Art. -Nr.: HY-10969A

Obatoclax

Name: Obatoclax
Brand: MedChemExpress
SKU: HY-10969A
Price: 130.00 USD
Availability: InStock
Rating: 5 (12 reviews)

(Synonyms: GX15-070)

12 Cited Publications

Kundenbewertung

Based on 12 publication(s) in Google Scholar

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

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Reinheit : 98.04%
CAS. Nr.: 803712-67-6
Formel: C₂₀H₁₉N₃O
Molecular Weight:317.38

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Obatoclax Chemical Structure

CAS. Nr.: 803712-67-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

^[1]^[2]

BCL2

200 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)

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

Alle Parasite Isoform-spezifische Produkte anzeigen :

In Vitro

Obatoclax (GX15-070) inhibits BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b with Ki values≈1-7 μM^[2].
Obatoclax (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 (400 nM; for 24 hours) induces autophagy in OSCC cells^[3].
Obatoclax (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations^[1].
Obatoclax (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM^[1].
Obatoclax 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 (200 nM; 1, 3, 6, 12, 24 hours). Obatoclax inhibits GSK3β but activates p38 MAPK, while barely affecting ERK1/2 activity in HT-29 cells^[1].
Obatoclax (50, 100, 150, 200, 250, 300, 350, 400, 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.

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:

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 (GX15-070; 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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 803712-67-6
Appearance Solid
Molecular Weight 317.38
Formel C₂₀H₁₉N₃O
Color Light brown to brown
SMILES

COC1=CC(C(N2)=CC3=C2C=CC=C3)=N/C1=C\C4=C(C)C=C(C)N4
Synonyms

GX15-070
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (12)

All In Vivo Efficacy StudyOthersCell Proliferation/Viability AssayIFWB

Sort by:

Journal Impact Factor

Cancer Lett

High-content drug screening in zebrafish xenografts reveals high efficacy of dual MCL-1/BCL-XL inhibition against Ewing sarcoma. [Abstract]

2023 Feb 1:554:216028. PMID: 36462556
Acta Pharmacol Sin

Combinations of proteasome inhibitors with obatoclax are effective for small cell lung cancer. [Abstract]

2021 Aug;42(8):1298-1310. PMID: 33139838
Drug Deliv Transl Res

Leveraging quantum chemical properties in transfer learning for predicting blood-brain barrier permeability of drugs. [Abstract]

2025 Oct 29. PMID: 41160380
Sci Rep

Drivers of AR indifferent anti-androgen resistance in prostate cancer cells. [Abstract]

2019 Sep 24;9(1):13786. PMID: 31551480

Obatoclax purchased from MedChemExpress. Usage Cited in: Sci Rep. 2019 Sep 24;9(1):13786. [Abstract]

Dose response curves showing the proliferation at increasing concentrations of the PARP inhibitor olaparib and the pan-BCL-2 inhibitor Obatoclax Mesylate in normal growth medium (containing 10 µM enzalutamide for ResA/ResB).
ACS Infect Dis

Bcl-2 Antagonist Obatoclax Reactivates Latent HIV-1 via the NF-κB Pathway and Induces Latent Reservoir Cell Apoptosis in Latently Infected Cells. [Abstract]

2023 Nov 10;9(11):2105-2118. PMID: 37796279
iScience

Identification of potent inhibitors of SARS-CoV-2 infection by combined pharmacological evaluation and cellular network prioritization. [Abstract]

2022 Sep 16;25(9):104925. PMID: 35992305

Obatoclax purchased from MedChemExpress. Usage Cited in: iScience. 2022 Sep 16;25(9):104925. [Abstract]

Male and female mice were infected with SARS-CoV-2 virus intranasally, and infection began 6 hours after daily treatment with 3 mg/kg Obatoclax Mesylate. Viral load in the lungs (FFU/g tissue) was measured 4 days post-infection.
Viruses

Identification and Tracking of Antiviral Drug Combinations. [Abstract]

2020 Oct 18;12(10):1178. PMID: 33080984

Obatoclax purchased from MedChemExpress. Usage Cited in: Viruses. 2020 Oct 18;12(10):1178. [Abstract]

The effects of 5 µM vemurafenib plus 0.1% DMSO, 0.2 µM emetine, 0.2 µM homoharringtonine, 0.2 µM Obatoclax Mesylate, 1 µL Gemcitabine, 0.1 µL Anisomycin and 1 µL Cycloheximide on viral replication measured by plaque reduction assay.
Am J Cancer Res

