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DT2216

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Catalog No. T13665Cas No. 2365172-42-3

DT2216 inhibits various Bcl-XL-dependent leukemias and cancer cells, but is significantly less toxic to platelets.DT2216 is a selective B-cell lymphoma, extremely large (BCL-XL), proteolytic targeting chimera (PROTAC).DT2216 targets bcl-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation.

DT2216

DT2216

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🥰Excellent
Purity: 99.78%
Catalog No. T13665Cas No. 2365172-42-3
DT2216 inhibits various Bcl-XL-dependent leukemias and cancer cells, but is significantly less toxic to platelets.DT2216 is a selective B-cell lymphoma, extremely large (BCL-XL), proteolytic targeting chimera (PROTAC).DT2216 targets bcl-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$67In StockIn Stock
5 mg$275In StockIn Stock
10 mg$440In StockIn Stock
25 mg$882In StockIn Stock
50 mg$1,400In StockIn Stock
100 mg$2,260In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.78%
Color:White
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Product Introduction

DT2216 AI Summary
DT2216 exhibits significant PROTAC activity targeting VHL/BCL-XL in human MOLT-4 cells, effectively inducing BCL-XL degradation with a DC50 of 53.0 nM and demonstrating 14.0% activity at 100 nM. It shows potent antiproliferative effects, with IC50 values of 77.1 nM in MOLT-4 cells, 213.0 nM in RS4-11 cells, and 278.0 nM in NCI-H146 cells. The compound displays low toxicity in human platelets, with an IC50 greater than 10,000 nM, and boasts a high selectivity index, as indicated by the IC50 ratio for human platelets to human MOLT-4 cells exceeding 130. Additionally, the compound's EC50 value of 63.0 nM and an Emax value of 90.8% reflect its high efficacy in promoting BCL-XL degradation..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
DT2216 inhibits various Bcl-XL-dependent leukemias and cancer cells, but is significantly less toxic to platelets.DT2216 is a selective B-cell lymphoma, extremely large (BCL-XL), proteolytic targeting chimera (PROTAC).DT2216 targets bcl-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation.
In vitro
DT2216 (0.1, 0.3 μM; 24 hours) kills MOLT-4 cells by caspase-3-mediated induction of apoptosis in a BCL-2 homologous antagonist killer (BAK)- and BCL-2-associated X protein (BAX)-dependent manner.DT2216 (62.5, 125 nM; 72?hours) kills MOLT-4 cells. DT2216 (0.001-10 μM; 72?hour) shows highly toxic to MOLT-4 cells with an EC50 of 0.052 μM.
In vivo
DT2216 (i.p.; 7.5, 15 mg/kg; weekly for 60 days) of 15 mg/kg is more effective at suppressing the growth of MOLT-4 T-ALL xenografts in mice than 7.5 mg/kg.
Chemical Properties
Molecular Weight1542.36
FormulaC77H96ClF3N10O10S4
Cas No.2365172-42-3
SmilesCC1(C)CCC(C2=CC=C(Cl)C=C2)=C(C1)CN3CCN(C4=CC=C(C(NS(=O)(C5=CC(S(C(F)(F)F)(=O)=O)=C(N[C@@H](CSC6=CC=CC=C6)CCN7CCN(C(CCCCCC(N[C@@H](C(C)(C)C)C(N8[C@@H](C[C@@H](O)C8)C(N[C@H](C9=CC=C(C%10=C(N=CS%10)C)C=C9)C)=O)=O)=O)=O)CC7)C=C5)=O)=O)C=C4)CC3
Relative Density.1.39 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 25 mg/mL (16.21 mM), Sonication is recommended.
H2O: < 0.1 mg/mL (insoluble)
In Vivo Formulation
10% DMSO+90% Corn Oil: 2 mg/mL (1.3 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.6484 mL3.2418 mL6.4836 mL32.4179 mL
5 mM0.1297 mL0.6484 mL1.2967 mL6.4836 mL
10 mM0.0648 mL0.3242 mL0.6484 mL3.2418 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 experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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