Details
Stereochemistry | ACHIRAL |
Molecular Formula | C24H23N5O2 |
Molecular Weight | 413.4717 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC2=C(C=CC=C2N1C3=NC(NCC4=CC=CC=C4)=C5COCCC5=N3)C(N)=O
InChI
InChIKey=RDALZZCKQFLGJP-UHFFFAOYSA-N
InChI=1S/C24H23N5O2/c1-15-12-18-17(22(25)30)8-5-9-21(18)29(15)24-27-20-10-11-31-14-19(20)23(28-24)26-13-16-6-3-2-4-7-16/h2-9,12H,10-11,13-14H2,1H3,(H2,25,30)(H,26,27,28)
Molecular Formula | C24H23N5O2 |
Molecular Weight | 413.4717 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/26565666Curator's Comment: Description was created based on several sources, including
http://www.fasebj.org/content/29/1_Supplement/LB137.short | https://www.ncbi.nlm.nih.gov/pubmed/26555175
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26565666
Curator's Comment: Description was created based on several sources, including
http://www.fasebj.org/content/29/1_Supplement/LB137.short | https://www.ncbi.nlm.nih.gov/pubmed/26555175
CB-5083 is a novel first in class, potent orally bio-available p97 inhibitor that disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models. CB-5083 causes rapid and sustained accumulation of poly-ubiquitin in tumor xenografts after a single administration. CB-5083 showed activity to inhibit tumor growth in multiple rodent models of human cancer. Furthermore, CB-5083 appears to exhibit greater potency over current proteasome inhibitors that further validate targeting p97 and protein homeostasis in the treatment of cancer. CB-5083 is a potent inhibitor of endoplasmic reticulum associated degradation and induces a lethal unfodled protein response. CB-5083 recently began Phase 1 testing in relapsed/refractory or refractory multiple myeloma, and advanced solid tumors.
Originator
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26565666
Mice: In mice bearing human HCT 116 colon tumor xenografts, CB-5083 (75 mg/kg, p.o.) significantly inhibits tumor growth. In mice bearing established human AMO-1 multiple myeloma and A549 lung carcinoma tumor xenografts, CB-5083 (100 mg/kg, p.o.) results in significant tumor growth inhibition.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26555175
CB-5083 (2.5 uM) induced CHOP protein in A549 cells
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:27:04 GMT 2023
by
admin
on
Sat Dec 16 09:27:04 GMT 2023
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Record UNII |
591IV6UL6J
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Record Status |
Validated (UNII)
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Record Version |
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-
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FDA ORPHAN DRUG |
483815
Created by
admin on Sat Dec 16 09:27:04 GMT 2023 , Edited by admin on Sat Dec 16 09:27:04 GMT 2023
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Code System | Code | Type | Description | ||
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591IV6UL6J
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C118287
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admin on Sat Dec 16 09:27:04 GMT 2023 , Edited by admin on Sat Dec 16 09:27:04 GMT 2023
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73051434
Created by
admin on Sat Dec 16 09:27:04 GMT 2023 , Edited by admin on Sat Dec 16 09:27:04 GMT 2023
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DTXSID801022542
Created by
admin on Sat Dec 16 09:27:04 GMT 2023 , Edited by admin on Sat Dec 16 09:27:04 GMT 2023
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1542705-92-9
Created by
admin on Sat Dec 16 09:27:04 GMT 2023 , Edited by admin on Sat Dec 16 09:27:04 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
IC50
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Related Record | Type | Details | ||
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ACTIVE MOIETY |