| Identification | Back Directory | [Name]
obatoclax | [CAS]
803712-67-6 | [Synonyms]
obatoclax
2-[2-[(3,5-Dimethyl-1H-pyrrol-2-yl)methylene]-3-methoxy-2H-pyrrol-5-yl]-1H-indole
1H-Indole, 2-[2-[(3,5-diMethyl-1H-pyrrol-2-yl)Methylene]-3-Methoxy-2H-pyrrol-5-yl]- | [Molecular Formula]
C20H19N3O | [MDL Number]
MFCD09833233 | [MOL File]
803712-67-6.mol | [Molecular Weight]
317.38 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 63 mg/mL (198.50 mM);Ethanol: Insoluble | [form ]
Solid | [color ]
Light brown to brown | [Water Solubility ]
Water: Insoluble |
| Hazard Information | Back Directory | [Uses]
Obatoclax is a small molecule mimetic of the BH3 domain of BCL-2 family proteins. | [Enzyme inhibitor]
This cell-permeable antiapoptotic agent (FWfree-base = 317.39 g/mol; FWmesylate-salt = 413.49 g/mol; CAS 803712-79-0; Solubility: 83 mg/mL DMSO, also known as GX15-070 and (Z)-2-(5-((3,5-dimethyl-1H-pyrrol-2- yl)methylene)-4-methoxy-5H-pyrrol-2-yl)-1H-indole mesylate, is a pan- Bcl-2 antagonist (Ki = 0.22 μM), binding to the BH3-binding groove of the B-cell lymphoma-2 (i.e., Bcl) family of proteins. Bcl-2 proteins confer a protective effect on malignant cells against death signals of apoptosis, and cancer cells that are resistant to various anti-cancer drugs and treatment regimen are often found to overexpress these Bcl-2, Bcl-XL, Mcl-1, Bcl-w, and A1/Bfl1. Obatoclax inhibits the binding of Bak to Mcl-1, up-regulating Bim, inducing cytochrome c release, and activating capase-3 in human myeloma cell lines. Acting as a single agent, it also induces potent cytotoxic responses against diverse patient-derived neoplasias, including multiple myeloma. Obatoclax retains its efficacy in cells overexpressing the P-glycoprotein multidrug-resistance transporter (P-gp), multidrug resistance-associated protein 2 (MRP2), or breast cancer resistance protein (BCRP) and might also act as a perpetrator drug in interactions with drugs, for example being substrates of CYP1A2 or BCRP. In human pharmacokinetic experiments, Obatoclax has Cmax of 10 to 80 ng/mL, below the level needed for effective in vitro activity against most tumor targets, a finding that is consistent with its failure to reach levels in a mouse xenograft tumor model sufficient to disrupt Mcl-1/Bax protein-protein interaction. | [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].
| 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.
|
| [IC 50]
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) |
|
| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Tel: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.approvedhomemanagement.com/ShowSupplierProductsList15748/0.htm |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
|