Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C96H129N21O20 |
| Molecular Weight | 1897.1802 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 16 / 16 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@](C)(O)[C@@H](NC(=O)[C@@H](CO)NC(=O)[C@H]1CCCN1C(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC2=CC=CC=C2)NC(=O)[C@@H](CC3=CC=CC=C3)NC(=O)[C@H](NC(=O)[C@@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](N)CC6=CNC7=C6C=CC=C7)[C@]([H])(C)O)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CC8=CNC9=C8C=CC=C9)C(=O)N[C@H](CCC(O)=O)C(=O)N[C@H](CCCNC(N)=N)C(=O)N[C@H](CCCCN)C(O)=O
InChI
InChIKey=FNQVICDIQNFNHD-NOQIVBDNSA-N
InChI=1S/C96H129N21O20/c1-52(2)41-71(85(126)110-74(46-59-49-103-66-31-17-14-28-62(59)66)88(129)106-69(36-37-79(121)122)84(125)105-68(34-21-39-101-96(99)100)83(124)107-70(95(136)137)33-19-20-38-97)111-92(133)81(55(6)120)116-90(131)77(51-118)114-91(132)78-35-22-40-117(78)94(135)76(42-53(3)4)113-87(128)72(43-56-23-9-7-10-24-56)109-86(127)73(44-57-25-11-8-12-26-57)112-93(134)80(54(5)119)115-89(130)75(47-60-50-104-67-32-18-15-29-63(60)67)108-82(123)64(98)45-58-48-102-65-30-16-13-27-61(58)65/h7-18,23-32,48-50,52-55,64,68-78,80-81,102-104,118-120H,19-22,33-47,51,97-98H2,1-6H3,(H,105,125)(H,106,129)(H,107,124)(H,108,123)(H,109,127)(H,110,126)(H,111,133)(H,112,134)(H,113,128)(H,114,132)(H,115,130)(H,116,131)(H,121,122)(H,136,137)(H4,99,100,101)/t54-,55-,64+,68+,69+,70+,71+,72+,73+,74+,75+,76+,77+,78+,80+,81+/m0/s1
| Molecular Formula | C96H129N21O20 |
| Molecular Weight | 1897.1802 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 16 / 16 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 12:03:29 UTC 2023
by
admin
on
Sat Dec 16 12:03:29 UTC 2023
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| Record UNII |
SR717JCM7M
|
| Record Status |
Validated (UNII)
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| Record Version |
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-
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Common Name | English | ||
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Systematic Name | English | ||
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Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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FDA ORPHAN DRUG |
331210
Created by
admin on Sat Dec 16 12:03:29 UTC 2023 , Edited by admin on Sat Dec 16 12:03:29 UTC 2023
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| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
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SR717JCM7M
Created by
admin on Sat Dec 16 12:03:29 UTC 2023 , Edited by admin on Sat Dec 16 12:03:29 UTC 2023
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PRIMARY | |||
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1311294-45-7
Created by
admin on Sat Dec 16 12:03:29 UTC 2023 , Edited by admin on Sat Dec 16 12:03:29 UTC 2023
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NO STRUCTURE GIVEN | |||
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145722610
Created by
admin on Sat Dec 16 12:03:29 UTC 2023 , Edited by admin on Sat Dec 16 12:03:29 UTC 2023
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PRIMARY | |||
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C103193
Created by
admin on Sat Dec 16 12:03:29 UTC 2023 , Edited by admin on Sat Dec 16 12:03:29 UTC 2023
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PRIMARY | NCIT | ||
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DB14786
Created by
admin on Sat Dec 16 12:03:29 UTC 2023 , Edited by admin on Sat Dec 16 12:03:29 UTC 2023
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PRIMARY | |||
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2120397-85-3
Created by
admin on Sat Dec 16 12:03:29 UTC 2023 , Edited by admin on Sat Dec 16 12:03:29 UTC 2023
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PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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TARGET -> ACTIVATOR |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |
Nerofe administered at doses up to 96 mg/m2 is safe, welltolerated
and demonstrates interesting anti-angiogenic activity
in combination with increased immune cytokines. Tumor T1/ST2
expression may be a biomarker for sensitivity to Nerofe.
Dose-escalation continues in this trial.
|
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ACTIVE MOIETY |
Official Title: A Phase 1, Open-Label, Dose-Escalation Study Evaluating the Safety, Pharmacokinetics, Pharmacodynamics, and Clinical Effects of Intravenously Administered Nerofe in Subjects With Advanced Malignancies
Purpose: This study will be the first to test the anti-cancer peptide Nerofe in humans. It will evaluate the safety, pharmacokinetic behavior, and pharmacodynamic and clinical effects of Nerofe given intravenously every other day to patients with advanced malignant disease.
|
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ACTIVE MOIETY |
Immunohistochemical studies localize Tumor-Cells Apoptosis Factor (TCApF) to the medulla and Hassal's corpuscles of the thymus gland, which are responsible for negative selection. Treatment of mice with induced AML terminates the cancer development and completely eliminates metastatic cell colonies from the bone marrow and the spleen that reduces probability of the cancer return. We find that TCApF binds to the T1/ST2 receptor and activates caspases 8, 9 and 3 mediated apoptosis, together with activation of JNKinase and p38 MAPKinase. Application of TCApF to cells induced apoptosis in acute myeloid leukemia proliferating cells (U937 premeyloid cells), in human breast carcinoma (MCF7), human glioblastoma, human neuroblastoma, human prostate cancer and human lung cancer proliferating cells. In contrast, TCApF was unable to induce apoptosis in non-proliferating cells.
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