Targeting sphingosine kinase 2 suppresses cell growth and synergizes with BCL2/BCL-XL inhibitors through NOXA-mediated MCL1 degradation in cholangiocarcinoma. [Abstract]

2019 Mar 1;9(3):546-561. PMID: 30949409

Obatoclax purchased from MedChemExpress. Usage Cited in: Am J Cancer Res. 2019 Mar 1;9(3):546-561. [Abstract]

RBE, HCCC9810, and HuH28 cells were treated with different concentrations of ABC294640 or Obatoclax Mesylate, alone or in combination, for 72 hours, and then cell viability was analyzed using the CCK-8 assay.
bioRxiv

2024 Jul 25.
Norwegian University of Science and Technology

2021 Oct.
Biomed Pharmacother

Biomimetic nanoparticle loading obatoclax mesylate for the treatment of non-small-cell lung cancer (NSCLC) through suppressing Bcl-2 signaling. [Abstract]

2020 Sep:129:110371. PMID: 32563984

Obatoclax purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Sep:129:110371. [Abstract]

Immunofluorescence staining displays weaker Bcl-2 fluorescence intensity in lung cancer cells incubated with RBCm-Obatoclax Mesylate (OM)/PLGA, accompanied with stronger expression of pro-apoptotic signal Bax in comparison to the Con group.

Obatoclax purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Sep:129:110371. [Abstract]

Bcl-2 and Bcl-xl protein expression levels are restrained in A549 and H1975 cells treated with RBCm-OM/PLGA; however, Bax, cleaved Caspase-3, Caspase-9 and PARP are up-regulated following RBCm-OM/PLGA incubation. Also, free Obatoclax Mesylate (OM) does not influence the expression change of all these proteins.
Universitat Politècnica de València

2020 Sep 7.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (315.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1508 mL

15.7540 mL

31.5080 mL

5 mM

0.6302 mL

3.1508 mL

6.3016 mL

10 mM

0.3151 mL

1.5754 mL

3.1508 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (7.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Or CR, et al. Obatoclax, a Pan-BCL-2 Inhibitor, Targets Cyclin D1 for Degradation to Induce Antiproliferation in Human Colorectal Carcinoma Cells. Int J Mol Sci. 2016 Dec 27;18(1). [Content Brief]

[2]. Nguyen M, et al. Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19512-7. Epub 2007 Nov 26. [Content Brief]

[3]. Sulkshane P, et al. BH3 mimetic Obatoclax (GX15-070) mediates mitochondrial stress predominantly via MCL-1 inhibition and induces autophagy-dependent necroptosis in human oral cancer cells. Oncotarget. 2016 Aug 5;8(36):60060-60079. [Content Brief]

[4]. Ehrenkaufer G, et al. Identification of anisomycin, prodigiosin and obatoclax as compounds with broad-spectrum anti-parasitic activity. PLoS Negl Trop Dis. 2020 Mar 20;14(3):e0008150. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.1508 mL	15.7540 mL	31.5080 mL	78.7699 mL
	5 mM	0.6302 mL	3.1508 mL	6.3016 mL	15.7540 mL
	10 mM	0.3151 mL	1.5754 mL	3.1508 mL	7.8770 mL
	15 mM	0.2101 mL	1.0503 mL	2.1005 mL	5.2513 mL
	20 mM	0.1575 mL	0.7877 mL	1.5754 mL	3.9385 mL
	25 mM	0.1260 mL	0.6302 mL	1.2603 mL	3.1508 mL
	30 mM	0.1050 mL	0.5251 mL	1.0503 mL	2.6257 mL
	40 mM	0.0788 mL	0.3938 mL	0.7877 mL	1.9692 mL
	50 mM	0.0630 mL	0.3151 mL	0.6302 mL	1.5754 mL
	60 mM	0.0525 mL	0.2626 mL	0.5251 mL	1.3128 mL
	80 mM	0.0394 mL	0.1969 mL	0.3938 mL	0.9846 mL
	100 mM	0.0315 mL	0.1575 mL	0.3151 mL	0.7877 mL

Bioz

Keywords

Obatoclax

12 Cited Publications

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Obatoclax

Publications Citing Use of MedChemExpress (MCE) Obatoclax

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