ABT 263

Description In vitro

Product Name: ABT 263
CAS No.: 923564-51-6
Chemical Name: ABT 263
Synonyms: Navitoclax;Navitoclax (ABT-263);ABT 263;CS-1967;CS-1871;Navitoclax-D8;ABT263;ABT-263;Navitoclax, >=98%;ABT 263 USP/EP/BP;ABT-263,Navitoclax
CBNumber: CB21872884
Molecular Formula: C47H55ClF3N5O6S3
Formula Weight: 974.61
MOL File: 923564-51-6.mol

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ABT 263 Property

Melting point:: 114-116°C
Density: 1.41±0.1 g/cm3(Predicted)
storage temp.: -20°C Freezer, Under Inert Atmosphere
solubility: Soluble in DMSO (up to 25 mg/ml).
form: solid
pka: 4.60±0.10(Predicted)
color: White
Stability:: Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
InChIKey: JLYAXFNOILIKPP-KXQOOQHDSA-N
SMILES: C(NS(C1=CC=C(N[C@@H](CSC2=CC=CC=C2)CCN2CCOCC2)C(S(C(F)(F)F)(=O)=O)=C1)(=O)=O)(=O)C1=CC=C(N2CCN(CC3CC(C)(C)CCC=3C3=CC=C(Cl)C=C3)CC2)C=C1
CAS DataBase Reference: 923564-51-6

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Safety

HS Code: 29339900

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 11500
Product name: ABT-263
Purity: ≥98%
Packaging: 1mg
Price: $26
Updated: 2024/03/01

Cayman Chemical

Product number: 11500
Product name: ABT-263
Purity: ≥98%
Packaging: 5mg
Price: $59
Updated: 2024/03/01

Cayman Chemical

Product number: 11500
Product name: ABT-263
Purity: ≥98%
Packaging: 10mg
Price: $104
Updated: 2024/03/01

Cayman Chemical

Product number: 11500
Product name: ABT-263
Purity: ≥98%
Packaging: 25mg
Price: $195
Updated: 2024/03/01

TRC

Product number: A112500
Product name: ABT263
Packaging: 50mg
Price: $215
Updated: 2021/12/16

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ABT 263 Chemical Properties,Usage,Production

Description

ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2.

In vitro

ABT-263 is structurally related to ABT-737; it is a disruptor of Bcl-2/Bcl-xL interactions with pro-apoptotic proteins. Overexpression of the prosurvival Bcl-2 family members is commonly associated with tumor maintenance, progression, and chemoresistance. [1] ABT-263 displays the protection afforded by overexpression of Bcl-2 or Bcl-xL with EC50 values of 60 nM and 20 nM, respectively. A wide range of cellular activity is observed with ABT-263 having a 50% growth inhibition (EC50) of 110 nM against the most sensitive line (H146), whereas its activity in the least sensitive line (H82) results in an EC50 at 22 μM. All four cell lines with EC50 values of <400 nM (H146, H889, H1963, and H1417) are also highly sensitive to ABT-737, and the two most resistant lines (H1048 and H82) are similarly resistant to ABT-263.

Description

ABT-263 (923564-51-6) is a potent and selective Bcl-2 family inhibitor / BH3 domain mimetic which binds to Bcl-2, Bcl-xL?and Bcl-w (Ki<1 nM). A useful tool compound which has shown interesting results in various cancer clinical trials.2?Synergizes with deoxyglucose and other agents, inducing apoptosis in cancer cells in a xenograft mouse model.3?A novel senolytic agent, inducing apoptosis preferentially in senescent cells in a cell type-restricted manner.4

Chemical Properties

Pale Yellow Solid

Uses

ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤ 1 nM, respectively.

Uses

A novel inhibitor of antiapoptotic BCL-2 proteins; a new promising anticancer drug candidate.

Definition

ChEBI: Navitoclax is a N-sulfonylcarboxamide resulting from the formal condensation of the carboxy group of 4-{4-[(4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro[biphenyl]-2-yl)methyl]piperazin-1-yl}benzoic acid with the amino group of 4-{[(2R)-4-(morpholin-4-yl)-1-(phenylsulfanyl)butan-2-yl]amino}-3-[(trifluoromethyl)sulfonyl]benzenesulfonamide. It is a BH3-mimetic drug which targets the anti-apoptotic B-cell lymphoma-2 (BCL-2) family proteins, including BCL-2, BCL-xL, and BCL-w, and induces apoptosis in cancer cells. Currently under clinical investigation as treatment for solid tumors and hematologic malignancies. It has a role as a B-cell lymphoma 2 inhibitor, an apoptosis inducer and an antineoplastic agent. It is a member of piperazines, a member of monochlorobenzenes, a member of morpholines, an aryl sulfide, a N-sulfonylcarboxamide, a sulfone, an organofluorine compound, a secondary amino compound and a tertiary amino compound.

