MS140

Catalog No.S9880 Batch:S988001

Technical Data

Formula	C₃₉H₄₀N₁₀O₇
Molecular Weight	760.80	CAS No.	2229974-83-6
Solubility (25°C)*	In vitro	DMSO	10 mg/mL (13.14 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]

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]

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models 5–7-week-old female athymic Nude-Foxn1^nu mice Dosages 25 mg/kg, 30 mg/kg Administration IP

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

Animal Models
5–7-week-old female athymic Nude-Foxn1^nu mice
Dosages
25 mg/kg, 30 mg/kg
Administration
IP

References

[1] Xuewei Wu, et al. Nature Cancer volume 2, pages429–443 (2021)

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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