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Navitoclax (ABT-263)

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InvivoChem Cat #: V0003

CAS #: 923564-51-6Purity ≥98%

Description: Navitoclax (formerly ABT-263) is a novel, highly potent, orally bioavailable small-molecule inhibitor of the BCL (B-cell leukemia) protein family such as Bcl-xL, Bcl-2 and Bcl-w with Ki of ~ 0.5 nM, ~1 nM and ~1 nM in cell-free assays. It has potential anticancer activity and is currently undergoing Phase studies for the treatment of both solid and liquid tumors. ABT-263 mimicks the Bad-like BH3 and binds to Bcl-2 family proteins Bcl-2, Bcl-xl and Bcl-w which disrupts the interaction between Bcl-2/Bcl-xl /Bcl-w and pro-apoptotic proteins such as Bim(Bcl-2-interacting mediator of cell death), Bad (Bcl-2-associated death promoter) and Bak(BCL2-antagonist/killer 1), eventually it will trigger the caspases-initiated cell death pathway to induce apoptosis.

References: Cancer Res. 2008, 68(9), 3421-428.; Clin Cancer Res, 2008, 14(11), 3268-77.

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Molecular Weight (MW)	974.61
Formula	C47H55ClF3N5O6S3
CAS No.	923564-51-6
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 100 mg/mL (102.6 mM)
	Water: <1 mg/mL (slightly soluble or insoluble)
	Ethanol: <1 mg/mL
Solubility (In vivo)	55% DMSO+Corn oil: 8mg/mL
Synonyms	Navitoclax; ABT 263; ABT-263; ABT263
SMILES Code	O=C(NS(=O)(C1=CC=C(N[[email protected]](CCN2CCOCC2)CSC3=CC=CC=C3)C(S(=O)(C(F)(F)F)=O)=C1)=O)C4=CC=C(N5CCN(CC6=C(C7=CC=C(Cl)C=C7)CCC(C)(C)C6)CC5)C=C4

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General	When ABT-263 is administered at 100 mg/kg/day in the H345 xenograft model, significant antitumor efficacy is observed with 80% TGI and 20% of treated tumors indicating at least a 50% reduction in tumor volume.
Animal model	C.B -17 scid-bg or C.B -17 scid mice
Formulation	Formulated in 10% ethanol, 30% polyethylene glycol 400, and 60% Phosal 50 PG
Dosages	100 mg/kg/day
Administration	Oral gavage
Reference	Cancer Res. 2008, 68(9), 3421-428.; Clin Cancer Res, 2008, 14(11), 3268-77.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Lot#: V000301,Purity ≥98%
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Lot#: V000302,Purity ≥98%
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ABT-737, or ABT-263 at the indicated doses for 24 hours. Survival data are shown for transitional B cells (n = 3 mice for each genotype) and are the results of 3 independent experiments, each performed in triplicate. Experiments depicted in panels C and D were performed concurrently. Values represent mean ± SEM.		As an inhibitor of Bcl-2, ABT263 is effective to reduce cell viability in HG3-CLL cells. Incubating the cells with ABT263 in 96 well plates (3×104 cells per well) for 24h shows a dose-dependent inhibition of cell viability with EC50 value of 2μM.

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