GGTI-297
GGTI-297 is a geranylgeranyl transferase I (GGTase-1) inhibitor with IC50 values of 56 nM and 203 nM for GGTase-1 and fanesyl transferase (FTase), respectively. GGTI-297 inhibits the processing of the geranylgeranylated protein Rap1A without affecting the farnesylated protein H-Ras.
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- CAS No.: 181045-83-0
- Formule: C26H31N3O3S
- Masse moléculaire:465.61
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice injected (8 week old) with A-549 or Calu-1 cells[2]
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Dosage:70 mg/kg
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Administration:ip; once a day; for 5 weeks (A-549 cells) and 12 weeks (Calu-1)
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Result:Inhibited the growth in nude mice of A-549 and Calu-1 xenografts.
Chemical Information
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CAS No. 181045-83-0
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Masse moléculaire 465.61
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Formule C26H31N3O3S
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SMILES
CC(C)C[C@@H](C(O)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=C3C=CC=CC3=CC=C2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Y Qian, et al. Selective inhibition of type-I geranylgeranyltransferase in vitro and in whole cells by CAAL peptidomimetics. Bioorg Med Chem. 1998 Mar;6(3):293-9. [Content Brief]
[2]. J Sun, et al. Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts. Oncogene. 1998 Mar;16(11):1467-73. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)