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DT2216

SKU: orb2815834

Description

DT2216 is a VHL-recruiting PROTAC that selectively degrades BCL-XL. It demonstrates potent activity against BCL-XL-dependent leukemia and cancer cell lines in vitro and in vivo, while showing reduced on-target toxicity to platelets compared to traditional inhibitors.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number2365172-42-3
MW1542.36
Purity99.78%
FormulaC77H96ClF3N10O10S4
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
TargetApoptosis,PROTACs,Bcl-2 Family
SolubilityH2O:< 0.1 mg/mL (insoluble);DMSO:25 mg/mL (16.21 mM);10% DMSO+90% Corn Oil:2 mg/mL (1.3 mM)

Bioactivity

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.
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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Apoptosis, DT 2216, DT2216, DT-2216, PROTAC, VHL

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Key Properties

No computed properties available.

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Protocol Information

DT2216 (orb2815834)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
$ 120.00
5 mg
$ 330.00
10 mg
$ 510.00
25 mg
$ 970.00
50 mg
$ 1,520.00
100 mg
$ 2,420.00
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