Drug Information

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
24978538
PubChem Substance ID
56311703, 56314453, 57304426, 57504587, 87219189, 87457108, 96099448, 99003698, 99245529, 99246089, 99431767, 99460835, 103640740, 104115920, 124756924, 124899202, 124899203, 125163731, 126583646, 126667000, 126724167, 131465096, 131465716, 134221945, 135263748, 135626669, 135727392, 136920253, 137126833, 141663047, 143499177, 152035716, 152164573, 152240012, 152258081, 152344157, 160646920, 162011689, 162037376, 162202714, 163123180, 163821637, 164194132, 164831796, 174007035, 174531509, 198955115, 204380851, 223388517, 223685382
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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