OBLIMERSEN SODIUM

OBLIMERSEN SODIUM structure

CAS No.: 190977-41-4

Chemical Name:: OBLIMERSEN SODIUM

Synonyms: Genasense;Augmerosen;Unii-sh55B0rq9k;OBLIMERSEN SODIUM;Dna, D(p-thio)(T-C-T-C-C-C-A-G-C-G-T-G-C-G-C-C-A-T)

CBNumber:: CB5987160

Molecular Formula:: C172H204N62Na17O91P17S17

Molecular Weight:: 6058.305987

MDL Number:: MFCD07772392

MOL File:: 190977-41-4.mol

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OBLIMERSEN SODIUM Properties

EWG's Food Scores	1
NCI Dictionary of Cancer Terms	augmerosen; Genasense; oblimersen sodium
FDA UNII	SH55B0RQ9K
NCI Drug Dictionary	Genasense

OBLIMERSEN SODIUM Chemical Properties,Uses,Production

Description

As the representative antisense oligonucleotide, Oblimersen (G3139, Genasense) is an 18-base phosphor- othioate antisense oligodeoxynucleotide that was developed to treat CLL, B-cell lymphoma, lung, and breast cancers. Oblimersen binds with the first six codons of Bcl-2 mRNA open reading frame and mediates RNA cleavage by RNase H to downregulate Bcl-2. The antitumor effect of oblimersen is associated with both apoptotic and nonapoptotic pathways.
In the apoptotic pathway, Bcl-2 downregulation by oblimersen could increase Bax and poly (ADP-ribose) Polymerase (PARP) to release cytochrome cand Smac/DIABLO to pro- mote apoptosis. For the nonapoptotic pathway, Bcl-2 downregulation by oblimersen may have promoted the release of Beclin-1 to induce autophagic cell death. In addition, oblimersen has been shown to enhance tumor immunity by promoting polyclonal antibodies production and activating dendritic cell maturation. In monotherapy, oblimersen failed in phase-III clinical trials of treating lymphoid malignancies, which could be due to limited uptake, intracellular compartmentalization, or degradation by nuclear enzymes. On the other hand, oblimersen has been found to increase the overall survival when combined with other chemotherapeutic drugs, such as dacarbazine, fludarabine, and cyclophosphamide, by increasing the sensitivity of those drugs.

Uses

Treatment of cancer and rheumatological diseases (an antisense oligonucleotide).

brand name

Genasense (Genta).

Clinical Use

Genta is developing a phosphorothioate antisense drug called oblimersen sodium that is complementary to the first six codons of the open reading frame of the human bcl-2 mRNA sequence. Oblimersen turns off production of the apoptosis inhibitor Bcl2 in tumor cells. This appears to increase a tumor cell's sensitivity to a variety of other anticancer therapies and, ultimately, may lead to cell death.

OBLIMERSEN SODIUM Preparation Products And Raw materials

Raw materials

Preparation Products

OBLIMERSEN SODIUM Suppliers

Global( 5)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
LGM Pharma	1-(800)-881-8210	inquiries@lgmpharma.com	United States	2127	70
TargetMol Chemicals Inc.	4008200310	marketing@tsbiochem.com	China	24018	58

Supplier	Advantage
LGM Pharma	70
TargetMol Chemicals Inc.	58

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OBLIMERSEN SODIUM Augmerosen Dna, D(p-thio)(T-C-T-C-C-C-A-G-C-G-T-G-C-G-C-C-A-T) Genasense Unii-sh55B0rq9k 190977-41-4