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> Obatoclax (Mesylate) [803712-79-0]

Obatoclax (Mesylate) [803712-79-0]

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Cat# HY-10969-5mg

Size : 5mg

Brand : MedChemExpress

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Description

Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2[1][2]. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity[3][4].

IC50 & Target[5]

Bcl-2

220 nM (Ki)

Mcl-1

1-7 μM (Ki)

Bcl-xL

1-7 μM (Ki)

Bcl-W

1-7 μM (Ki)

Bcl-B

1-7 μM (Ki)

In Vitro

Obatoclax Mesylate (GX15-070 Mesylate) inhibits BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b with Ki values≈1-7 μM[2].
Obatoclax Mesylate (50-200 nM; 24-72 hours) induces a dose- and time-dependent reduction of cell numbers in all human colorectal cancer cell lines. In particular, the IC50 of cell proliferation at 72 h are 25.85, 40.69, and 40.01 nM for HCT116, HT-29, and LoVo cells, respectively[1].
Obatoclax Mesylate (400 nM; for 24 hours) induces autophagy in OSCC cells[3].
Obatoclax Mesylate (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations[1].
Obatoclax Mesylate (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM[1].
Obatoclax Mesylate induces T286 phosphorylation-dependent or -independent cyclin D1 degradation. in HCT116 and LoVo cells, the steady-state levels of p-Cyclin D (T286) began to decline once exposed to obatoclax Mesylate (200 nM; 1, 3, 6, 12, 24 hours). Obatoclax Mesylate inhibits GSK3β but activates p38MAPK, while barely affecting ERK1/2 activity in HT-29 cells[1].
Obatoclax Mesylate (50-450 nM) potently inhibits the clonogenic potential of oral cancer cells[1].

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

Obatoclax Mesylate Related Antibodies

Cell Proliferation Assay[1]

Cell Line: human colorectal cancer HCT116, HT-29 and LoVo cells
Concentration: 50, 100, 200 nM
Incubation Time: 24, 48, and 72 hours
Result: Induced a dose- and time-dependent reduction of cell numbers.

Cell Autophagy Assay[3]

Cell Line: AW8507 and SCC029B cells
Concentration: 400 nM
Incubation Time: 24 hours
Result: Induced autophagy in OSCC cells.

Cell Cycle Analysis[1]

Cell Line: HCT116 and HT-29 cells
Concentration: 50, 100, 200 nM
Incubation Time: 24 hours
Result: Provoked a dose-dependent increase in the G1-phase cell populations.

Western Blot Analysis[1]

Cell Line: HCT116, HT-29 and LoVo cells
Concentration: 25, 50, 100, 200 nM
Incubation Time: 24 hours
Result: Indicated a marked drop in cyclin D1 levels as low as 50 nM.
In Vivo

Obatoclax Mesylate (GX15-070 Mesylate; 1.15-5 mg/kg; intravenously injected; five consecutive days) exhibits potent antitumor activity in xenograft mouse models in a dose-dependent manner[4].

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

Animal Model: 6-8 weeks old female BALB/C nude mice bearing subcutaneous tumors[4]
Dosage: 1.15, 2.5, 5 mg/kg
Administration: Intravenously injected (through lateral tail vein); five consecutive days (i.e. 5 injections)
Result: Exhibited potent antitumor activity in xenograft mouse models in a dose-dependent manner.
Clinical Trial
Molecular Weight

413.49

Formula

C21H23N3O4S
CAS No.
Appearance

Solid

Color

Purple to black

SMILES

COC1=CC(C2=CC3=C(C=CC=C3)N2)=N/C1=C\C4=C(C=C(N4)C)C.CS(=O)(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (30.23 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 2.4184 mL 12.0922 mL 24.1844 mL
5 mM 0.4837 mL 2.4184 mL 4.8369 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.83 mg/mL (2.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.83 mg/mL (2.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.
Purity & Documentation
References

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