1. Apoptosis Cytoskeleton
  2. MDM-2/p53 Integrin Apoptosis
  3. 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.

Cyclo(phg-isoDGR-k)-PEG4-non-cleavable-SAR405838

Cyclo(phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 Chemical Structure

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Description

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[1].

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.

Western Blot Analysis[1]

Cell Line: U87-MG glioblastoma cells
Concentration: 0.1-10.0 μM
Incubation Time: 24 h
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.

Cell Cycle Analysis[1]

Cell Line: U87-MG glioblastoma cells
Concentration: 10.0 μM
Incubation Time: 24 h
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.
Molecular Weight

1605.64

Formula

C75H104Cl2FN17O17

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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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Product Name:
Cyclo(phg-isoDGR-k)-PEG4-non-cleavable-SAR405838
Cat. No.:
HY-181606
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