Description In vitro
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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

Lanzhou HuaHao Pharmaceutical Co., Ltd.
Tel
18189674620
Email
761137152@qq.com
Country
China
ProdList
489
Advantage
55
Guangzhou Isun Pharmaceutical Co., Ltd
Tel
020-39119399 18927568969
Fax
020-39119999
Email
isunpharm@qq.com
Country
China
ProdList
4428
Advantage
55
Zhengzhou HSH Science & Technology Co., Ltd.
Tel
0371-55932928 18937192232
Fax
0086-0371-55932928
Email
1282296214@qq.com
Country
China
ProdList
495
Advantage
55
Hunan Huayi Zhide Pharmaceutical Technology Co., Ltd.
Tel
17752881701
Email
190060276@qq.com
Country
China
ProdList
111
Advantage
58
TargetMol Chemicals Inc.
Tel
021-021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7783
Advantage
58
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ:65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
7267
Advantage
58
Shanghai Aladdin Biochemical Technology Co.,Ltd.
Tel
+86-18521732826
Email
market@aladdin-e.com
Country
China
ProdList
48461
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
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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:


  • 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