Mechanism of action

ABT‐263 exerts its senolytic activity in senescent tumor cells by inhibiting BCL‐XL's interaction with BAX. ABT‐263 is a BH3 mimetic that inhibits anti‐apoptotic BCL‐2 family proteins by impeding their ability to bind pro‐apoptotic proteins, such as BAK and BAX. BCL‐2 and BCL‐XL are the primary targets of ABT‐263 in cancer cells.

storage

Store at -20°C

References

1) Tse?et al.?(2008),?ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor; Cancer Res.,?68?3421 2) Vogler?et al.?(2009),?Bcl-2 inhibitors: small molecules with a big impact on cancer therapy; Cell Death Differ.,?16?360 3) Yamaguchi?et al.?(2011),?Efficient elimination of cancer cells by deoxyglucose-ABT-263/737 combination therapy; PLoS ONE,?6(9)?e24102 4) Zhu?et al.?(2016),?Identification of a novel senolytic agent, navitoclax, targeting the Bcl-2 family of anti-apoptotic factors; Aging Cell,?15?428

ABT 263 Preparation Products And Raw materials

Raw materials

Preparation Products

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ABT 263 Suppliers

Canada 1 China 210 China Hong Kong 1 India 4 United Kingdom 2 United States 23 Global 241

AdooQ BioScience, LLC

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View Lastest Price from ABT 263 manufacturers

Career Henan Chemical Co

Product: ABT 263 923564-51-6
Price: US $2.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: customise
Release date: 2018-08-09

923564-51-6, ABT 263Related Search:

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ABT263;ABT-263

4-[4-[[2-(4-chlorophenyl)-5,5-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-[[(2r)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide

CS-1871

CS-1967

(R)-4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(4-(4-morpholino-1-(phenylthio)butan-2-ylamino)-3-(trifluoromethylsulfonyl)phenylsulfonyl)benzamide

NAVITOCLAX;ABT 263;ABT263

(R)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide

4-[4-[[2-(4-Chlorophenyl)-5,5-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(4-morpholinyl)-1-[(phenylthio)methyl]propyl]amino]-3-[(trifluoromethyl)sulfonyl]phenyl]sulfonyl]benzamide

ABT 263

Navitoclax

BenzaMide, 4-(4-((2-(4-chlorophenyl)-5,5-diMe

Navitoclax (ABT-263)

Benzamide, 4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohexen-1-yl)methyl)-1-piperazinyl)-N-((4-(((1R)-3-(4-morpholinyl)-1-((phenylthio)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)-

ABT-263,Navitoclax

(S)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide

4-[4-[[2-(4-Chlorophenyl)-5,5-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(4-morpholinyl)-1-[(phenylthio)methyl]propyl]amino]-3-[(trifluoromethyl)sulfonyl]phenyl]sulfonyl]benzamide ABT-26

ABT 263 4-[4-[[2-(4-Chlorophenyl)-5,5-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(4-morpholinyl)-1-[(phenylthio)methyl]propyl]amino]-3-[(trifluoromethyl)sulfonyl]phenyl]sulfonyl]benzamide

Navitoclax, >=98%

(S)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperaz

(R)-4-(4-((2-(4-Chlorophenyl)-5,5-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(4-(4-morph

ABT 263, 98%, potent inhibitor of Bcl-xL,Bcl-2 and Bcl-w

(R)-4-[4-[[2-(4-Chlorophenyl)-5,5-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[4-[[3-morpholino-1-[(phenylthio)methyl]propyl]amino]-3-[(trifluoromethyl)sulfonyl]phenyl]sulfonyl]benzamide

ABT 263 USP/EP/BP

Navitoclax-D8

ABT-263(Navitoclax)/ABT263

(R)-4-(4-((4'-Chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide

923564-51-6

23564-51-6

C47H55ClF3N5O6S3

Inhibitor

Apis

Chiral Reagents

Inhibitors

Intermediates & Fine Chemicals

Pharmaceuticals

Sulfur & Selenium Compounds