Home Cell Cycle CDK inhibitor MS140 For research use only.

MS140

MS140 is a specific and highly potent CDK4/6 kinase inhibitor and also a CDK4/6 degrader (PROTAC).

MS140 Chemical Structure

MS140 Chemical Structure

CAS: 2229974-83-6

Purity & Quality Control

Batch: S988001 DMSO] 10 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.25%
99.25

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Biological Activity

Description MS140 is a specific and highly potent CDK4/6 kinase inhibitor and also a CDK4/6 degrader (PROTAC).
Targets
CDK4 [1] CDK6 [1]
In vitro
In vitro

MS140 potently and selectively both inhibits and degrades CDK4/6 kinases in CDK4/6i-S tumor cells by targeting them to the CRL4–CRBN–E3 ubiquitin complex.[1]
Cell Research Cell lines Colo205 cells
Concentrations 0.3 μM
Incubation Time 5 h
Method

Colo205 cells are treated with 0.3 µM MS140 or MS140-ve for 5 h in duplicate. Cell pellets are lysed in lysis buffer (8 M urea, 100 mM Tris-HCl pH 8.0). Sonication (5 s on, 5 s off; 2 × 30 s) is performed to shear genome DNA. Lysates are centrifuged for 30 min at 3,500g at 4 °C, and the supernatants are transferred to clean tubes. Protein concentration is determined (BCA assay), and protein is reduced with 5 mM dithiothreitol (DTT), alkylated with 15 mM iodoacetamide (IAA) in the dark, then diluted with 3× volume of 25 mM Tris (pH 8.0), 1 mM CaCl2. The final urea concentration is 2 M.
In Vivo
In vivo

Treatment of mice with MS140 promoted degradation of CDK4/6 kinases and suppression of RB–E2F output in JeKo-1 (MCL) and Colo25 (colorectal carcinoma) xenografts in vivo.[1]
Animal Research Animal Models 5–7-week-old female athymic Nude-Foxn1nu mice
Dosages 25 mg/kg, 30 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 760.80 Formula

C39H40N10O7
CAS No. 2229974-83-6 SDF --
Smiles CC(=O)C1=C(C)C2=C(N=C(NC3=NC=C(C=C3)N4CCN(CC4)C(=O)CNC5=CC=CC6=C5C(=O)N(C7CCC(=O)NC7=O)C6=O)N=C2)N(C8CCCC8)C1=O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 10 mg/mL ( (13.14 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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