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ABT-263

CAS No.:
923564-51-6
Catalog Number:
AG0036XG
Molecular Formula:
C47H55ClF3N5O6S3
Molecular Weight:
974.6127
Pack Size
Purity
Availability
Location
Price(USD)
Quantity
  
1mg
≥98%
1 week
United States
$105
- +
5mg
99%
1 week
United States
$126
- +
10mg
99%
1 week
United States
$154
- +
50mg
99%
1 week
United States
$307
- +
100mg
99%
1 week
United States
$404
- +
Product Description
Catalog Number:
AG0036XG
Chemical Name:
ABT-263
CAS Number:
923564-51-6
Molecular Formula:
C47H55ClF3N5O6S3
Molecular Weight:
974.6127
MDL Number:
MFCD12756219
IUPAC Name:
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
InChI:
InChI=1S/C47H55ClF3N5O6S3/c1-46(2)20-18-42(34-8-12-37(48)13-9-34)36(31-46)32-55-22-24-56(25-23-55)39-14-10-35(11-15-39)45(57)53-65(60,61)41-16-17-43(44(30-41)64(58,59)47(49,50)51)52-38(19-21-54-26-28-62-29-27-54)33-63-40-6-4-3-5-7-40/h3-17,30,38,52H,18-29,31-33H2,1-2H3,(H,53,57)/t38-/m1/s1
InChI Key:
JLYAXFNOILIKPP-KXQOOQHDSA-N
SMILES:
Clc1ccc(cc1)C1=C(CN2CCN(CC2)c2ccc(cc2)C(=O)NS(=O)(=O)c2ccc(c(c2)S(=O)(=O)C(F)(F)F)N[C@@H](CSc2ccccc2)CCN2CCOCC2)CC(CC1)(C)C
UNII:
XKJ5VVK2WD
Properties
Complexity:
1800  
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
1  
Defined Bond Stereocenter Count:
0
Exact Mass:
973.296g/mol
Formal Charge:
0
Heavy Atom Count:
65  
Hydrogen Bond Acceptor Count:
14  
Hydrogen Bond Donor Count:
2  
Isotope Atom Count:
0
Molecular Weight:
974.611g/mol
Monoisotopic Mass:
973.296g/mol
Rotatable Bond Count:
16  
Topological Polar Surface Area:
170A^2
Undefined Atom Stereocenter Count:
0
Undefined Bond Stereocenter Count:
0
XLogP3:
9.6  
Literature
Title Journal
Human breast cancer cells display different sensitivities to ABT-263 based on the level of survivin. Toxicology in vitro : an international journal published in association with BIBRA 20180201
Discovery of new selective cytotoxic agents against Bcl-2 expressing cancer cells using ligand-based modeling. Chemico-biological interactions 20160425
Antioncogenic and Oncogenic Properties of Nrf2 in Arsenic-induced Carcinogenesis. The Journal of biological chemistry 20151106
Nrf2/p62 signaling in apoptosis resistance and its role in cadmium-induced carcinogenesis. The Journal of biological chemistry 20141010
Identification of potent Yes1 kinase inhibitors using a library screening approach. Bioorganic & medicinal chemistry letters 20130801
ABT-737 resistance in B-cells isolated from chronic lymphocytic leukemia patients and leukemia cell lines is overcome by the pleiotropic kinase inhibitor quercetin through Mcl-1 down-regulation. Biochemical pharmacology 20130401
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nature medicine 20130201
Bax and Bcl-xL exert their regulation on different sites of the ceramide channel. The Biochemical journal 20120701
Copy number aberrations of BCL2 and CDKN2A/B identified by array-CGH in thymic epithelial tumors. Cell death & disease 20120701
In vivo imaging of drug-induced mitochondrial outer membrane permeabilization at single-cell resolution. Cancer research 20120615
Bcl-2, Bcl-x(L), and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells. Blood 20120614
Phase II study of single-agent navitoclax (ABT-263) and biomarker correlates in patients with relapsed small cell lung cancer. Clinical cancer research : an official journal of the American Association for Cancer Research 20120601
Navitoclax (ABT-263) reduces Bcl-x(L)-mediated chemoresistance in ovarian cancer models. Molecular cancer therapeutics 20120401
ABT-263 sensitizes TRAIL-resistant hepatocarcinoma cells by downregulating the Bcl-2 family of anti-apoptotic protein. Cancer chemotherapy and pharmacology 20120301
WZ4002, a third-generation EGFR inhibitor, can overcome anoikis resistance in EGFR-mutant lung adenocarcinomas more efficiently than Src inhibitors. Laboratory investigation; a journal of technical methods and pathology 20120301
3'-deoxy-3'-18F-fluorothymidine PET/CT to guide therapy with epidermal growth factor receptor antagonists and Bcl-xL inhibitors in non-small cell lung cancer. Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20120301
Substantial susceptibility of chronic lymphocytic leukemia to BCL2 inhibition: results of a phase I study of navitoclax in patients with relapsed or refractory disease. Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20120210
Targeted therapy for chronic lymphocytic leukemia: a glimpse into the future. Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20120210
From mitochondrial biology to magic bullet: navitoclax disarms BCL-2 in chronic lymphocytic leukemia. Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20120210
A comprehensive strategy to discover inhibitors of the translesion synthesis DNA polymerase κ. PloS one 20120101
Identification of chemosensitivity nodes for vinblastine through small interfering RNA high-throughput screens. The Journal of pharmacology and experimental therapeutics 20111201
