1. PROTAC
    Apoptosis
  2. PROTAC
    Apoptosis
  3. DT2216

DT2216 

Cat. No.: HY-130604 Purity: 99.92%
Handling Instructions

DT2216 is a potent and selective BCL-XL degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. 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

Size Price Stock Quantity
1 mg USD 900 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1900 In-stock
Estimated Time of Arrival: December 31
10 mg USD 3300 In-stock
Estimated Time of Arrival: December 31
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Description

DT2216 is a potent and selective BCL-XL degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (16.21 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.6484 mL 3.2418 mL 6.4836 mL
5 mM 0.1297 mL 0.6484 mL 1.2967 mL
10 mM 0.0648 mL 0.3242 mL 0.6484 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (1.62 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (1.62 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (1.62 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.92%

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Keywords:

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

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DT2216
Cat. No.:
HY-130604
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