Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C22H25BrN4O2 |
| Molecular Weight | 457.364 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC2=NC=NC3=C2C=C1OCCCCCN(C)CC4=CC=C(Br)C=C4N3
InChI
InChIKey=JXDYOSVKVSQGJM-UHFFFAOYSA-N
InChI=1S/C22H25BrN4O2/c1-27-8-4-3-5-9-29-21-11-17-19(12-20(21)28-2)24-14-25-22(17)26-18-10-16(23)7-6-15(18)13-27/h6-7,10-12,14H,3-5,8-9,13H2,1-2H3,(H,24,25,26)
| Molecular Formula | C22H25BrN4O2 |
| Molecular Weight | 457.364 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:32:25 GMT 2023
by
admin
on
Sat Dec 16 11:32:25 GMT 2023
|
| Record UNII |
16720VER1H
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Code | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
CHEMBL3545133
Created by
admin on Sat Dec 16 11:32:25 GMT 2023 , Edited by admin on Sat Dec 16 11:32:25 GMT 2023
|
PRIMARY | |||
|
807640-87-5
Created by
admin on Sat Dec 16 11:32:25 GMT 2023 , Edited by admin on Sat Dec 16 11:32:25 GMT 2023
|
PRIMARY | |||
|
JNJ-26483327
Created by
admin on Sat Dec 16 11:32:25 GMT 2023 , Edited by admin on Sat Dec 16 11:32:25 GMT 2023
|
PRIMARY | |||
|
JNJ-26483327
Created by
admin on Sat Dec 16 11:32:25 GMT 2023 , Edited by admin on Sat Dec 16 11:32:25 GMT 2023
|
PRIMARY | Official Title: An Open-label, Phase I Study to Determine the Safety and Pharmacokinetics of JNJ-26483327, a Multi-targeted Kinase Inhibitor, Administered to Subjects With Advanced Stage and/or Refractory Solid MalignanciesDetailed Description:JNJ-26483327, a multi-targeted reversible kinase inhibitor, is a new drug in development for treatment of cancer. This study will test the safety (the effect on the body) of JNJ-26483327 and the highest dose of JNJ-26483327 that patients with advanced cancer can tolerate will be determined. Antitumor activity of JNJ-26481585 will be evaluated. | ||
|
11952856
Created by
admin on Sat Dec 16 11:32:25 GMT 2023 , Edited by admin on Sat Dec 16 11:32:25 GMT 2023
|
PRIMARY | |||
|
16720VER1H
Created by
admin on Sat Dec 16 11:32:25 GMT 2023 , Edited by admin on Sat Dec 16 11:32:25 GMT 2023
|
PRIMARY | |||
|
C77866
Created by
admin on Sat Dec 16 11:32:25 GMT 2023 , Edited by admin on Sat Dec 16 11:32:25 GMT 2023
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
ACTIVE MOIETY |
RESULTS: JNJ-26483327 was well tolerated in doses up to 1500 mg BID, with target-inhibition-related toxicity such as diarrhoea and skin rash, and other common reported toxicities being nausea, vomiting, anorexia and fatigue. At 2100 mg, two episodes of dose-limiting toxicity were observed, consisting of grade 3 anorexia and a combination of grade 3 anorexia and fatigue, respectively. Pharmacokinetics were dose proportional up to 1500 mg in which plasma levels were obtained showing anti-tumour activity in xenograft mouse models. Pharmacodynamic analysis did not show a substantial effect on expression of Ki-67, p27(kip1), phosphorylated mitogen-activated protein kinase, phosphorylated Akt and EGFR, and serum levels of sVEGFR-2, VEGF-C and VEGF-D remained unchanged. Stable disease was noted in six patients (32%).
|
||
|
ACTIVE MOIETY |
Class: Antineoplastic, Macrocyclic compound, Small molecule; Mechanism of Action: Epidermal growth factor receptor antagonist, Protein tyrosine kinase inhibitor, Src-Family kinase inhibitor, Vascular endothelial growth factor receptor 3 antagonist; Highest Development Phase: Phase I for Solid tumours; Most Recent Events: 14 Oct 2011 JNJ 26483327 licensed to BeiGene worldwide, 19 Nov 2009 Interim adverse events, pharmacokinetic and efficacy data from a phase I trial in Solid tumours presented at the 21st AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics (AACR-NCI-EORTC-2009), 31 Aug 2006 Phase I clinical trials in advanced and/or refractory solid tumours in the US (PO)
|
