L-744832
L-744832 is a farnesyl transferase inhibitor. L-744832 effectively inhibits the farnesylation of H-Ras and N-Ras, but has little effect on K-Ras treatment. L-744832 not only directly targets the oncogenic pathway by inhibiting Ras farnesylation, but also enhances radiosensitivity by restoring TGF-β signaling through epigenetic reprogramming. L-744832 can induce cell cycle arrest and apoptosis. L-744832 can be used in combination therapy studies for Ras-driven tumors such as pancreatic cancer.
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- No. CAS: 160141-09-3
- Fòrmula: C26H45N3O6S2
- Peso molecular:559.78
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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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Chemical Information
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Actividad biológica
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H-Ras |
NRAS rG4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | IC50 |
78 μM
Compound: L-744832
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Anticancer activity against hormone-resistant human DU145 cells assessed as cell proliferation after 72 hrs by MTT assay
Anticancer activity against hormone-resistant human DU145 cells assessed as cell proliferation after 72 hrs by MTT assay
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[PMID: 21299244] |
| PC-3 | IC50 |
75 μM
Compound: L-744832
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Anticancer activity against hormone-resistant human PC3 cells assessed as cell proliferation after 72 hrs by MTT assay
Anticancer activity against hormone-resistant human PC3 cells assessed as cell proliferation after 72 hrs by MTT assay
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[PMID: 21299244] |
L-744832 (0.1-50 μM, 24-72 h) shows significant differences in sensitivity in Panc-1, Capan-2, BxPC-3, AsPC-1 and CFPAC-1 cells with IC50s of 1.3, 2.1, 12.3, 14.3 and > 50 μM[1].
L-744832 (0.1-50 μM, 72 h) arrest the sensitive cell lines (Panc-1, Capan-2, BxPC-3 and AsPC-1) in the G2/M phase of the cell cycle and the arrest occurs during the mitotic entry stage downstream of the G2/M checkpoint[1].
L-744832 (10 μM, 24-72 h) induces above five types of cell apoptosis, and the combination of radiotherapy can significantly increase the apoptosis rate of MIA PaCa-2 cells, while this effect is not observed in BxPC-3 cells[1][2].
L-744832 (0.1-10 μM) with ionizing radiation results in enhanced cytotoxicity in human pancreatic cancer cells[1].
L-744832 (5-10 μM) effectively inhibits the farnesylation of H-Ras and N-Ras and MIA PaCa-2 cells are more sensitive than BxPC-3 cells[2].
L-744832 (5-10 μM, 3-6 h) restores the expression of TGF-β type II receptor (RII) through regulating DNMT1, thereby re-establishing the tumor-suppressing function of TGF-β[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Panc-1, Capan-2, BxPC-3, AsPC-1 and CFPAC-1 cells
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Concentration:0.1, 0.5, 1, 10, 25 and 50 μM
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Incubation Time:72 h
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Result:Dose-dependent increased in G2/M phase accumulation and the proportion of G2/M phase cells in Panc-1 cells increased nearly threefold.
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Cell Line:Panc-1, Capan-2, BxPC-3, AsPC-1 and CFPAC-1 cells
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Concentration:10 μM
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Incubation Time:72 h
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Result:Showed chromatin condensation and nuclear fragmentation.
Increased the apoptotic index in each group, and this occurred in both wild-type p53 (Capan-2) cells and mutant p53 (Panc-1) cells.
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Cell Line:Panc-1, Capan-2, BxPC-3, AsPC-1 and CFPAC-1 cells
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Concentration:10 μM
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Incubation Time:72 h
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Result:Significantly increased the activity of Cyclin B1/Cdc2 kinase.
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Cell Line:MIA PaCa-2 cells
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Concentration:10 μM
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Incubation Time:3 and 6 h
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Result:Activated the RII promoter to increase its mRNA levels.
Reduced the mRNA levels of DNMT1.
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Cell Line:MIA PaCa-2 cells
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Concentration:10 μM
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Incubation Time:3 and 6 h
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Result:Activated the RII promoter to increase its protein levels.
Reduced the protein levels of DNMT1.
Chemical Information
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No. CAS 160141-09-3
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Peso molecular 559.78
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Fòrmula C26H45N3O6S2
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SMILES
O=C(OC(C)C)[C@@H](NC([C@@H](OC[C@@H](NC[C@@H](N)CS)[C@@H](C)CC)CC1=CC=CC=C1)=O)CCS(=O)(C)=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
[1]. Song SY, et al. K-Ras-independent effects of the farnesyl transferase inhibitor L-744,832 on cyclin B1/Cdc2 kinase activity, G2/M cell cycle progression and apoptosis in human pancreatic ductal adenocarcinoma cells. Neoplasia. 2000 May-Jun;2(3):261-72. [Content Brief]
[2]. Alcock RA, et al. Farnesyltransferase inhibitor (L-744,832) restores TGF-beta type II receptor expression and enhances radiation sensitivity in K-ras mutant pancreatic cancer cell line MIA PaCa-2. Oncogene. 2002 Nov 7;21(51):7883-90. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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