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Navitoclax [923564-51-6]

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Referência HY-10087-10mg

Tamanho : 10mg

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Description

Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-x_L, Bcl-2 and Bcl-w, with a K_i of less than 1 nM^[1].

IC₅₀ & Target^[1]

Bcl-W

1 nM (Ki)

Bcl-xL

1 nM (Ki)

Bcl-2

1 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
FL5.12	EC₅₀	4.2 nM Compound: 2, ABT-263	Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum	[PMID: 18841882]
FL5.12	EC₅₀	5.9 nM Compound: 2, ABT-263	Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum	[PMID: 18841882]
MOLT-4	EC₅₀	0.3 μM Compound: 1; ABT-263	Cytotoxicity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by celltiter-glo assay Cytotoxicity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by celltiter-glo assay	[PMID: 34141086]
MOLT-4	IC₅₀	212.3 nM Compound: ABT-263	Cytotoxicity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Cytotoxicity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 34533954]
NCI-H1417	IC₅₀	54.2 nM Compound: 2, ABT-263	Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay	[PMID: 23448298]
NCI-H146	EC₅₀	0.08 μM Compound: 2, ABT-263	Cytotoxicity against human NCI-H146 after 48 hrs by MTS assay in presence of 10% human serum Cytotoxicity against human NCI-H146 after 48 hrs by MTS assay in presence of 10% human serum	[PMID: 21366295]
NCI-H146	EC₅₀	86.7 nM Compound: 2, ABT-263	Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum	[PMID: 18841882]
NCI-H187	IC₅₀	38.4 nM Compound: 2, ABT-263	Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay	[PMID: 23448298]
NCI-H1963	EC₅₀	0.051 μM Compound: 2, ABT-263	Cytotoxicity against human NCI-H1963 after 48 hrs by MTS assay in presence of 10% human serum Cytotoxicity against human NCI-H1963 after 48 hrs by MTS assay in presence of 10% human serum	[PMID: 21366295]
NCI-H1963	IC₅₀	26.6 nM Compound: 2, ABT-263	Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay	[PMID: 23448298]
NCI-H889	EC₅₀	0.12 μM Compound: 2, ABT-263	Cytotoxicity against human NCI-H889 after 48 hrs by MTS assay in presence of 10% human serum Cytotoxicity against human NCI-H889 after 48 hrs by MTS assay in presence of 10% human serum	[PMID: 21366295]
Platelet	IC₅₀	0.189 μM Compound: ABT-263	Cytotoxicity against human platelet assessed as cell viability measured after 72 hrs by MTS assay Cytotoxicity against human platelet assessed as cell viability measured after 72 hrs by MTS assay	[PMID: 32388279]
Platelet	IC₅₀	0.325 μM Compound: ABT-263	Cytotoxicity against platelets in human PRP assessed as reduction in cell viability measured after 48 hrs by MTS assay Cytotoxicity against platelets in human PRP assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 34533954]
RS4-11	EC₅₀	0.014 μM Compound: Navitoclax, ABT-263	Induction of apoptosis in human RS4:11 cells overexpressing BCL-2 assessed as caspase 3/7 activation after 6 hrs by quantitative luminescence assay Induction of apoptosis in human RS4:11 cells overexpressing BCL-2 assessed as caspase 3/7 activation after 6 hrs by quantitative luminescence assay	[PMID: 24881567]
RS4-11	EC₅₀	0.11 μM Compound: 1; ABT-263	Cytotoxicity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by celltiter-glo assay Cytotoxicity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by celltiter-glo assay	[PMID: 34141086]
RS4-11	IC₅₀	42.6 nM Compound: ABT-263	Cytotoxicity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Cytotoxicity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 34533954]
WI-38	IC₅₀	8.06 μM Compound: ABT-263	Cytotoxicity against human WI-38 cells assessed as cell viability measured after 72 hrs by MTS assay Cytotoxicity against human WI-38 cells assessed as cell viability measured after 72 hrs by MTS assay	[PMID: 32388279]

In Vitro

Navitoclax (ABT-263) is active against approximately one-half of the cell lines of the PPTP in vitro panel. The median IC₅₀ for all of the lines in the panel is 1.91 μM^[1]. Navitoclax in combination with chemotherapy agents leads most ovarian cancer cell lines a synergistic response, and enhances the caspase activation in both SK-OV-3 and IGROV-1 cell lines^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvant et solubilité

In Vitro:

DMF : ≥ 100 mg/mL (102.61 mM)

DMSO : 75 mg/mL (76.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.0261 mL	5.1303 mL	10.2605 mL
5 mM	0.2052 mL	1.0261 mL	2.0521 mL
10 mM	0.1026 mL	0.5130 mL	1.0261 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% Ethanol 60% Phosal 50 PG 30% PEG400
Solubility: 7.5 mg/mL (7.70 mM); Clear solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (2.13 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (2.13 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (2.13 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation

Purity: 99.97% ee.: 99.92%

Fiche technique (277 KB) SDS (393 KB)

COA (252 KB) HNMR (233 KB) LCMS (122 KB) Elemental Analysis Report (109 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Lock R1, et al. Initial testing (stage 1) of the BH3 mimetic ABT-263 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2008 Jun;50(6):1181-1189. [Content Brief]

[2]. Wong M, et al. Navitoclax (ABT-263) reduces Bcl-x(L)-mediated chemoresistance in ovarian cancer models.Mol Cancer Ther. 2012 Apr;11(4):1026-1035. [Content Brief]

[3]. Chen J, et al. The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo. Mol Cancer Ther. 2011 Dec;10(12):2340-9. [Content Brief]

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Navitoclax [923564-51-6]

Referência HY-10087-10mg

Contactar o distribuidor local :

Marca : MedChemExpress

Contactar o distribuidor local :

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