Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C38H47ClN4O4 |
| Molecular Weight | 659.257 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC2=C(C=C1OC(C)C)[C@@H](N(C(=O)C2)C3=CC=C(C=C3)N(C)C[C@H]4CC[C@@H](CC4)N5CCN(C)C(=O)C5)C6=CC=C(Cl)C=C6
InChI
InChIKey=CLRSLRWKONPSRQ-IIPSPAQQSA-N
InChI=1S/C38H47ClN4O4/c1-25(2)47-35-22-33-28(20-34(35)46-5)21-36(44)43(38(33)27-8-10-29(39)11-9-27)32-16-14-30(15-17-32)41(4)23-26-6-12-31(13-7-26)42-19-18-40(3)37(45)24-42/h8-11,14-17,20,22,25-26,31,38H,6-7,12-13,18-19,21,23-24H2,1-5H3/t26-,31-,38-/m0/s1
| Molecular Formula | C38H47ClN4O4 |
| Molecular Weight | 659.257 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 12:07:18 UTC 2023
by
admin
on
Sat Dec 16 12:07:18 UTC 2023
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| Record UNII |
4UF6MSL0ZH
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| Record Status |
Validated (UNII)
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| Record Version |
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Code | English |
| Code System | Code | Type | Description | ||
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300000041483
Created by
admin on Sat Dec 16 12:07:18 UTC 2023 , Edited by admin on Sat Dec 16 12:07:18 UTC 2023
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PRIMARY | |||
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1313363-54-0
Created by
admin on Sat Dec 16 12:07:18 UTC 2023 , Edited by admin on Sat Dec 16 12:07:18 UTC 2023
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CGM-097
Created by
admin on Sat Dec 16 12:07:18 UTC 2023 , Edited by admin on Sat Dec 16 12:07:18 UTC 2023
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PRIMARY | Biological Activity: CGM-097 is a potent and selective MDM2 inhibitor.An orally bioavailable HDM2 (human homolog of double minute 2) antagonist with potential antineoplastic activity. Upon oral administration, p53/HDM2 interaction inhibitor CGM097 inhibits the binding of the HDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. By preventing this HDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited, which may result in the restoration of p53 signaling and, thus, the p53-mediated induction of tumor cell apoptosis. HDM2, a zinc finger nuclear phosphoprotein, is a negative regulator of the p53 pathway, often overexpressed in cancer cells and has been implicated in cancer cell proliferation and survival. | ||
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4UF6MSL0ZH
Created by
admin on Sat Dec 16 12:07:18 UTC 2023 , Edited by admin on Sat Dec 16 12:07:18 UTC 2023
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PRIMARY | |||
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C104280
Created by
admin on Sat Dec 16 12:07:18 UTC 2023 , Edited by admin on Sat Dec 16 12:07:18 UTC 2023
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PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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TARGET -> INHIBITOR | |||
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TARGET -> INHIBITOR |
TR-FRET Biochemical Assay
IC50
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |
Originator: Novartis; Developer: Novartis Oncology; Class: Antineoplastic, Small molecule; Mechanism of Action: Proto-oncogene protein c mdm2 inhibitor, Tumour suppressor protein p53 inhibitor; Orphan Drug Status: No; On Fast track: No; New Molecular Entity: Yes; Highest Development Phase: No development reported for Solid tumours; Most Recent Events: 16 Jul 2016 No recent reports of development identified for phase-I development in Solid-tumours(Late-stage disease) in USA (PO), 16 Jul 2016 No recent reports of development identified for phase-I development in Solid-tumours(Late-stage disease) in Switzerland (PO), 16 Jul 2016 No recent reports of development identified for phase-I development in Solid-tumours(Late-stage disease) in Singapore (PO)
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