BIM-46068
BIM-46068 is a potent, selectively human brain Farnesyltransferase (FTase) inhibitor (IC50 = 91.4 nM). BIM-46068 can specifically inhibit Ras processing in MiaPaCa-2 cancer cells. BIM-46068 can be used for the study of pancreatic cancer.
For research use only. We do not sell to patients.
- CAS No.: 201487-53-8
- Formula: C21H42N4O3S3
- Molecular Weight:494.78
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
BIM-46068 (0.1-10 µM, 48 h) specifically inhibits the processing of Ras in MiaPaCa-2 cancer cells[1].
BIM-46068 (96 h) inhibits the growth of cells bearing the wild-type ras as well as cells with the different mutated ras (K-ras, N-ras, or H-ras) and effectively inhibits the multidrug-resistant cell line T24R[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MiaPaCa-2 cells
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Concentration:0.1 µM, 1 µM, 10 µM
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Incubation Time:48 h
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Result:Caused a change in the electrophoretic migration rate of H-Ras protein in MiaPaCa-2 cells, from rapid migration (farnesylated form) to slow migration (unfarnesylated form).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice were implanted s.c. with MiaPaCa-2 cells (5 × 106), a human pancreatic tumor cell line expressing mutated K-ras[1].
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Dosage:1 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:I.p., once daily for 10 days
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Result:Significantly reduced tumor growth in a dose-dependent manner.
On day 34 post-implantation, the mean tumor volume in the 30 mg/kg group was reduced by 50% compared to the control group.
Chemical Information
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CAS No. 201487-53-8
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Molecular Weight 494.78
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Formula C21H42N4O3S3
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SMILES
CSCC[C@@H](C(OC)=O)NC([C@H]1N(C[C@@H](NC[C@@H](N)CS)[C@@H](C)CC)CSC1(C)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)