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ABT 737

description Biological activity In vitro study In vivo studies Feature
ABT 737
ABT 737 structure
CAS No.
852808-04-9
Chemical Name:
ABT 737
Synonyms
ABT 737;ABT-737, >=98%;ABT737/ABT-737;Bcl-2 Inhibitor VI, ABT-737 - CAS 852808-04-9 - Calbiochem;4-{4-[(4'-Chlorobiphenyl-2-yl)Methyl]piperazin-1-yl}-N-[(4-{[(2R)-4-(diMethylaMino)-1-;BenzaMide, 4-[4-[(4'-chloro[1,1'-biphenyl]-2-yl)Methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(diMethylaMino)-1-[(phenylthio)Methyl]propyl]aMin;(R)-4-(4-((4'-chlorobiphenyl-2-yl)Methyl)piperazin-1-yl)-N-(4-(4-(diMethylaMino)-1-(phenylthio)butan-2-ylaMino)-3-nitrophenylsulfonyl)benzaMide;4-{4-[(4'-Chlorobiphenyl-2-yl)Methyl]piperazin-1-yl}-N-[(4-{[(2R)-4-(diMethylaMino)-1-(phenylsulfanyl)butan-2-yl]aMino}-3-nitrophenyl)sulfonyl]benzaMide;4-[4-[(4'-Chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]benzamide;BenzaMide, 4-[4-[(4'-chloro[1,1'-biphenyl]-2-yl)Methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(diMethylaMino)-1-[(phenylthio)Methyl]propyl]aMino]-3-nitrophenyl]sulfonyl]-
CBNumber:
CB51872885
Molecular Formula:
C42H45ClN6O5S2
Formula Weight:
813.43
MOL File:
852808-04-9.mol

ABT 737 Properties

Melting point:
152-154°C
storage temp. 
-20°C Freezer
form 
Yellow solid
SAFETY
  • Risk and Safety Statements
HS Code  29309090

ABT 737 price More Price(5)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich 197333 Bcl-2 Inhibitor VI, ABT-737 - CAS 852808-04-9 - Calbiochem
The Bcl-2 Inhibitor VI, ABT-737, also referenced under CAS 852808-04-9, controls the biological activity of Bcl-2. This small molecule/inhibitor is primarily used for Activators/Inducers applications.
852808-04-9 10mg $218 2018-11-23 Buy
Cayman Chemical 11501 ABT-737 ≥98% 852808-04-9 1mg $65 2018-11-13 Buy
Cayman Chemical 11501 ABT-737 ≥98% 852808-04-9 5mg $111 2018-11-13 Buy
Cayman Chemical 11501 ABT-737 ≥98% 852808-04-9 10mg $182 2018-11-13 Buy
Cayman Chemical 11501 ABT-737 ≥98% 852808-04-9 25mg $276 2018-11-13 Buy

ABT 737 Chemical Properties,Uses,Production

description

ABT-737 is a small-molecule inhibitor of the anti-apoptotic proteins Bcl-2, Bcl-X(L) and Bcl-w, with potential pro-apoptotic and antineoplastic activities,  with an affinity two to three orders of magnitude more potent than previously reported compounds but no affinity towards less homologous proteins, such as BCL-B, MCL-1, and A1. Mechanistic studies reveal that ABT-737 does not directly initiate the apoptotic process, but enhances the effects of death signals, displaying synergistic cytotoxicity with chemotherapeutics and radiation. ABT-737 exhibits single-agent-mechanism-based killing of cells from lymphoma and small-cell lung carcinoma lines, as well as primary patient-derived cells, and in animal models, ABT-737 improves survival, causes regression of established tumors, and produces cures in a high percentage of the mice. ABT-737 binds to Bcl-2, Bcl-xL and Bcl-w with very high affinities (Ki <1 nM) and also shows a very high specificity over Mcl-1 and A1.
ABT-737 induces apoptosis in MM cells, including those resistant to conventional therapy. Importantly, ABT-737 decreases the viability of bortezomib-, dexamethasone-(Dex) and thalidomide-refractory patient MM cells. Additionally, ABT-737 abrogates MM cell growth triggered by interleukin-6 or insulin-like growth factor-1. Mechanistic studies show that ABT-737-induced apoptosis is associated with activation of caspase-8, caspase-9 and caspase-3, followed by poly(ADP-ribose) polymerase cleavage.
ABT-737 has shown single-agent activity against lymphoma and small-cell lung cancer as well as substantial antimyeloma activity both in vitro and in vivo. In recent studies, acute myeloid leukemia blast, origenitor, and stem cells are effectively killed by ABT-737 with normal hematopoietic cells intact. The disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway could also be induced by ABT-737.

