Navitoclax (Synonyms: ABT-263)

Name: Navitoclax
Brand: MedChemExpress
SKU: HY-10087
Rating: 5.0 (89 reviews)

Cat. No.: HY-10087 Purity: 99.72%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Navitoclax Chemical Structure

CAS No. : 923564-51-6

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10 mM * 1 mL in DMSO ready for reconstitution	USD 75	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 75	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
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Based on 89 publication(s) in Google Scholar

Other Forms of Navitoclax:

Navitoclax-d₈ Get quote
Navitoclax dihydrochloride Get quote

87 Publications Citing Use of MCE Navitoclax

Proliferation Assay

: Navitoclax purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Sep 24;9(10):986. [Abstract]; Cells are treated with 25 nM siRNA for 48 hours followed by 1 μM ABT-263 for 36 hours.

: Navitoclax purchased from MedChemExpress. Usage Cited in: ACS Med Chem Lett. 2015 Jun 22;6(8):948-52. [Abstract]; Combination treatment. (a) Comparison of AZD-8055 and ABT-263 treatment in all cell lines. Red indicates sensitivity, while blue indicates resistance. (b) Depiction of synergism where the values shown are excess over Bliss Independence, a prediction of inhibition without synergism. Increased synergism is evident by an increased number, shown in red, while negative numbers in blue represent an antagonistic effect.

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

In Vivo

Navitoclax (100 mg/kg; orally; 21-day treatment) enhances the activity of OSI-744 in vivo. As a single agent, 100 mg/kg Navitoclax alone dosed daily has no significant antitumor activity, whereas daily dosing of OSI-744 at 50 mg/kg results in significant tumor stasis (%TGI=52) during a 21-day treatment period. Notably, the combination of Navitoclax and OSI-744 dosed daily for 21 consecutive days results in 98% TGI and durable tumor regressions in 100% of treated tumor-bearing mice^[3].

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

Animal Model:	Mice with NCI-H1650 model^[3]
Dosage:	100 mg/kg
Administration:	Orally; daily; for 21 consecutive days
Result:	As a single agent, 100 mg/kg alone dosed daily had no significant antitumor activity. Notably, the combination with OSI-744 resulted in 98% TGI and durable tumor regressions in 100% of treated tumor-bearing mice.

Clinical Trial

Molecular Weight

974.61

Formula

C₄₇H₅₅ClF₃N₅O₆S₃

CAS No.

923564-51-6

Appearance

Solid

Color

White to light yellow

SMILES

O=S(C1=CC(S(NC(C2=CC=C(N3CCN(CC4=C(CCC(C)(C4)C)C5=CC=C(Cl)C=C5)CC3)C=C2)=O)(=O)=O)=CC=C1N[C@H](CCN6CCOCC6)CSC7=CC=CC=C7)(C(F)(F)F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.97% ee.: 99.92%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

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

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / DMF	1 mM	1.0261 mL	5.1303 mL	10.2605 mL	25.6513 mL
	5 mM	0.2052 mL	1.0261 mL	2.0521 mL	5.1303 mL
	10 mM	0.1026 mL	0.5130 mL	1.0261 mL	2.5651 mL
	15 mM	0.0684 mL	0.3420 mL	0.6840 mL	1.7101 mL
	20 mM	0.0513 mL	0.2565 mL	0.5130 mL	1.2826 mL
	25 mM	0.0410 mL	0.2052 mL	0.4104 mL	1.0261 mL
	30 mM	0.0342 mL	0.1710 mL	0.3420 mL	0.8550 mL
	40 mM	0.0257 mL	0.1283 mL	0.2565 mL	0.6413 mL
	50 mM	0.0205 mL	0.1026 mL	0.2052 mL	0.5130 mL
	60 mM	0.0171 mL	0.0855 mL	0.1710 mL	0.4275 mL
DMF	80 mM	0.0128 mL	0.0641 mL	0.1283 mL	0.3206 mL
DMF	100 mM	0.0103 mL	0.0513 mL	0.1026 mL	0.2565 mL

Navitoclax Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Navitoclax923564-51-6ABT-263ABT263ABT 263Bcl-2 FamilyInhibitorinhibitorinhibit

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Navitoclax (Synonyms: ABT-263)

Customer Review

Other Forms of Navitoclax:

Navitoclax Related Antibodies

87 Publications Citing Use of MCE Navitoclax

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View All Bcl-2 Family Isoform Specific Products:

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References

Customer Review

Navitoclax Related Antibodies

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Complete Stock Solution Preparation Table

Navitoclax Related Classifications

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