1. PROTAC
    Apoptosis
  2. PROTAC
    Apoptosis
  3. DT2216

DT2216 

Cat. No.: HY-130604
Handling Instructions

DT2216 is a selective B-cell lymphoma extra large (BCL-XL) proteolysis-targeting chimera (PROTAC). DT2216 targets BCL-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.

For research use only. We do not sell to patients.

DT2216 Chemical Structure

DT2216 Chemical Structure

CAS No. : 2365172-42-3

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Description

DT2216 is a selective B-cell lymphoma extra large (BCL-XL) proteolysis-targeting chimera (PROTAC). DT2216 targets BCL-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets[1].

IC50 & Target[1]

VHL

 

In Vitro

DT2216 (62.5, 125 nM; 72 hours) kills MOLT-4 cells[1].
DT2216 (0.001-10 μM; 72 hour) shows highly toxic to MOLT-4 cells with an EC50 of 0.052 μM[1].
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[1].

Apoptosis Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 62.5, 125 nM
Incubation Time: 72 hours
Result: Killed MOLT-4 cells.

Cell Cytotoxicity Assay[1]

Cell Line: MOLT-4 cells
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Showed highly toxic to MOLT-4 cells with an EC50 of 0.052 μM.

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 0.1, 0.3 μM
Incubation Time: 24 hours
Result: Killed 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.
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[1].

Animal Model: CB17/Icr-Prkdcscid/IcrIcoCrl (CB-17 SCID) mice aged 5-6 weeks[1]
Dosage: 7.5, 15 mg/kg
Administration: i.p.; weekly for 60 days
Result: Suppressed the growth of MOLT-4 T-ALL xenografts in mice.
Molecular Weight

1542.36

Formula

C₇₇H₉₆ClF₃N₁₀O₁₀S₄

CAS No.

2365172-42-3

SMILES

CC1(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[[email protected]@H](CSC6=CC=CC=C6)CCN7CCN(C(CCCCCC(N[[email protected]@H](C(C)(C)C)C(N8[[email protected]@H](C[[email protected]@H](O)C8)C(N[[email protected]](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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

DT2216DT 2216DT-2216PROTACApoptosisProteolysis-targeting chimeraB-celllymphomaBCL-XLproteolysis-targetingchimeraVHLE3ligaseleukemiaplateletsInhibitorinhibitorinhibit

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