GS-9191
GS-9191 is the prodrug of the nucleotide analog PMEG. GS-9191 is a topical agent to permeate skin and be metabolized to the active nucleoside triphosphate analog in the epithelial layer. GS-9191 inhibits NA synthesis, arrests cell in S phase, and induces cell apoptosis. GS-9191 can be used for research of human papillomaviruses (HPV) infection.
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- No. CAS: 859209-84-0
- Fòrmula: C37H51N8O6P
- Peso molecular:734.82
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Ca-Ski | EC50 |
2.03 nM
Compound: GS-9191
|
Antiproliferative activity against HPV-transformed human CaSki cells after 7 days by SRB assay
Antiproliferative activity against HPV-transformed human CaSki cells after 7 days by SRB assay
|
[PMID: 19398642] |
| HeLa | EC50 |
0.71 nM
Compound: GS-9191
|
Antiproliferative activity against HPV-transformed human HeLa cells after 7 days by SRB assay
Antiproliferative activity against HPV-transformed human HeLa cells after 7 days by SRB assay
|
[PMID: 19398642] |
| HT-3 | EC50 |
5.42 nM
Compound: GS-9191
|
Antiproliferative activity against HPV-non-transformed human HT3 cells after 7 days by SRB assay
Antiproliferative activity against HPV-non-transformed human HT3 cells after 7 days by SRB assay
|
[PMID: 19398642] |
| ME-180 | EC50 |
1.83 nM
Compound: GS-9191
|
Antiproliferative activity against HPV-transformed human ME180 cells after 7 days by SRB assay
Antiproliferative activity against HPV-transformed human ME180 cells after 7 days by SRB assay
|
[PMID: 19398642] |
| SCC-4 | EC50 |
5.03 nM
Compound: GS-9191
|
Antiproliferative activity against HPV-non-transformed human SCC4 cells after 7 days by SRB assay
Antiproliferative activity against HPV-non-transformed human SCC4 cells after 7 days by SRB assay
|
[PMID: 19398642] |
| SCC-9 | EC50 |
15.3 nM
Compound: GS-9191
|
Antiproliferative activity against HPV-non-transformed human SCC9 cells after 7 days by SRB assay
Antiproliferative activity against HPV-non-transformed human SCC9 cells after 7 days by SRB assay
|
[PMID: 19398642] |
| SiHa | EC50 |
>74 nM
Compound: GS-9191
|
Inhibition of DNA synthesis in HPV-transformed human SiHa cells assessed as decrease in BrdU incorporation after 3 hrs by ELISA
Inhibition of DNA synthesis in HPV-transformed human SiHa cells assessed as decrease in BrdU incorporation after 3 hrs by ELISA
|
[PMID: 19398642] |
| SiHa | EC50 |
0.03 nM
Compound: GS-9191
|
Antiproliferative activity against HPV-transformed human SiHa cells after 7 days by SRB assay
Antiproliferative activity against HPV-transformed human SiHa cells after 7 days by SRB assay
|
[PMID: 19398642] |
| SiHa | EC50 |
1 nM
Compound: GS-9191
|
Inhibition of DNA synthesis in HPV-transformed human SiHa cells assessed as decrease in BrdU incorporation after 6 to 9 hrs by ELISA
Inhibition of DNA synthesis in HPV-transformed human SiHa cells assessed as decrease in BrdU incorporation after 6 to 9 hrs by ELISA
|
[PMID: 19398642] |
| SiHa | EC50 |
1.8 nM
Compound: GS-9191
|
Inhibition of DNA synthesis in HPV-transformed human SiHa cells assessed as decrease in BrdU incorporation after 24 to 27 hrs by ELISA
Inhibition of DNA synthesis in HPV-transformed human SiHa cells assessed as decrease in BrdU incorporation after 24 to 27 hrs by ELISA
|
[PMID: 19398642] |
| SiHa | EC50 |
11.5 nM
Compound: GS-9191
|
Inhibition of DNA synthesis in HPV-transformed human SiHa cells assessed as decrease in BrdU incorporation after 72 to 75 hrs by ELISA
Inhibition of DNA synthesis in HPV-transformed human SiHa cells assessed as decrease in BrdU incorporation after 72 to 75 hrs by ELISA
|
[PMID: 19398642] |
| SiHa | EC50 |
7.8 nM
Compound: GS-9191
|
Inhibition of DNA synthesis in HPV-transformed human SiHa cells assessed as decrease in BrdU incorporation after 3 to 6 hrs by ELISA
Inhibition of DNA synthesis in HPV-transformed human SiHa cells assessed as decrease in BrdU incorporation after 3 to 6 hrs by ELISA
|
[PMID: 19398642] |
| SiHa | EC50 |
7.9 nM
Compound: GS-9191
|
Inhibition of DNA synthesis in HPV-transformed human SiHa cells assessed as decrease in BrdU incorporation after 48 to 51 hrs by ELISA
Inhibition of DNA synthesis in HPV-transformed human SiHa cells assessed as decrease in BrdU incorporation after 48 to 51 hrs by ELISA
|
[PMID: 19398642] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 859209-84-0
-
Peso molecular 734.82
-
Fòrmula C37H51N8O6P
-
SMILES
CC(C)COC([C@H](CC1=CC=CC=C1)NP(COCCN2C3=NC(N)=NC(NC4CC4)=C3N=C2)(N[C@H](C(OCC(C)C)=O)CC5=CC=CC=C5)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)