Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C18H21IN6O2S |
| Molecular Weight | 509.37 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)NCCCN1C(SC2=C([124I])C=C3OCOC3=C2)=NC4=C(N)N=CN=C14
InChI
InChIKey=SUPVGFZUWFMATN-JVYRTNJDSA-N
InChI=1S/C18H21IN6O2S/c1-10(2)21-4-3-5-25-17-15(16(20)22-8-23-17)24-18(25)28-14-7-13-12(6-11(14)19)26-9-27-13/h6-8,10,21H,3-5,9H2,1-2H3,(H2,20,22,23)/i19-3
| Molecular Formula | C18H21IN6O2S |
| Molecular Weight | 509.37 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 19:44:24 UTC 2023
by
admin
on
Fri Dec 15 19:44:24 UTC 2023
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| Record UNII |
35RT31667F
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| Record Status |
Validated (UNII)
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| Record Version |
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-
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1352930-11-0
Created by
admin on Fri Dec 15 19:44:24 UTC 2023 , Edited by admin on Fri Dec 15 19:44:24 UTC 2023
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56643475
Created by
admin on Fri Dec 15 19:44:24 UTC 2023 , Edited by admin on Fri Dec 15 19:44:24 UTC 2023
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35RT31667F
Created by
admin on Fri Dec 15 19:44:24 UTC 2023 , Edited by admin on Fri Dec 15 19:44:24 UTC 2023
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PRIMARY |
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ACTIVE MOIETY |
Summary: This phase I trial studies the side effects and best dose of heat shock protein (HSP)90 inhibitor PU-H71 (PU-H71) in treating patients with cancer that has spread to other places in the body and usually cannot be cured or controlled with treatment. HSP90 inhibitor PU-H71 may stop the growth of cancer cells by blocking some of the enzymes needed for cell growth.
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ACTIVE MOIETY |
Originator: Memorial Sloan-Kettering Cancer Center; Developer: Memorial Sloan-Kettering Cancer Center, National Cancer Institute (USA), Samus Therapeutics; Class: Antineoplastic, Purine, Small molecule; Mechanism of Action: HSP90 heat-shock protein inhibitor; Orphan Drug Status: No
On Fast track: No; New Molecular Entity: Yes; Highest Development Phases: No development reported for Lymphoma, Non-Hodgkin's lymphoma, Solid tumours, Most Recent Events: 16 Jul 2016 No recent reports of development identified for phase-I development in Solid-tumours(Second-line therapy or greater) in USA (IV, Infusion), 16 Jul 2016 No recent reports of development identified for phase-I development in Solid-tumours(Late-stage disease, Metastatic disease) in USA (IV, Infusion), 16 Jul 2016 No recent reports of development identified for phase-I development in Non-Hodgkin's-lymphoma(Second-line therapy or greater) in USA (IV, Infusion)
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ACTIVE MOIETY |
PU-H71, a heat shock protein 90 (Hsp90) inhibitor, has yielded therapeutic efficacy in many preclinical models and is currently in clinical trials. Carbon-ion radiotherapy (CIRT) has provided successful tumor control, however, there is still room for improvement, particularly in terms of tumor-specific radiosensitization. The Hsp90 inhibitor PU-H71 has been shown to sensitize tumor cells to X-ray radiation. A murine osteosarcoma cell line (LM8) and a normal human fibroblast cell line (AG01522) were treated with PU-H71 before X-ray, 14- or 50-keV/undefinedm carbon-ion beam (C-ion) irradiation. Cell survival and protein expression were evaluated with colony formation and western blot, respectively. Treatment with PU-H71 alone was shown to be non-toxic to both cell lines, however, PU-H71 was shown to significantly sensitize LM8 cells to not only X-ray, but also to C-ion irradiation, while only a minimal sensitizing effect was observed in AG01522 cells. PU-H71 treatment was found to suppress the protein expression levels of Rad51 and Ku70, which are associated with the homologous recombination pathway and the non-homologous end-joining pathway of double-strand break repair. The findings reported here suggest that PU-H71 could be a promising radiosensitizer for CIRT.
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