Details
Stereochemistry | ACHIRAL |
Molecular Formula | C26H29N3O3 |
Molecular Weight | 431.5268 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O=C(CC1=NC=C(C=C1)C2=CC=C(OCCN3CCOCC3)C=C2)NCC4=CC=CC=C4
InChI
InChIKey=HUNGUWOZPQBXGX-UHFFFAOYSA-N
InChI=1S/C26H29N3O3/c30-26(28-19-21-4-2-1-3-5-21)18-24-9-6-23(20-27-24)22-7-10-25(11-8-22)32-17-14-29-12-15-31-16-13-29/h1-11,20H,12-19H2,(H,28,30)
Molecular Formula | C26H29N3O3 |
Molecular Weight | 431.5268 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
KX-01 is a dual inhibitor of Src kinase and tubulin polymerization. KX01 promotes the induction of p53, G2/M arrest of proliferating cell populations and subsequent apoptosis via the stimulation of Caspase-3 and PARP cleavage. The drug was developed by Kinex Pharmaceuticals and reached phase II of clinical trials for the treatment of Castration-Resistant Prostate Cancer and Actinic Keratosis. KX-01 demonstrated good in vitro pofile against different cancer cell lines with IC50 in nanomolar range.
Originator
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro. | 2009 Jul |
|
Synthesis and pharmacological evaluation of thieno[2,3-b]pyridine derivatives as novel c-Src inhibitors. | 2011 Apr 15 |
|
KX-01, a novel Src kinase inhibitor directed toward the peptide substrate site, synergizes with tamoxifen in estrogen receptor α positive breast cancer. | 2012 Apr |
|
A phase I trial of KX2-391, a novel non-ATP competitive substrate-pocket- directed SRC inhibitor, in patients with advanced malignancies. | 2013 Aug |
Sample Use Guides
Patients recieve 40 mg of oral KX-01 twice-daily. Ointment form should be applied once daily.
Route of Administration:
Oral; Topical
Substance Class |
Chemical
Created
by
admin
on
Edited
Tue Oct 22 08:19:54 UTC 2019
by
admin
on
Tue Oct 22 08:19:54 UTC 2019
|
Record UNII |
4V9848RS5G
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Code | English |
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
CHEMBL571546
Created by
admin on Tue Oct 22 08:19:54 UTC 2019 , Edited by admin on Tue Oct 22 08:19:54 UTC 2019
|
PRIMARY | |||
|
897016-82-9
Created by
admin on Tue Oct 22 08:19:54 UTC 2019 , Edited by admin on Tue Oct 22 08:19:54 UTC 2019
|
PRIMARY | |||
|
23635314
Created by
admin on Tue Oct 22 08:19:54 UTC 2019 , Edited by admin on Tue Oct 22 08:19:54 UTC 2019
|
PRIMARY | |||
|
897016-82-9
Created by
admin on Tue Oct 22 08:19:54 UTC 2019 , Edited by admin on Tue Oct 22 08:19:54 UTC 2019
|
PRIMARY | |||
|
10864
Created by
admin on Tue Oct 22 08:19:54 UTC 2019 , Edited by admin on Tue Oct 22 08:19:54 UTC 2019
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
TARGET -> INHIBITOR |
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |