Home Tools
Log in
Cart

Obatoclax

Catalog No. T41278   CAS 803712-67-6

Obatoclax (GX15-070), a pan-BCL-2 family proteins inhibitor and BH3 mimetic, exhibits a binding affinity (K_i) of 220 nM for BCL-2. It promotes autophagy-dependent cell death and cyclin D1 degradation via the proteasome. Additionally, Obatoclax demonstrates anti-cancer properties and broad-spectrum antiparasitic activity.

All TargetMol products are for research or drug registration purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose in violation of laws and regulations.
Obatoclax Chemical Structure
Obatoclax, CAS 803712-67-6
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,520.00
50 mg 6-8 weeks $ 1,980.00
100 mg 6-8 weeks $ 2,500.00
Bulk Inquiry
Get quote
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description Obatoclax (GX15-070), a pan-BCL-2 family proteins inhibitor and BH3 mimetic, exhibits a binding affinity (K_i) of 220 nM for BCL-2. It promotes autophagy-dependent cell death and cyclin D1 degradation via the proteasome. Additionally, Obatoclax demonstrates anti-cancer properties and broad-spectrum antiparasitic activity.
In vitro Obatoclax (GX15-070) inhibits several BCL-2 family proteins, with Ki values around 1-7 μM, demonstrating its potency in apoptosis regulation. In colorectal cancer cell lines (HCT116, HT-29, LoVo), it significantly reduces cell numbers in a dose- and time-specific manner, with the IC50 for cell proliferation at 72 hours being 25.85, 40.69, and 40.01 nM, respectively. At 400 nM for 24 hours, Obatoclax induces autophagy in OSCC cells and provokes an increase in G1-phase cell populations at doses of 50-200 nM for 24 hours. Similarly, it decreases cyclin D1 levels significantly at these concentrations. It leads to both phosphorylation-dependent and -independent cyclin D1 degradation in HCT116 and LoVo cells, with a notable decline in p-Cyclin D (T286) levels after treatment. Furthermore, Obatoclax inhibits GSK3β, activates p38 MAPK without significantly affecting ERK1/2 activity in HT-29 cells, and effectively inhibits the clonogenic potential of oral cancer cells across a range of concentrations (50-450 nM), underscoring its broader impact on cancer cell survival and proliferation mechanisms.
In vivo Obatoclax (GX15-070; administered at doses of 1.15-5 mg/kg intravenously through the lateral tail vein for five consecutive days) demonstrated significant antitumor efficacy in xenograft mouse models in a dose-dependent manner. This study utilized 6-8 week old female BALB/C nude mice with subcutaneous tumors, and the results indicate that increasing doses of Obatoclax correspond to greater antitumor activity.
Molecular Weight 317.38
Formula C20H19N3O
CAS No. 803712-67-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolCitations

1. Zhou X, Qian Y, Ling C, et al.An integrated framework for prognosis prediction and drug response modeling in colorectal liver metastasis drug discovery.Journal of Translational Medicine.2024, 22(1): 321.

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Obatoclax 803712-67-6 inhibitor inhibit

 

TargetMol