DT2216
Based on 2 publication(s) in Google Scholar
DT2216 is a potent and selective BCL-XL (Bcl-2 family member) 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.
(Pink: Bcl-xL ligand (HY-44432); Blue: VHL ligand (HY-112078); Black: linker (HY-Y1139)).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.93%
- CAS No.: 2365172-42-3
- 화학식: C77H96ClF3N10O10S4
- 분자량:1542.36
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보관:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) DT2216
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Customer Validation & Images
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
All PROTACs Isoforms
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Biological Activity
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VHL |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLT-4 | IC50 |
77.1 nM
Compound: 1e; DT2216
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Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
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[PMID: 32145645] |
| NCI-H146 | IC50 |
278 nM
Compound: 1e; DT2216
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Antiproliferative activity against human NCI-H146 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
Antiproliferative activity against human NCI-H146 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
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[PMID: 32145645] |
| Platelet | IC50 |
>10000 nM
Compound: 1e; DT2216
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Toxicity in human platelet assessed as reduction in cell viability measured after 48 hrs by MTS assay
Toxicity in human platelet assessed as reduction in cell viability measured after 48 hrs by MTS assay
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[PMID: 32145645] |
| RS4-11 | IC50 |
213 nM
Compound: 1e; DT2216
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Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
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[PMID: 32145645] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLT-4 cells
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Concentration:62.5, 125 nM
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Incubation Time:72 hours
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Result:Killed MOLT-4 cells.
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Cell Line:MOLT-4 cells
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Concentration:0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:72 hours
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Result:Showed highly toxic to MOLT-4 cells with an EC50 of 0.052 μM.
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Cell Line:MOLT-4 cells
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Concentration:0.1, 0.3 μM
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Incubation Time:24 hours
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17/Icr-Prkdcscid/IcrIcoCrl (CB-17 SCID) mice aged 5-6 weeks[1]
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Dosage:7.5, 15 mg/kg
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Administration:i.p.; weekly for 60 days
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Result:Suppressed the growth of MOLT-4 T-ALL xenografts in mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2365172-42-3
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Appearance Solid
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분자량 1542.36
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화학식 C77H96ClF3N10O10S4
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Color White to light yellow
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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[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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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Blood Adv
Preclinical efficacy of tasquinimod-based combinations in advanced myeloproliferative neoplasms (MPN) in blastic phase. [Abstract]2025 Aug 19:bloodadvances.2025016898. PMID: 40829105
DT2216 purchased from MedChemExpress. Usage Cited in: Blood Adv. 2025 Aug 19:bloodadvances.2025016898. [Abstract]
Cotreatment with TQ and DT-2216 induced synergistic loss of viability in PD post-MPN sAML samples, with delta synergy scores >1.0 by the ZIP method at each concentration of the drugs.
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Blood Adv
CBFA2T3::GLIS2 Pediatric Acute Megakaryoblastic Leukemia is Sensitive to BCL-XL Inhibition by Navitoclax and DT2216. [Abstract]2024 Jan 9;8(1):112-129. PMID: 37729615
DT2216 purchased from MedChemExpress. Usage Cited in: Blood Adv. 2024 Jan 9;8(1):112-129. [Abstract]
Workflow of experimental procedures to assess the in vivo activity of navitoclax or DT2216 in CBFA2T3::GLS2 (mCG2-1) AMKL xenografts.
DT2216 purchased from MedChemExpress. Usage Cited in: Blood Adv. 2024 Jan 9;8(1):112-129. [Abstract]
Leukemic burden (GFP+hCD45+) was monitored by bleeding in mCG2-1 vehicle-treated mice vs DT2216 (15 mg/kg, ip, every 4 days)-treated mice.
DT2216 purchased from MedChemExpress. Usage Cited in: Blood Adv. 2024 Jan 9;8(1):112-129. [Abstract]
Percentage infiltration (% GFP+hCD45+) in the BM of mice that received xenotransplantation and that were treated was compared at the end point between matched Vehicle controls and mice either treated with DT2216 (15 mg/kg, ip, every 4 days) or navitoclax (Navito).
DT2216 purchased from MedChemExpress. Usage Cited in: Blood Adv. 2024 Jan 9;8(1):112-129. [Abstract]
Dose response curves and IC50 values were determined after incubation of AMKL or AML xenografts with DT2216 (0.001-10 μM; BCL-XL proteolysis-targeting chimera) or DMSO for 6 days, followed by viability readout with Cell-Titer Glo. Viability readout was normalized against DMSO for each sample.
DT2216 purchased from MedChemExpress. Usage Cited in: Blood Adv. 2024 Jan 9;8(1):112-129. [Abstract]
Amount of apoptosis assessed by annexin V staining and flow cytometry in AMKL xenografts or normal CB CD34+ cells after 72 hours of incubation with DT2216 at 100 nM or 1 μM in comparison with cells treated with DMSO.
용액&용해도
DMSO : 50 mg/mL (32.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (275 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.6484 mL | 3.2418 mL | 6.4836 mL | 16.2089 mL |
| 5 mM | 0.1297 mL | 0.6484 mL | 1.2967 mL | 3.2418 mL | |
| 10 mM | 0.0648 mL | 0.3242 mL | 0.6484 mL | 1.6209 mL | |
| 15 mM | 0.0432 mL | 0.2161 mL | 0.4322 mL | 1.0806 mL | |
| 20 mM | 0.0324 mL | 0.1621 mL | 0.3242 mL | 0.8104 mL | |
| 25 mM | 0.0259 mL | 0.1297 mL | 0.2593 mL | 0.6484 mL | |
| 30 mM | 0.0216 mL | 0.1081 mL | 0.2161 mL | 0.5403 mL |
DT2216 Related Classifications
HY-130604 Related Classifications
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