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MS-8709

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Catalog No. T202458Cas No. 3060730-06-2
Alias MS8709, MS 8709

MS-8709 is a potent and selective G9a/GLP PROTAC Degrader with a DC50(G9a) of 274 nM and a DC50(GLP) of 260 nM. It induces G9a/GLP protein degradation in a concentration-dependent and time-dependent manner via the ubiquitin-proteasome system, without affecting mRNA expression levels. MS-8709 demonstrates superior cell growth inhibition compared to the parent compound UNC0642 in prostate cancer, leukemia, and lung cancer cell models, and exhibits mouse pharmacokinetic characteristics suitable for in vivo efficacy studies.

MS-8709

MS-8709

😃Good
Catalog No. T202458Alias MS8709, MS 8709Cas No. 3060730-06-2
MS-8709 is a potent and selective G9a/GLP PROTAC Degrader with a DC50(G9a) of 274 nM and a DC50(GLP) of 260 nM. It induces G9a/GLP protein degradation in a concentration-dependent and time-dependent manner via the ubiquitin-proteasome system, without affecting mRNA expression levels. MS-8709 demonstrates superior cell growth inhibition compared to the parent compound UNC0642 in prostate cancer, leukemia, and lung cancer cell models, and exhibits mouse pharmacokinetic characteristics suitable for in vivo efficacy studies.
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Product Introduction

Bioactivity
Description
MS-8709 is a potent and selective G9a/GLP PROTAC Degrader with a DC50(G9a) of 274 nM and a DC50(GLP) of 260 nM. It induces G9a/GLP protein degradation in a concentration-dependent and time-dependent manner via the ubiquitin-proteasome system, without affecting mRNA expression levels. MS-8709 demonstrates superior cell growth inhibition compared to the parent compound UNC0642 in prostate cancer, leukemia, and lung cancer cell models, and exhibits mouse pharmacokinetic characteristics suitable for in vivo efficacy studies.
In vitro
In separate cell proliferation assays involving 22Rv1, K562, and NCI-H1299 cell lines, MS-8709 displayed superior antiproliferative activity compared to the parent inhibitor UNC0642, yielding GI50 values ranging from 4.1 to 5 μM [1].
SynonymsMS8709, MS 8709
Chemical Properties
Molecular Weight1200.57
FormulaC64H95F2N11O7S
Cas No.3060730-06-2
SmilesN(C=1C2=C(N=C(N1)N3CCC(F)(F)CC3)C=C(OCCCN4CCCC4)C(OC)=C2)C5CCN(CCCC(NCCCCCCCCCCCC(N[C@H](C(=O)N6[C@H](C(NCC7=CC=C(C=C7)C8=C(C)N=CS8)=O)C[C@@H](O)C6)[C@@](C)(C)C)=O)=O)CC5
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 40 mg/mL (33.32 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.8329 mL4.1647 mL8.3294 mL41.6469 mL
5 mM0.1666 mL0.8329 mL1.6659 mL8.3294 mL
10 mM0.0833 mL0.4165 mL0.8329 mL4.1647 mL
20 mM0.0416 mL0.2082 mL0.4165 mL2.0823 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Stock solution preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (stock solution concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
The above example illustrates how to use "In Vivo Formulation Calculator" and does not represent a recommended formulation for any specific compound. Please select an appropriate dissolution method based on your experimental animals and route of administration.
All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.
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2 Enter the in vivo formulation:
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