Biological activity

ABT-737 is a kind of BH3 mimic inhibitor, acting on Bcl-xL, Bcl-2 and Bcl-w, with the EC50 being 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays; However, it has no inhibitory effect on Mcl-1, Bcl-B and Bfl-1.
ABT737 up-regulates the expression of apoptosis-related gene Bim through JNK/c-Jun signaling pathway, and induce the apoptosis of Hela cells.
Use MTT assay to measure the inhibitory effect of ABT-737 on the growth of human cervical cancer Hela cells; apoptosis rate was detected by flow cytometry; the expression of JNK, phospho-JNK, c-Jun and phospho-c-Jun were detected by Western blot; the mRNA expression of Bim protein was detected by RT-PCR. The activity of JNK and c-Jun was inhibited by transiently transfect of the JNK-specific inhibitor SP600125 and siRNA.
ABT-737 can inhibit the growth of HeLa cells and induce HeLa cells to encounter apoptosis. ABT737 can activate the JNK kinase activity as well as its downstream target molecule c-Jun, further up-regulating the mRNA expression and protein expression of apoptosis-related gene Bim. ABT737-induced up-regulation of Bim and apoptosis were also blocked through inhibiting the activity or the expression of JNK or c-Jun by JNK-specific inhibitor SP600125 and siRNA targeting JNK and c-Jun.
This information is compiled and edited by Xiao Nan from Chemicalbook.

In vitro study

ABT-737 can reduce the amount of the BCL-2/BAX heterodimer while inducing the apoptosis of the HL60 cell, but have no inhibitory effect on the cell cycle distribution. ABT-737 can also induce the release of cytochrome c from mitochondria, promoting the conformational changes of BAX which was associated with apoptosis. In the leukemia model, ABT-737, at a dosage of 30 mg/kg, can block 53% of the leukemia load and significantly extend the lifespan of the mouse. ABT-737 does not lead to abnormal blood cell count and serum composition. It makes the resistant cells (Hela and MCF-7) be sensitive to ABT-737 through inactivating Mcl-1. ABT-737 can also cause the release of the BAX/BAK-dependent cytochrome c when Mcl-1 is not effective. ABT-737 can prolong the lifespan of BCL-2-bearing mice. ABT-737 is capable of replacing the BIM from the BCL2’s BH3 binding pocket, activating BAX through BIM, further inducing mitochondrial permeabilization and rapidly killing the chronic lymphocytic leukemia (CLL) cells. Noxa can positive modulates the sensitivity of H196 cells to ABT-737. ABT-737 is capable of inhibiting the proliferation of various kinds of SCLC cell lines, including NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, and induces apoptosis. Recent studies have shown that ABT-737 acts on ATLL cells and significantly induced HTLV-1-infected T cell apoptosis. ABT-737, when acting on ATLL mouse model at 100 mg/kg dose, shows strong anti-cancer activity.

In vivo studies

ABT-737, when acting on the leukemia model at a dose of 30 mg/kg, can inhibit the leukemia burden to up to 53%, and significantly prolong the life of the mouse. ABT-737 does not cause changes in blood cell count and plasma chemistry. ABT-737 can prolong the survival time of BCL-2-sensitized tumors. ABT-737 has a strong anti-cancer activity upon acting on the ATLL mouse model at a dose of 100 mg/kg.

Feature

ABT-737 is the first-generation small molecule inhibitors of the anti-apoptotic BCL-2 family protein.

Chemical Properties

Yellow Solid

Uses

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM, respectively.

Uses

A selective inhibitor of BCL-2, in small cell lung cancer. ABT-737 induced dramatic regressions in tumors derived from some SCLC cell lines.

ABT 737 Preparation Products And Raw materials

Raw materials

Preparation Products


ABT 737 Suppliers

Global( 119)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19918 60
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24191 60
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30001 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 969 58
Hubei xin bonus chemical co. LTD
86-13657291602
027-59338440 sales@guangaobio.com CHINA 23049 58
BOC Sciences
1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20115 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 35440 58
Alchem Pharmtech,Inc.
8485655694
sales@alchempharmtech.com United States 63729 58
Lancrix Chemicals 86-21-50817262
86-21-57712035 sales@lancrix.com China 1504 55
Shanghai Hanxiang Biotechnology Co. Ltd. 15971444841
amber@biochempartner.net China 5000 58

View Lastest Price from ABT 737 manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-08-20 ABT 737
852808-04-9
US $2.00 / KG 1KG 99% customsie career henan chemical co

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