MD-265

MD-265 : Degrader (PROTAC) of MDM2

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe MD-265 is in the process of SERP review.

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Information

MDM2

Degrader (PROTAC)

up to 100 nM
Reviewer recommended concentration: up to 30 nM

Probe Availability:

MedKoo

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): MD-265 was evaluated in a panel of acute leukemia cell lines. In each of these acute leukemia cell lines carrying a wild-type p53, MD-265 potently inhibited cell growth and achieved IC50 values of 0.9 nM to 212 nM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This probe is a very promising probe for MDM2 degradation with appropriate negative controls and would highly recommend using MD-265 between 10-50 nM for cellular in vitro assays and use in vivo via the i.v route in mice and rats at 10mg/kg and 5mg/kg respectively

(last updated: 28 Nov 2024 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This is a high quality chemical probe for investigating MDM2 function in cells and in vivo. One point of caution is a lack of proteome wide specificity evaluation and so off-targets and their contribution to phenotypes observed cannot be rule out.

(last updated: 3 Dec 2024 )