Home Apoptosis Bcl-2 inhibitor - PROTAC inhibitor DT2216 For research use only.

DT2216

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.

DT2216 Chemical Structure

DT2216 Chemical Structure

CAS: 2365172-42-3

Purity & Quality Control

Batch: Purity: 99.82%
99.82

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Signaling Pathway

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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
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]
Cell Research 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.
In Vivo
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]
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04886622 Recruiting
Solid Tumor|Hematologic Malignancy
Dialectic Therapeutics Inc
 August 25 2021 Phase 1

Chemical Information & Solubility

Molecular Weight 1542.36 Formula

C77H96ClF3N10O10S4
CAS No. 2365172-42-3 SDF --
Storage (From the date of receipt) 3 years-20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (64.83 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : 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.

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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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