obatoclax
- CAS No.
- 803712-67-6
- Chemical Name:
- obatoclax
- 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]-
- CBNumber:
- CB72498826
- Molecular Formula:
- C20H19N3O
- Molecular Weight:
- 317.38
- MDL Number:
- MFCD09833233
- MOL File:
- 803712-67-6.mol
| storage temp. | Store at -20°C |
|---|---|
| solubility | DMSO: 63 mg/mL (198.50 mM);Ethanol: Insoluble |
| Water Solubility | Water: Insoluble |
| FDA UNII | QN4128B52A |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
obatoclax Chemical Properties,Uses,Production
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.
obatoclax Preparation Products And Raw materials
Raw materials
Preparation Products
obatoclax Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131980 | 58 |
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2923 | 55 | |
| Hangzhou Sage Chemical Co., Ltd. | +86057186818502 13588463833 | info@sagechem.com | China | 10269 | 58 |
| Nanjing JinruiJiuAn Biotechnology Co., Ltd. | 025-58196018 800028039 | sales@fartop.net | China | 2231 | 55 |
| NCE Biomedical Co.,Ltd. | 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 | China | 1494 | 55 | |
| LETOPHARM LIMITED | +86-21-5821 5861 | sales@letopharm.com | China | 2384 | 58 |
| SPIRO PHARMA | eric_feng1954@126.com | China | 9254 | 55 |