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obatoclax

Product Name: 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
Formula Weight: 317.38
MOL File: 803712-67-6.mol

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obatoclax Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

TRC

Product number: O099000
Product name: Obatoclax
Packaging: 50mg
Price: $100
Updated: 2021/12/16

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obatoclax Chemical Properties,Usage,Production

Uses

Obatoclax is a small molecule mimetic of the BH3 domain of BCL-2 family proteins.

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.

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.

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)

obatoclax Preparation Products And Raw materials

Raw materials

Preparation Products

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803712-67-6, obatoclaxRelated Search:

obatoclax

1H-Indole, 2-[2-[(3,5-diMethyl-1H-pyrrol-2-yl)Methylene]-3-Methoxy-2H-pyrrol-5-yl]-

2-[2-[(3,5-Dimethyl-1H-pyrrol-2-yl)methylene]-3-methoxy-2H-pyrrol-5-yl]-1H-indole

803712-67-6

803712-67-0