Cyclo(phg-isoDGR-k)-PEG4-non-cleavable-SAR405838
Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 is a dual MDM2 and α5β1 integrin modulator. Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 acts as an antiproliferative agent, apoptosis inducer and cell cycle regulator, induces reactivation of p53 and upregulation of p21, redistributes glioblastoma cells from the G0/G1 phase to the G2/M phase, and enhances apoptosis. Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 is applicable to the research of glioblastoma.
For research use only. We do not sell to patients.
- Formula: C75H104Cl2FN17O17
- Molecular Weight:1605.64
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
α5β1 |
In Vitro
Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 (Compound 1) potently inhibits the viability of U87-MG glioblastoma cells at 72 h, with an IC50 of 1.46 μM[1].
Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 (0.1-10.0 μM; 24 h) upregulates p53 and p21 in a dose-dependent manner[1].
Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 (10.0 μM; 24 h) induces cell cycle arrest at the G2/M phase and generates a high proportion of apoptotic cell population in the sub-G1 phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87-MG glioblastoma cells
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Concentration:0.1-10.0 μM
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Incubation Time:24 h
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Result:Induced a dose-dependent increase in p53 and p21 protein expression.
Markedly attenuated MDM2 induction at 3.0 μM compared to the reference MDM2 inhibitor.
Caused only a slight increment in MDM2 expression at 10.0 μM.
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Cell Line:U87-MG glioblastoma cells
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Concentration:10.0 μM
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Incubation Time:24 h
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Result:Drove prominent accumulation of cells in the G2/M phase (35.90%).
Caused a substantial increase in the sub-G1 (apoptotic) fraction (12.01%).
Reduced the G0/G1 phase fraction (41%) compared to control and reference treatments.
Chemical Information
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Molecular Weight 1605.64
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Formula C75H104Cl2FN17O17
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SMILES
O=C([C@H](N[C@H]1CC(C)(C)C)[C@H](C2=CC=CC(Cl)=C2F)[C@@]31C(NC4=C3C=CC(Cl)=C4)=O)N[C@H]5CC[C@H](OC(N(C)CCN(C)C(CCC6=CN(N=N6)CCOCCOCCOCCOCC(NCCCC[C@H](C(N[C@H](C7=CC=CC=C7)C(N[C@H](C(O)=O)C8)=O)=O)NC([C@H](CCCNC(N)=N)NC(CNC8=O)=O)=O)=O)=O)=O)CC5
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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)
Cyclo(phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 Related Classifications
HY-181606 Related Classifications
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