UA8967
UA8967 is a membrane-active antitumor agent. UA8967 exhibits enhanced cytotoxicity against cancer cells harboring a deletion of the tumor suppressor gene DPC4. By disrupting the integrity of the cytoplasmic membrane, UA8967 triggers early caspase-independent autophagy and ultimately leads to non-apoptotic cell lytic death. UA8967 can be used in research on colon cancer and pancreatic cancer.
For research use only. We do not sell to patients.
- CAS No.: 17511-50-1
- Formula: C20H23N3
- Molecular Weight:305.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HpDe6 | IC50 |
41.66 μM
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Cytotoxicity and growth inhibition against normal immortalized pancreatic epithelial HPDE-6 cells assessed by MTT assay after 72 h incubation.
Cytotoxicity and growth inhibition against normal immortalized pancreatic epithelial HPDE-6 cells assessed by MTT assay after 72 h incubation.
|
23179338 |
In Vitro
UA8967 (72 h) inhibits growth of MiaPaCa-2, Panc-1, BxPC3, CF-PAC1, AsPC1, T3M4, HCT-116 DPC4(+/+), HCT-116 DPC4(−/−), and HPDE-6 cells with IC50 values ranging from 12-61 μM after 72 h, with 4.75-fold greater potency in HCT-116 DPC4(−/−) cells compared to HCT-116 DPC4(+/+) cells[1].
UA8967 (72 h) does not selectively inhibit DNA, RNA, or protein synthesis in MiaPaCa-2 cells, with IC50 values of 40 μM, 40 μM, and 28 μM respectively after 72 h, matching its growth inhibitory potency[1].
UA8967 (0-50 μM; 24-72 h) causes a small accumulation of HCT-116 DPC4+/+ and HCT-116 DPC4−/− cells in G0/G1 phase and a reduction in S-phase cells after 24-48 h, with a more pronounced, dose-dependent S-phase reduction in HCT-116 DPC4−/− cells that persists at 72 h[1].
UA8967 (up to 100 μM; 24 h) induces less than 20% non-apoptotic, non-necrotic cell death in HCT-116 DPC4(+/+) and HCT-116 DPC4(−/−) cells at concentrations up to 100 μM after 24 h, with no caspase activation involved[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 DPC4(+/+) and HCT-116 DPC4(-/-)
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Concentration:5 μM, 25 μM, 50 μM (24-48 h); 2.5 μM, 5.0 μM, 10.0 μM (72 h)
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Incubation Time:24 h, 48 h, 72 h
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Result:Caused a small accumulation of cells in G0/G1 phase and a slight reduction in S-phase cells. The reduction in the percent of cells in S-phase was more pronounced and dose-dependent in the DPC4-deficient HCT-116(-/-) cell line.
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Cell Line:HCT-116 DPC4(+/+) and HCT-116 DPC4(-/-)
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Concentration:25 μM, 50 μM, 100 μM
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Incubation Time:24 h
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Result:Failed to cause significant necrotic or apoptotic cell death (both less than 20%).
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Cell Line:MiaPaCa-2, HCT-116 DPC4(+/+), HCT-116 DPC4(−/−)
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Concentration:50 μM
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Incubation Time:1, 2, 4, 8, 16, 24 h
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Result:Increased cleaved LC3 (LC3II, 14 kDa) in a dose- and time-dependent fashion across all tested cell lines.
Showed notable increase in cleaved LC3 as early as 1 h after exposure that continued up to 24 h.
Demonstrated more prominent increase in cleaved LC3 in HCT-116 DPC4(−/−) cells.
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Cell Line:MiaPaca-2 cells
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Concentration:100 μM
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Incubation Time:4 h
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Result:Induced the formation of autophagic vacuoles.
Chemical Information
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CAS No. 17511-50-1
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Molecular Weight 305.42
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Formula C20H23N3
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SMILES
C1(CN2CCN(CC2)CC3=CNC4=C3C=CC=C4)=CC=CC=C1
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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)