DT2216

Catalog No.S8924 Batch:S892402

Technical Data

Formula	C₇₇H₉₆ClF₃N₁₀O₁₀S₄
Molecular Weight	1542.36	CAS No.	2365172-42-3
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (64.83 mM)
		Ethanol	100 mg/mL (64.83 mM)
		Water	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

DT2216 is a potent and selective degrader of BCL-XL based on PROTAC technology. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.

Targets

BCL-XL ^[1]

In vitro

DT2216 is a BCL-XL proteolysis targeting chimera (PROTAC) that targets BCL-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation. DT2216 is more potent against various BCL-XL-dependent leukemia and cancer cells but significantly less toxic to platelets than ABT263 in vitro because VHL is poorly expressed in platelets.^[1]

In vivo

In vivo, DT2216 effectively inhibits the growth of several xenograft tumors as a single agent or in combination with other chemotherapeutic agents, without causing significant thrombocytopenia.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines MOLT-4, RS4;11, NCI-H146, MDA-MB-231, PC-3, HepG2, SW620, 786-O, WI-38, HEK 293T cells Concentrations 0.1 μM, 0.3 μM Incubation Time 24 h Method MOLT-4 cells are seeded in 60 mm dishes (2.5 × 10⁶ cells in 5 mL complete cell culture medium/dish), and then treated with indicated concentrations of DT2216 or ABT263 for 24 h. Cells are lysed in 1X cell lysis buffer by subjecting them to a freeze-thaw cycle in ice-ethanol bath or by 30 min incubation on ice.
Animal Study:^{^[1]}	Animal Models female 5–6 week-old CB-17 SCID, CB-17 SCID-beige, NOD-SCID mice Dosages 7.5 mg/kg, 15 mg/kg, 25 mg/kg Administration IP

Cell Assay:^{^[1]}

Cell lines
MOLT-4, RS4;11, NCI-H146, MDA-MB-231, PC-3, HepG2, SW620, 786-O, WI-38, HEK 293T cells
Concentrations
0.1 μM, 0.3 μM
Incubation Time
24 h
Method
MOLT-4 cells are seeded in 60 mm dishes (2.5 × 10⁶ cells in 5 mL complete cell culture medium/dish), and then treated with indicated concentrations of DT2216 or ABT263 for 24 h. Cells are lysed in 1X cell lysis buffer by subjecting them to a freeze-thaw cycle in ice-ethanol bath or by 30 min incubation on ice.

Animal Study:^{^[1]}

Animal Models
female 5–6 week-old CB-17 SCID, CB-17 SCID-beige, NOD-SCID mice
Dosages
7.5 mg/kg, 15 mg/kg, 25 mg/kg
Administration
IP

References

[1] Sajid Khan, et al. Nat Med. 2019 Dec;25(12):1938-1947.

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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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