Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C20H22N4O3S.2ClH |
| Molecular Weight | 471.401 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.CNC(=O)C1=NC=CC(OC2=CC=C3N=C(N[C@@H]4CCCC[C@H]4O)SC3=C2)=C1
InChI
InChIKey=ZIHWHYXECXSBNA-LVVRIOTCSA-N
InChI=1S/C20H22N4O3S.2ClH/c1-21-19(26)16-10-13(8-9-22-16)27-12-6-7-15-18(11-12)28-20(24-15)23-14-4-2-3-5-17(14)25;;/h6-11,14,17,25H,2-5H2,1H3,(H,21,26)(H,23,24);2*1H/t14-,17-;;/m1../s1
| Molecular Formula | C20H22N4O3S |
| Molecular Weight | 398.479 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/24056773 | https://www.ncbi.nlm.nih.gov/pubmed/21653914
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/24056773 | https://www.ncbi.nlm.nih.gov/pubmed/21653914
BLZ 945, an orally active antagonist of the colony-stimulating factor1
receptor (CSF1R), is being developed by Novartis and Celgene Corporation for the treatment of advanced solid tumors and tumor-induced osteolytic lesions in bone and skeletal-related events. Phase I/II development for solid tumors is underway in the US, Italy, Spain, and Singapore. Preclinical trials were ongoing for tumor-induced osteolysis in Europe and the US. However, no recent reports of development had been identified for this indication.
CNS Activity
Originator
Approval Year
Sample Use Guides
Mice received 200 mg per kg body weight BLZ945 or vehicle (20% Captisol) by oral gavage once daily. BLZ945 was formulated in 20% Captisol at a concentration of 12.5 mg ml−1. Mice were dosed daily for 15 d, and tumor growth was monitored every 5 d by bioluminescence imaging.
Route of Administration:
Oral
Treatment of wild-type (WT) bone marrow–derived macrophages (BMDMs) with BLZ945 inhibited CSF-1–dependent prolifera¬tion (half-maximum effective concentration (EC50) = 67 nM) and decreased CSF-1R phosphorylation, similarly to blockade with CSF-1R–specific antibody. Primary bone marrow-derived macrophages (BMDMs) were cultured in the absence of CSF-1 for 12 hours prior to stimulation, followed by CSF-1 addition for the indicated time points (1.5, 3 and 5 minutes).
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 14:34:42 GMT 2023
by
admin
on
Sat Dec 16 14:34:42 GMT 2023
|
| Record UNII |
QJE0UTG9TS
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Code | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
C183175
Created by
admin on Sat Dec 16 14:34:42 GMT 2023 , Edited by admin on Sat Dec 16 14:34:42 GMT 2023
|
PRIMARY | |||
|
2222138-40-9
Created by
admin on Sat Dec 16 14:34:42 GMT 2023 , Edited by admin on Sat Dec 16 14:34:42 GMT 2023
|
PRIMARY | |||
|
138455086
Created by
admin on Sat Dec 16 14:34:42 GMT 2023 , Edited by admin on Sat Dec 16 14:34:42 GMT 2023
|
PRIMARY | |||
|
QJE0UTG9TS
Created by
admin on Sat Dec 16 14:34:42 GMT 2023 , Edited by admin on Sat Dec 16 14:34:42 GMT 2023
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
ACTIVATOR -> TARGET |
