Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C30H23N5O |
| Molecular Weight | 469.5365 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C(=O)N(C2=C1C=NC3=C2C=C(C=C3)C4=CC5=CC=CC=C5N=C4)C6=CC=C(C=C6)C(C)(C)C#N
InChI
InChIKey=JOGKUKXHTYWRGZ-UHFFFAOYSA-N
InChI=1S/C30H23N5O/c1-30(2,18-31)22-9-11-23(12-10-22)35-28-24-15-19(21-14-20-6-4-5-7-25(20)32-16-21)8-13-26(24)33-17-27(28)34(3)29(35)36/h4-17H,1-3H3
| Molecular Formula | C30H23N5O |
| Molecular Weight | 469.5365 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Dactolisib is a dual inhibitor of phosphatidylinositol 3-kinase (P13K) and the downstream mammalian target of rapamycin (mTOR) by binding to the ATP-binding cleft of these enzymes (inhibitor of PI3K/Akt/mTOR cascade). It is being investigated as a possible anti-cancer cancer agent and drug against Influenza virus infections. Frequently reported adverse events included nausea, vomiting, diarrhoea, fatigue/asthenia, anaemia, and anorexia.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. | 2008 Jul |
|
| Loss of Phosphatase and Tensin homologue deleted on chromosome 10 engages ErbB3 and insulin-like growth factor-I receptor signaling to promote antiestrogen resistance in breast cancer. | 2009 May 15 |
|
| Inhibition profiles of phosphatidylinositol 3-kinase inhibitors against PI3K superfamily and human cancer cell line panel JFCR39. | 2010 Apr |
|
| Dual targeting of phosphoinositide 3-kinase and mammalian target of rapamycin using NVP-BEZ235 as a novel therapeutic approach in human ovarian carcinoma. | 2011 Apr 15 |
|
| Identification of human triple-negative breast cancer subtypes and preclinical models for selection of targeted therapies. | 2011 Jul |
|
| A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations. | 2011 Jun |
|
| Comparison of the effects of the PI3K/mTOR inhibitors NVP-BEZ235 and GSK2126458 on tamoxifen-resistant breast cancer cells. | 2011 Jun 1 |
|
| The dual PI3K/mTOR inhibitor BEZ235 is effective in lung cancer cell lines. | 2011 Mar |
|
| Modulators of sensitivity and resistance to inhibition of PI3K identified in a pharmacogenomic screen of the NCI-60 human tumor cell line collection. | 2012 |
|
| The synergistic interaction of MEK and PI3K inhibitors is modulated by mTOR inhibition. | 2012 Apr 10 |
|
| Antitumor action of the MET tyrosine kinase inhibitor crizotinib (PF-02341066) in gastric cancer positive for MET amplification. | 2012 Jul |
|
| Phosphatidylinositol 3-kinase/Akt signaling pathway activates the WNK-OSR1/SPAK-NCC phosphorylation cascade in hyperinsulinemic db/db mice. | 2012 Oct |
|
| PI3Kδ inhibition augments the efficacy of rapamycin in suppressing proliferation of Epstein-Barr virus (EBV)+ B cell lymphomas. | 2013 Aug |
|
| Dual inhibitor of phosphoinositide 3-kinase/mammalian target of rapamycin NVP-BEZ235 effectively inhibits cisplatin-resistant urothelial cancer cell growth through autophagic flux. | 2013 Jul 18 |
|
| Preclinical evaluation of the mTOR-PI3K inhibitor BEZ235 in nasopharyngeal cancer models. | 2014 Feb 1 |
|
| Synergistic induction of cell death in haematological malignancies by combined phosphoinositide-3-kinase and BET bromodomain inhibition. | 2015 Jul |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Oct 21 23:24:09 UTC 2019
by
admin
on
Mon Oct 21 23:24:09 UTC 2019
|
| Record UNII |
RUJ6Z9Y0DT
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
NCI_THESAURUS |
C2152
Created by
admin on Mon Oct 21 23:24:09 UTC 2019 , Edited by admin on Mon Oct 21 23:24:09 UTC 2019
|
||
|
NCI_THESAURUS |
C129825
Created by
admin on Mon Oct 21 23:24:09 UTC 2019 , Edited by admin on Mon Oct 21 23:24:09 UTC 2019
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
C531198
Created by
admin on Mon Oct 21 23:24:09 UTC 2019 , Edited by admin on Mon Oct 21 23:24:09 UTC 2019
|
PRIMARY | |||
|
915019-65-7
Created by
admin on Mon Oct 21 23:24:09 UTC 2019 , Edited by admin on Mon Oct 21 23:24:09 UTC 2019
|
PRIMARY | |||
|
11977753
Created by
admin on Mon Oct 21 23:24:09 UTC 2019 , Edited by admin on Mon Oct 21 23:24:09 UTC 2019
|
PRIMARY | |||
|
9545
Created by
admin on Mon Oct 21 23:24:09 UTC 2019 , Edited by admin on Mon Oct 21 23:24:09 UTC 2019
|
PRIMARY | |||
|
BEZ235
Created by
admin on Mon Oct 21 23:24:09 UTC 2019 , Edited by admin on Mon Oct 21 23:24:09 UTC 2019
|
PRIMARY | |||
|
CHEMBL1879463
Created by
admin on Mon Oct 21 23:24:09 UTC 2019 , Edited by admin on Mon Oct 21 23:24:09 UTC 2019
|
PRIMARY | |||
|
915019-65-7
Created by
admin on Mon Oct 21 23:24:09 UTC 2019 , Edited by admin on Mon Oct 21 23:24:09 UTC 2019
|
PRIMARY | |||
|
SUB183868
Created by
admin on Mon Oct 21 23:24:09 UTC 2019 , Edited by admin on Mon Oct 21 23:24:09 UTC 2019
|
PRIMARY | |||
|
C74072
Created by
admin on Mon Oct 21 23:24:09 UTC 2019 , Edited by admin on Mon Oct 21 23:24:09 UTC 2019
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
TARGET -> INHIBITOR | |||
|
TARGET -> INHIBITOR | |||
|
TARGET -> INHIBITOR |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
ACTIVE MOIETY |
