DT2216

Name: DT2216
Brand: MedChemExpress
SKU: HY-130604
Rating: 5.0 (2 reviews)

製品番号: HY-130604 純度: 99.93%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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. DT2216 is composed of the Bcl-2 family protein inhibitor Navitoclax-piperazine (HY-44432), a linker, and a VHL E3 ubiquitin ligase (Pink: Navitoclax-piperazine; Blue: VHL ligand; Black: linker).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。

CAS 番号 : 2365172-42-3

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 950	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 950	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$140	在庫あり	Estimated Time of Arrival: December 31
5 mg	$350	在庫あり	Estimated Time of Arrival: December 31
10 mg	$560	在庫あり	Estimated Time of Arrival: December 31
25 mg	$950	在庫あり	Estimated Time of Arrival: December 31
50 mg	$1420	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1980	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

顧客検証

Bio/Physico-chemical Assay

In Vivo Efficacy Study

Cell Proliferation/Viability Assay

Flow Cytometry

: 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.

: 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.

Bcl-2 Family アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]

VHL

Cellular Effect

Cell Line	Type	Value	Description	References
MOLT-4	IC₅₀	77.1 1 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]
MOLT-4	IC₅₀	77.1 1 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]
MOLT-4	IC₅₀	77.1 1 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]
RS4-11	IC₅₀	213 1 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]
NCI-H146	IC₅₀	278 1 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]
NCI-H146	IC₅₀	278 1 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]
NCI-H146	IC₅₀	278 1 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 1 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]
Platelet	IC₅₀	> 10000 1 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 1 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]
RS4-11	IC₅₀	213 1 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]
Platelet	IC₅₀	>10 3 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]

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

分子量

1542.36

分子式

C₇₇H₉₆ClF₃N₁₀O₁₀S₄

CAS 番号

2365172-42-3

Appearance

Solid

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)

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)

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

純度とドキュメンテーション

純度: 99.97%

Select Batch:

データシート (275 KB) SDS (394 KB)

COA (245 KB) HNMR (266 KB) RP-HPLC (248 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]

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 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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参考文献

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Molarity Calculator

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Complete Stock Solution Preparation Table

DT2216 Related Classifications

Molarity Calculator

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The molarity calculator equation

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おすすめ

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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

純度とドキュメンテーション

参考文献

カスタマーレビュー

DT2216 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

DT2216 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

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