Drug General Information
Drug ID
D06ETI
Former ID
DCL000415
Drug Name
ABT-263
Synonyms
Navitoclax; ABT 263; S1001_Selleck; ABT263, Navitoclax; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-({(1R)-3-morpholin-4-yl-1-[(phenylsulfanyl)methyl]propyl}amino)-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)benzamide
Drug Type
Small molecular drug
Indication Advanced small cell lung cancer; Relapsed or refractory chronic lymphocytic leukemia; Lymphoid malignancies [ICD9: 140-229, 140-239, 162, 162.9, 202, 204.0, 204.1, 208.9; ICD10:C33-C34, C34.90, C81-C86, C91-C95, C91.0, C91.1] Phase 2 [543070], [551607]
Company
Roche; Genentech
Structure
Download
2D MOL

3D MOL

Formula
C47H55ClF3N5O6S3
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
InChIKey
JLYAXFNOILIKPP-KXQOOQHDSA-N
CAS Number
CAS 119229-65-1
PubChem Compound ID
PubChem Substance ID
Target and Pathway
Target(s) Apoptosis regulator Bcl-2 Target Info Inhibitor [536702], [536883], [551607]
Antiapoptotic protein BCL-XL Target Info Inhibitor [536702], [536883], [551607]
Bcl-2-like protein 2 Target Info Inhibitor [536702], [536883], [551607]
KEGG Pathway NF-kappa B signaling pathway
HIF-1 signaling pathway
Sphingolipid signaling pathway
Protein processing in endoplasmic reticulum
PI3K-Akt signaling pathway
Apoptosis
Adrenergic signaling in cardiomyocytes
Focal adhesion
Neurotrophin signaling pathway
Cholinergic synapse
Amyotrophic lateral sclerosis (ALS)
Toxoplasmosis
Tuberculosis
Hepatitis B
Epstein-Barr virus infection
Pathways in cancer
MicroRNAs in cancer
Colorectal cancer
Prostate cancer
Small cell lung cancerhsa04014:Ras signaling pathway
Jak-STAT signaling pathway
HTLV-I infection
Transcriptional misregulation in cancer
Pancreatic cancer
Chronic myeloid leukemia
Small cell lung cancerhsa05206:MicroRNAs in cancer
NetPath Pathway IL5 Signaling Pathway
TCR Signaling Pathway
IL2 Signaling Pathway
IL3 Signaling Pathway
Leptin Signaling Pathway
RANKL Signaling Pathway
TSLP Signaling PathwayNetPath_14:IL2 Signaling Pathway
TGF_beta_Receptor Signaling Pathway
Notch Signaling Pathway
PANTHER Pathway Apoptosis signaling pathway
Oxidative stress response
CCKR signaling map STP00006:Apoptosis signaling pathway
Pathway Interaction Database Role of Calcineurin-dependent NFAT signaling in lymphocytes
IL2-mediated signaling events
IL2 signaling events mediated by PI3K
Ceramide signaling pathway
Direct p53 effectors
RXR and RAR heterodimerization with other nuclear receptor
ATF-2 transcription factor network
C-MYB transcription factor network
HIV-1 Nef: Negative effector of Fas and TNF-alpha
Caspase Cascade in Apoptosis
Signaling events mediated by Stem cell factor receptor (c-Kit)
EPO signaling pathway
IL2 signaling events mediated by STAT5
Validated targets of C-MYC transcriptional repressionil2_pi3kpathway:IL2 signaling events mediated by PI3K
IL3-mediated signaling events
IL2 signaling events mediated by STAT5p53downstreampathway:Direct p53 effectors
Reactome Activation of BAD and translocation to mitochondria
BH3-only proteins associate with and inactivate anti-apoptotic BCL-2 members
The NLRP1 inflammasomeR-HSA-111453:BH3-only proteins associate with and inactivate anti-apoptotic BCL-2 members
The NLRP1 inflammasome
WikiPathways DNA Damage Response (only ATM dependent)
Senescence and Autophagy in Cancer
IL-2 Signaling Pathway
FAS pathway and Stress induction of HSP regulation
Focal Adhesion
Kit receptor signaling pathway
IL-3 Signaling Pathway
Nucleotide-binding domain, leucine rich repeat containing receptor (NLR) signaling pathways
Apoptosis
Nanoparticle triggered autophagic cell death
Amyotrophic lateral sclerosis (ALS)
Integrated Pancreatic Cancer Pathway
Corticotropin-releasing hormone
Interleukin-11 Signaling Pathway
Prostate Cancer
miR-targeted genes in muscle cell - TarBase
miR-targeted genes in lymphocytes - TarBase
miR-targeted genes in leukocytes - TarBase
Integrated Breast Cancer Pathway
Integrated Cancer pathway
Intrinsic Pathway for Apoptosis
Apoptosis Modulation and Signaling
TP53 Network
Influenza A virus infection
IL-5 Signaling PathwayWP364:IL-6 signaling pathway
TNF alpha Signaling Pathway
IL-7 Signaling Pathway
Leptin signaling pathway
Apoptosis Modulation and SignalingWP254:Apoptosis
References
Ref 543070(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8319).
Ref 551607Clinical pipeline report, company report or official report of Roche (2009).
Ref 536702ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer Res. 2008 May 1;68(9):3421-8.
Ref 536883ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo. Mol Cancer Ther. 2008 Oct;7(10):3265-74.
Ref 551607Clinical pipeline report, company report or official report of Roche (2009).

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