours
Method:
Human tumor cell lines SCLC cell lines are maintained at 37℃ containing 5% CO2. SCLC cell lines are cultured in RPMI 1640 with 10% fetal bovine serum (FBS), 1% sodium pyruvate, 25 mM HEPES, 4.5 g/L glucose, and 1% penicillin/streptomycin. Leukemia and lymphoma cell lines are cultured in RPMI 1640 supplemented with 10% FBS and 1% penicillin/streptomycin. Cells (1-5×10 4) are treated by ABT-263 for 48 hours in 96-well culture plates in a final volume of 100 μL and cytotoxicity is assessed with the CellTiter Glo assay. In vitro cyto toxicity of ABT-263 is assayed.

Animal Research:

Cancer Res, 2008 May 1;68(9):3421-8.

ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor.[Pubmed: 18451170]

Animal Models: C.B.-17 scid-bg or C.B.-17 scid mice
Dosages:100 mg/kg/d
Administration: Administered via p.o.

Product Name	Navitoclax (ABT-263)
Price:
CAS No.:	923564-51-6
Catalog No.:	CFN60060
Molecular Formula:	C₄₇H₅₅ClF₃N₅O₆S₃
Molecular Weight:	974.61 g/mol
Purity:	>=98%
Type of Compound:	Alkaloids
Physical Desc.:	Powder
Source:
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download:	COA MSDS
Similar structural:	Comparison
Guestbook:

Size /Price /Stock	10 mM * 100 uL in DMSO / Inquiry / In-stock 10 mM * 1 mL in DMSO / Inquiry / In-stock
Related Libraries	Alkaloids Compound Library

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	1.0261 mL	5.1303 mL	10.2605 mL	20.521 mL	25.6513 mL
5 mM	0.2052 mL	1.0261 mL	2.0521 mL	4.1042 mL	5.1303 mL
10 mM	0.1026 mL	0.513 mL	1.0261 mL	2.0521 mL	2.5651 mL
50 mM	0.0205 mL	0.1026 mL	0.2052 mL	0.4104 mL	0.513 mL
100 mM	0.0103 mL	0.0513 mL	0.1026 mL	0.2052 mL	0.2565 mL

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