製品番号: HY-130604

DT2216

2 Cited Publications

カスタマーレビュー

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)).

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.93%
CAS 番号: 2365172-42-3
分子式: C₇₇H₉₆ClF₃N₁₀O₁₀S₄
分子量:1542.36

保管条件:

-20°C, stored under nitrogen

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

DT2216 構造式

CAS 番号: 2365172-42-3

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

MedChemExpress（MCE）の使用を引用している文献 DT2216

Customer Validation & Images

Bio/Physico-chemical AssayIn Vivo Efficacy StudyCell Proliferation/Viability AssayFlow Cytometry

Bio/Physico-chemical Assay
In Vivo Efficacy Study
In Vivo Efficacy Study
In Vivo Efficacy Study
Cell Proliferation/Viability Assay
Flow Cytometry

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (2)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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^[1]. (Pink: Bcl-xL ligand (HY-44432); Blue: VHL ligand (HY-112078); Black: linker (HY-Y1139)).

IC₅₀ & Target^[1]

VHL

Bcl-2 Family アイソフォーム固有の製品をすべて表示 :

PROTACs アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
MOLT-4	IC₅₀	77.1 nM Compound: 1e; DT2216	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	[PMID: 32145645]
NCI-H146	IC₅₀	278 nM Compound: 1e; DT2216	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	[PMID: 32145645]
Platelet	IC₅₀	>10000 nM Compound: 1e; DT2216	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	[PMID: 32145645]
RS4-11	IC₅₀	213 nM Compound: 1e; DT2216	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	[PMID: 32145645]

体外実験

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.

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.

体内実験

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].

MedChemExpress (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.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 2365172-42-3
性状 Solid
分子量 1542.36
分子式 C₇₇H₉₆ClF₃N₁₀O₁₀S₄
Color White to light yellow
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, stored under nitrogen

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

Publications (2)

All Bio/Physico-chemical AssayIn Vivo Efficacy StudyCell Proliferation/Viability AssayFlow Cytometry

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Journal Impact Factor

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.
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-X_L 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.

溶剤 & 溶解度

体外:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 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

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.

Protocol 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

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (275 KB)
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)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Khan S, et al. A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity. Nat Med. 2019 Dec;25(12):1938-1947. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

2 Cited Publications

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DT2216

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 DT2216

Bcl-2 Family アイソフォーム固有の製品をすべて表示

PROTACs アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (2)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

DT2216

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Mitochondria-Targeted Compound Library

Coagulation and Anti-coagulation Compound Library

PROTAC Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 DT2216

Bcl-2 Family アイソフォーム固有の製品をすべて表示

PROTACs アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (2)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

DT2216 関連分類

HY-130604 関連分類