1. Apoptosis Others
  2. MDM-2/p53 Drug Derivative
  3. RG7388-PEG3-Click-F

RG7388-PEG3-Click-F is a fluorinated analog of the MDM2 inhibitor RG7388 (HY-15676), with an IC50 of 16.8 nM against MDM2. [18F]RG7388-PEG3-Click-F exhibits high uptake and specificity in MDM2-expressing myeloma cells, and can be used for non-invasive assessment of MDM2 protein expression levels in tumors.

For research use only. We do not sell to patients.

RG7388-PEG3-Click-F

RG7388-PEG3-Click-F Chemical Structure

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Description

RG7388-PEG3-Click-F is a fluorinated analog of the MDM2 inhibitor RG7388 (HY-15676), with an IC50 of 16.8 nM against MDM2. [18F]RG7388-PEG3-Click-F exhibits high uptake and specificity in MDM2-expressing myeloma cells, and can be used for non-invasive assessment of MDM2 protein expression levels in tumors[1].

In Vitro

[18F]RG7388-PEG3-Click-F (18.5 kBq; 0.5-2 h) exhibits MDM2-specific uptake in U2OS osteosarcoma cells, and its uptake levels at incubation time points of 0.5 h, 1 h and 2 h are comparable to those in SJSA-1 cells[1].
[18F]RG7388-PEG3-Click-F binds specifically to SJSA-1 osteosarcoma cells, with an equilibrium dissociation constant (KD) of 100.9 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

18F]RG7388-PEG3-click-F (1.48 MBq; i.v.; single dose) exhibits hepatobiliary and renal clearance in healthy athymic mice, with minimal normal tissue retention by 3 h post-injection and no significant in vivo defluorination[1].
18F]RG7388-PEG3-click-F (7.03 MBq; i.v.; single dose) shows specific, time-stable uptake in SJSA-1 osteosarcoma xenografts in athymic mice, with measurable tumor-to-muscle contrast at 30 and 60 min post-injection[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

874.78

Formula

C42H48Cl2F3N7O6

SMILES

COC1=C(C=CC(C(NCCOCCOCCOCC2=CN(N=N2)CCF)=O)=C1)NC([C@@H]3N[C@H]([C@](C4=CC=C(C=C4F)Cl)([C@H]3C5=CC=CC(Cl)=C5F)C#N)CC(C)(C)C)=O

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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.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
RG7388-PEG3-Click-F
Cat. No.:
HY-182746
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