| Size | Price | Stock | Qty |
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| 25mg |
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| 500mg |
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| 1g |
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Obatoclax (also known as GX-15070; GX15 070) is a potent pan-BCL-2 family proteins inhibitor with a Ki of 0.22 μM in a cell-free assay. Obatoclax binds to the BH3-binding site of BCL-2 and other related BCL-2 family members (including BCL-XL, MCL-1, A1, and BCL-B). As a pan-BCL-2 inhibitor, it is being investigated for the treatment of refractory malignancies, obatoclax mesylate directly induce apoptosis in cultured acute myeloid leukemia (AML) cells as well as primary patient samples and exhibits antitumor activity in mouse xengografts of solid tumor and myeloma cell lines. The Bcl-2 family of proteins are overexpressed in various cancers such as the lymphatic system, breast, lung, prostate, and colon. Therefore, Obatoclax has anticancer activity as an Bcl-2 inhibitor.
| ln Vitro |
Obatoclax (GX15-070) has a Ki value of around 1-7 μM and inhibits BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b [2]. In all human colorectal cancer cell lines, obatoclax (50-200 nM; 24-72 hours) causes dose- and time-dependent decreases in cell number. Specifically, at 72 hours, the IC50 values for cell proliferation of HCT116, HT-29, and LoVo cells were 25.85, 40.69, and 40.01 nM, respectively [1]. For a duration of 24 hours, obatoclax (400 nM) stimulates autophagy in OSCC cells [3]. The dose-dependent rise in the G1 cell population is brought about by obatoclax (50-200 nM) for a 24-hour period [1]. Cyclin D1 levels are significantly reduced by obatoclax (25-200 nM; for 24 hours); the lowest level observed was 50 nM [1]. Obatoclax causes cyclin D1 degradation that is either -independent or -dependent on T286 phosphorylation. After being exposed to obatoclax (200 nM; 1, 3, 6, 12, 24 hours), steady-state levels of p-Cyclin D (T286) in HCT116 and LoVo cells started to decline. In HT-29 cells, obatoclax hardly affects ERK1/2 activity but inhibits GSK3β and activates p38 MAPK [1]. The clonogenic potential of oral cancer cells is successfully inhibited by obatoclax (50, 100, 150, 200, 250, 300, 350, 400, 450 nM) [1].
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| ln Vivo |
In a xenograft mouse model, obatoclax (GX15-070; 1.15–5 mg/kg; intravenous injection; five consecutive days) exhibited strong anticancer efficacy in a dose-dependent manner [4].
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| Cell Assay |
Cell proliferation assay[1]
Cell Types: Human colorectal cancer HCT116, HT-29 and LoVo Cell Tested Concentrations: 50, 100, 200 nM Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Induced dose- and time-dependent reduction in cell proliferation Number of cells. Autophagy assay [3] Cell Types: AW8507 and SCC029B Cell Tested Concentrations: 400 nM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of autophagy in OSCC cells. Cell cycle analysis[1] Cell Types: HCT116 and HT-29 Cell Tested Concentrations: 50, 100, 200 nM Incubation Duration: 24 hrs (hours) Experimental Results: Caused a dose-dependent increase in the G1 phase cell population. Western Blot Analysis[1] Cell Types: HCT116, HT-29 and LoVo Cell Tested Concentrations: 50, 100, 200 nM Incubation Duration: 24 hrs (hours) Experimental Results: Demonstrated significant decrease in cyclin D1 levels, as low as 50 nM. |
| Animal Protocol |
Animal/Disease Models: 6-8 weeks old female subcutaneoustumor BALB/C nude mice [4]
Doses: 1.15, 2.5, 5 mg/kg Route of Administration: intravenous (iv) (iv)injection (through tail vein); five days (i.e. 5 injections ) Experimental Results: Demonstrated potent antitumor activity in a dose-dependent manner in xenograft mouse models. |
| References |
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| Additional Infomation |
Obatoclax has been used in trials studying the treatment of AML, Leukemia, Myelofibrosis, Hodgkin's Lymphoma, and Mantle-Cell Lymphoma, among others.
Obatoclax is a small molecule and a pan-inhibitor of Bcl-2 family proteins, with pro-apoptotic activity. GX015-070 is a selective antagonist of the BH3-binding groove of the Bcl-2 family proteins, which are frequently overexpressed in cancers including chronic lymphocytic leukemia (CLL). This agent induces/restores apoptosis in cancer cells by inhibiting apoptosis suppressors in multiple members of the Bcl-2 family simultaneously. Mechanism of Action Obatoclax binds anti-apoptotic Bcl-2 proteins and interferes with their ability to interact with pro-apoptotic proteins. |
| Molecular Formula |
C20H19N3O
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|---|---|
| Molecular Weight |
317.384364366531
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| Exact Mass |
317.152
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| CAS # |
803712-67-6
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| Related CAS # |
Obatoclax Mesylate;803712-79-0
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| PubChem CID |
11404337
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| Appearance |
Light brown to brown solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
570.5±50.0 °C at 760 mmHg
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| Flash Point |
298.8±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.652
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| LogP |
3.89
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
777
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=C(N1)/C=C\2/C(=C/C(=C/3\C=C4C=CC=CC4=N3)/N2)OC)C
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| InChi Key |
RFTSSZJZXOSICM-GRSHGNNSSA-N
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| InChi Code |
InChI=1S/C20H19N3O/c1-12-8-13(2)21-16(12)10-19-20(24-3)11-18(23-19)17-9-14-6-4-5-7-15(14)22-17/h4-11,21-22H,1-3H3/b19-10-
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| Chemical Name |
1H-indole, 2-(2-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)-3-methoxy-2H-pyrrol-5-yl)-
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| Synonyms |
GX15-070 GX-05-070GX 15-070ObatoclaxGX05-070 GX 05-070 GX-15-070
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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