J 104871
J 104871 (J-104135) is a farnesyl pyrophosphate (FPP)-competitive farnesyltransferase (FTase) inhibitor. J 104871 inhibits rat brain FTase with an IC50 of 3.9 nM in the presence of farnesyl pyrophosphate (FPP).
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- CAS No.: 191088-19-4
- Formule: C38H32N2O12
- Masse moléculaire:708.67
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
In Vitro
J 104871 inhibits rat brain FTase with an IC50 of 3.9 nM in the presence of 0.6 μM farnesyl pyrophosphate (FPP), whereas it scarcely inhibits rat brain protein geranylgeranyltransferase-I or squalene synthase (SS)[1].
J 104871 also inhibits Ras processing in activated H-ras-transformed NIH3T3 cells with an IC50 value of 3.1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice (8 weeks old) injected activated H-ras-transformed NIH3T3 cells [1]
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Dosage:40 mg/kg, 80 mg/kg
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Administration:ip; once daily; 6 days
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Result:Suppressed tumor growth in nude mice transplanted with activated H-ras-transformed NIH3T3 cells.
Chemical Information
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CAS No. 191088-19-4
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Masse moléculaire 708.67
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Formule C38H32N2O12
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SMILES
O=C(C1(C(O)=O)O[C@H](C(N([C@H](C)[C@@H](C2=CC=C(OCO3)C3=C2)C/C=C/C4=NC5=CC=CC=C5O4)CC6=CC=C7C=CC=CC7=C6)=O)[C@H](C(O)=O)O1)O
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Synonyms
J-104135
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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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)