The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo. Molecular cancer therapeutics 20111201
Mcl-1 downregulation by YM155 contributes to its synergistic anti-tumor activities with ABT-263. Biochemical pharmacology 20111101
Mcl-1 levels need not be lowered for cells to be sensitized for ABT-263/737-induced apoptosis. Cell death & disease 20111101
Overcoming blocks in apoptosis with BH3-mimetic therapy in haematological malignancies. Pathology 20111001
Bcl-xL-inhibitory BH3 mimetics can induce a transient thrombocytopathy that undermines the hemostatic function of platelets. Blood 20110811
Bcl-2 is a better therapeutic target than c-Myc, but attacking both could be a more effective treatment strategy for B-cell lymphoma with concurrent Bcl-2 and c-Myc overexpression. Experimental hematology 20110801
Navitoclax (ABT-263) accelerates apoptosis during drug-induced mitotic arrest by antagonizing Bcl-xL. Cancer research 20110701
BCL2/BCL-X(L) inhibition induces apoptosis, disrupts cellular calcium homeostasis, and prevents platelet activation. Blood 20110630
Vorinostat-induced apoptosis in mantle cell lymphoma is mediated by acetylation of proapoptotic BH3-only gene promoters. Clinical cancer research : an official journal of the American Association for Cancer Research 20110615
The B-cell lymphoma 2 (BCL2)-inhibitors, ABT-737 and ABT-263, are substrates for P-glycoprotein. Biochemical and biophysical research communications 20110506
Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. Journal of medicinal chemistry 20110324
Navitoclax enhances the efficacy of taxanes in non-small cell lung cancer models. Clinical cancer research : an official journal of the American Association for Cancer Research 20110315
ABT-263, a Bcl-2 inhibitor, enhances the susceptibility of lung adenocarcinoma cells treated with Src inhibitors to anoikis. Oncology reports 20110301
Phase I study of Navitoclax (ABT-263), a novel Bcl-2 family inhibitor, in patients with small-cell lung cancer and other solid tumors. Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20110301
Survivin inhibition is critical for Bcl-2 inhibitor-induced apoptosis in hepatocellular carcinoma cells. PloS one 20110101
Efficient elimination of cancer cells by deoxyglucose-ABT-263/737 combination therapy. PloS one 20110101
Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity. The Lancet. Oncology 20101201
A microRNA screen to identify modulators of sensitivity to BCL2 inhibitor ABT-263 (navitoclax). Molecular cancer therapeutics 20101101
Teaching an old drug new tricks: Actinomycin D synergistically enhances sensitivity to the Bcl-2 antagonist ABT-737. Cancer biology & therapy 20101101
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. Journal of medicinal chemistry 20101014
The Bcl-2 inhibitor ABT-263 enhances the response of multiple chemotherapeutic regimens in hematologic tumors in vivo. Cancer chemotherapy and pharmacology 20101001
Drugs targeting Bcl-2 family members as an emerging strategy in cancer. Expert reviews in molecular medicine 20100908
Diminished sensitivity of chronic lymphocytic leukemia cells to ABT-737 and ABT-263 due to albumin binding in blood. Clinical cancer research : an official journal of the American Association for Cancer Research 20100815
Identification of expression signatures predictive of sensitivity to the Bcl-2 family member inhibitor ABT-263 in small cell lung carcinoma and leukemia/lymphoma cell lines. Molecular cancer therapeutics 20100301
Aileron staples peptides. Chemistry & biology 20090925
Update on developmental therapeutics for acute lymphoblastic leukemia. Current hematologic malignancy reports 20090701
Bcl-2 inhibitors: small molecules with a big impact on cancer therapy. Cell death and differentiation 20090301
Bcl-2 inhibitors: targeting mitochondrial apoptotic pathways in cancer therapy. Clinical cancer research : an official journal of the American Association for Cancer Research 20090215
Non-peptidic small molecule inhibitors against Bcl-2 for cancer therapy. Journal of cellular physiology 20090101
Mimicking the BH3 domain to kill cancer cells. Oncogene 20081201
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. Journal of medicinal chemistry 20081113
ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo. Molecular cancer therapeutics 20081001
Initial testing (stage 1) of the BH3 mimetic ABT-263 by the pediatric preclinical testing program. Pediatric blood & cancer 20080601
Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models. Clinical cancer research : an official journal of the American Association for Cancer Research 20080601
ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer research 20080501
A matter of life and death. Cancer cell 20020201
An informatics approach identifying markers of chemosensitivity in human cancer cell lines. Cancer research 20001101
Properties