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Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

Navitoclax [923564-51-6]

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Referência HY-10087-5mg

Tamanho : 5mg

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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
DMS-79	EC₅₀	0.44 μM Compound: ABT-263	Antiproliferative activity against human DMS 79 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human DMS 79 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
EOL1	EC₅₀	0.011 μM Compound: ABT-263	Antiproliferative activity against human EOL1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human EOL1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
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]
GDM-1	EC₅₀	0.011 μM Compound: ABT-263	Antiproliferative activity against human GDM-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human GDM-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
HEL	EC₅₀	0.07 μM Compound: ABT-263	Antiproliferative activity against human HEL harboring JAK2 V617F mutant assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human HEL harboring JAK2 V617F mutant assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
HL-60	EC₅₀	0.04 μM Compound: ABT-263	Antiproliferative activity against human HL-60 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human HL-60 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
Kasumi 1	EC₅₀	0.03 μM Compound: ABT-263	Antiproliferative activity against human Kasumi 1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human Kasumi 1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
KG-1	EC₅₀	0.11 μM Compound: ABT-263	Antiproliferative activity against human KG-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human KG-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
ML-2	EC₅₀	0.05 μM Compound: ABT-263	Antiproliferative activity against human ML-2 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human ML-2 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
MOLM-13	EC₅₀	0.03 μM Compound: ABT-263	Antiproliferative activity against human MOLM-13 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human MOLM-13 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
MOLM-16	EC₅₀	0.12 μM Compound: ABT-263	Antiproliferative activity against human MOLM16 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human MOLM16 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
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	EC₅₀	112 nM Compound: ABT-263	Antiproliferative activity against Bcl-2 dependent human MOLT-4 cells assessed as reduction in cell viability by measuring effect concentration by CellTiter-Glo reagent based assay Antiproliferative activity against Bcl-2 dependent human MOLT-4 cells assessed as reduction in cell viability by measuring effect concentration by CellTiter-Glo reagent based assay	[PMID: 25787766]
MOLT-4	EC₅₀	303 nM Compound: 21	Antiproliferative activity against human MOLT4 cells in presence of 10% human serum Antiproliferative activity against human MOLT4 cells in presence of 10% human serum	[PMID: 28926247]
MOLT-4	EC₅₀	303 nM Compound: ABT-263	Antiproliferative activity against Bcl-xl dependent human MOLT-4 cells assessed as reduction in cell viability by measuring effect concentration by CellTiter-Glo reagent based assay Antiproliferative activity against Bcl-xl dependent human MOLT-4 cells assessed as reduction in cell viability by measuring effect concentration by CellTiter-Glo reagent based assay	[PMID: 25787766]
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]
MV4-11	EC₅₀	0.04 μM Compound: ABT-263	Antiproliferative activity against human MV4-11 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human MV4-11 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
NCI-H1048	EC₅₀	0.9 μM Compound: ABT-263	Antiproliferative activity against human NCI-H1048 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human NCI-H1048 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
NCI-H1417	EC₅₀	0.1 μM Compound: ABT-263	Antiproliferative activity against human NCI-H1417 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human NCI-H1417 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
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-H1836	EC₅₀	0.26 μM Compound: ABT-263	Antiproliferative activity against human NCI-H1836 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human NCI-H1836 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
NCI-H187	EC₅₀	0.037 μM Compound: ABT-263	Antiproliferative activity against human NCI-H187 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human NCI-H187 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
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-H211	EC₅₀	0.1 μM Compound: ABT-263	Antiproliferative activity against human NCI-H211 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human NCI-H211 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
NCI-H345	EC₅₀	0.3 μM Compound: ABT-263	Antiproliferative activity against human NCI-H345 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human NCI-H345 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
NCI-H446	EC₅₀	0.85 μM Compound: ABT-263	Antiproliferative activity against human NCI-H446 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human NCI-H446 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
NCI-H69	EC₅₀	0.18 μM Compound: ABT-263	Antiproliferative activity against human NCI-H69 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human NCI-H69 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
NCI-H889	EC₅₀	0.053 μM Compound: ABT-263	Antiproliferative activity against human NCI-H889 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human NCI-H889 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
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]
NOMO-1	EC₅₀	>5 μM Compound: ABT-263	Antiproliferative activity against human NOMO-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human NOMO-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
OCI-AML2	EC₅₀	0.011 μM Compound: ABT-263	Antiproliferative activity against human OCI-AML2 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human OCI-AML2 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
OCI-AML-3	EC₅₀	>5 μM Compound: ABT-263	Antiproliferative activity against human OCI-AML-3 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human OCI-AML-3 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
OCI-AML-5	EC₅₀	0.18 μM Compound: ABT-263	Antiproliferative activity against human OCI-AML5 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human OCI-AML5 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
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	EC₅₀	112 nM Compound: 21	Antiproliferative activity against human RS4:11 cells in presence of 10% human serum Antiproliferative activity against human RS4:11 cells in presence of 10% human serum	[PMID: 28926247]
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]
SET-2	EC₅₀	0.06 μM Compound: ABT-263	Antiproliferative activity against human SET2 harboring JAK2 V617F mutant assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human SET2 harboring JAK2 V617F mutant assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
SIG-M5	EC₅₀	0.011 μM Compound: ABT-263	Antiproliferative activity against human SIG-M5 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human SIG-M5 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
SKM-1	EC₅₀	0.24 μM Compound: ABT-263	Antiproliferative activity against human SKM-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human SKM-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
THP-1	EC₅₀	0.45 μM Compound: ABT-263	Antiproliferative activity against human THP-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay Antiproliferative activity against human THP-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay	[PMID: 25787766]
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:

DMSO : 100 mg/mL (102.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation

Purity: 99.97% ee.: 99.92%

Fiche technique (276 KB) SDS (396 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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Referência

Descrição

Cond.

Price Bef. VAT

NB-64-10652-5mg

Navitoclax [923564-51-6]

5mg

NB-64-10652-10mg

Navitoclax [923564-51-6]

10mg

NB-64-10652-1mL

Navitoclax [923564-51-6]

1mLx10mM(inDMSO)

Navitoclax [923564-51-6]

Referência HY-10087-5mg

Contactar o distribuidor local :

Marca : MedChemExpress

Contactar o distribuidor local :

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