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ABT-263

ABT-263 Structure
ABT-263 structure
CAS No.
923564-51-6
Chemical Name:
ABT-263
Synonyms
Navitoclax;Navitoclax (ABT-263);ABT 263;CS-1871;CS-1967;Navitoclax-D8;ABT263;ABT-263;Navitoclax, >=98%;ABT 263 USP/EP/BP;ABT-263,Navitoclax
CBNumber:
CB21872884
Molecular Formula:
C47H55ClF3N5O6S3
Molecular Weight:
974.61
MDL Number:
MFCD12756219
MOL File:
923564-51-6.mol
Last updated:2024-12-02 09:45:58
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ABT-263 Properties

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
NCI Dictionary of Cancer Terms ABT-263; navitoclax
FDA UNII XKJ5VVK2WD
NCI Drug Dictionary navitoclax

SAFETY

Risk and Safety Statements

HS Code  29339900

ABT-263 price More Price(32)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 11500 ABT-263 ≥98% 923564-51-6 1mg $26 2024-03-01 Buy
Cayman Chemical 11500 ABT-263 ≥98% 923564-51-6 5mg $59 2024-03-01 Buy
Cayman Chemical 11500 ABT-263 ≥98% 923564-51-6 10mg $104 2024-03-01 Buy
Cayman Chemical 11500 ABT-263 ≥98% 923564-51-6 25mg $195 2024-03-01 Buy
TRC A112500 ABT263 923564-51-6 50mg $215 2021-12-16 Buy
Product number Packaging Price Buy
11500 1mg $26 Buy
11500 5mg $59 Buy
11500 10mg $104 Buy
11500 25mg $195 Buy
A112500 50mg $215 Buy

ABT-263 Chemical Properties,Uses,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

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

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.

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. 

Pharmacokinetics

The pharmacokinetic profile of ABT-263 is characterized by low plasma clearance values and low volumes of distribution in mice, rats, dogs, and monkeys, with plasma elimination half-lives after i.v. Dose of 4.6 to 8.4 hours. Bioavailability after oral gavage was ～20% in all four species. Due to its low aqueous solubility, ABT-263 displays a prolonged dissolution rate-limited oral absorption. P.o. administration in lipid-based formulations, in which the compound is significantly more soluble, yields enhanced absorption with bioavailability near 50% and an oral elimination half-life of 8.9 hours in dogs[5].

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
[5] Tse, Christin et al. “Data from ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor.” 2023. 0.

ABT-263 Preparation Products And Raw materials

Raw materials

Preparation Products

ABT-263 Suppliers

Global( 252)Suppliers
Supplier Tel Email Country ProdList Advantage
Capot Chemical Co.,Ltd. 		+86-（0）57185586718 +86-13336195806 sales@capot.com China 29730 60
Henan Tianfu Chemical Co.,Ltd. 		+86-0371-55170693 +86-19937530512 info@tianfuchem.com China 21629 55
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 33024 60
career henan chemical co 		+86-0371-86658258 +8613203830695 sales@coreychem.com China 29860 58
TianYuan Pharmaceutical CO.,LTD 		+86-755-23284190 13684996853 sales@tianpharm.com CHINA 304 58
Biochempartner 		0086-13720134139 candy@biochempartner.com CHINA 965 58
Jinan Carbotang Biotech Co.,Ltd. 		+8615866703830 figo.gao@foxmail.com China 8497 58
Hubei xin bonus chemical co. LTD 		86-13657291602 linda@hubeijusheng.com CHINA 22963 58
BOC Sciences 		+1-631-485-4226 inquiry@bocsci.com United States 19552 58
Chongqing Chemdad Co., Ltd 		+86-023-6139-8061 +86-86-13650506873 sales@chemdad.com China 39894 58
Supplier Advantage
Capot Chemical Co.,Ltd. 		60
Henan Tianfu Chemical Co.,Ltd. 		55
ATK CHEMICAL COMPANY LIMITED 		60
career henan chemical co 		58
TianYuan Pharmaceutical CO.,LTD 		58
Biochempartner 		58
Jinan Carbotang Biotech Co.,Ltd. 		58
Hubei xin bonus chemical co. LTD 		58
BOC Sciences 		58
Chongqing Chemdad Co., Ltd 		58

Related articles

  • ABT-263
  • Navitoclax, also known as ABT-263 and ABT 263, is a potent, oral biologically active inhibitor of the Bcl-2 protein family, ac....
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View Lastest Price from ABT-263 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Navitoclax pictures 2024-11-18 Navitoclax
923564-51-6
 US $41.00-88.00 / mg 99.67% 10g TargetMol Chemicals Inc.
ABT 263 pictures 2019-07-06 ABT 263
923564-51-6
 US $2.00 / KG 1KG 99% customise Career Henan Chemical Co
  • Navitoclax pictures
  • Navitoclax
    923564-51-6
  • US $41.00-88.00 / mg
  • 99.67%
  • TargetMol Chemicals Inc.
  • ABT 263 pictures
  • ABT 263
    923564-51-6
  • US $2.00 / KG
  • 99%
  • Career Henan Chemical Co

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1of3

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 BenzaMide, 4-(4-((2-(4-chlorophenyl)-5,5-diMe 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 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 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 Navitoclax Navitoclax (ABT-263) ABT-263(Navitoclax)/ABT263 ABT-263, Bcl-2 family protein inhibitor Navitoclax, 10 mM in DMSO 923564-51-6 23564-51-6 C47H55ClF3N5O6S3 Inhibitor Apis Chiral Reagents Inhibitors Intermediates & Fine Chemicals Pharmaceuticals Sulfur & Selenium Compounds