DT2216

Name: DT2216
Brand: MedChemExpress
SKU: HY-130604
Rating: 5.0 (1 reviews)

Cat. No.: HY-130604 Purity: 99.81%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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 (HY-10087), a linker, and a VHL E3 ubiquitin ligase (Red: Navitoclax; Blue: VHL ligand; Black: linker).

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

DT2216 Chemical Structure

CAS No. : 2365172-42-3

Size	Price	Stock	Quantity
5 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 560	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1120	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1790	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2900	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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

Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE DT2216

•Blood Adv. 2023 Sep 20;bloodadvances.2022008899. [Abstract]

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Bcl-2 Family Isoform Specific Products:

View All Isoforms

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

View All PROTACs Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

VHL

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]

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].

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.

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].

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.

Molecular Weight

1542.36

Formula

C₇₇H₉₆ClF₃N₁₀O₁₀S₄

CAS No.

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

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; 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)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Purity & Documentation

Purity: 99.97%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (246 KB) HNMR (266 KB) RP-HPLC (248 KB)

Handling Instructions (2659 KB)

References

[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

DT2216 Related Classifications

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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DT2216

Customer Review

DT2216 Related Antibodies

1 Publications Citing Use of MCE DT2216

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Bcl-2 Family Isoform Specific Products:

View All PROTACs Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

DT2216 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

DT2216 Related Classifications

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