Cat. No.: HY-122830

DD-03-171

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DD-03-171 is a PROTAC BTK degrader. DD-03-171 inhibits mantle cell lymphoma (MCL) cell proliferation (IC₅₀ = 5.1 nM) and prolongs the survival of mice bearing a lymphoma PDX model by degrading BTK, IKFZ1, and IKFZ3. DD-03-171 also inhibits platelet function and thrombosis. (Pink: BTK ligand 9 (HY-168292); Black: linker (HY-28875); Blue: Thalidomide-NH-CH2-COOH (HY-131717)).
(Pink: Btk ligand (HY-168292); Blue: Cereblon ligand (HY-131717); Black: linker).

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Pureté: 98.72%
CAS No.: 2366132-45-6
Formule: C₅₅H₆₂N₁₀O₈
Masse moléculaire:991.14

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

DD-03-171 Chemical Structure

CAS No.: 2366132-45-6

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Use of MCE Products

Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

DD-03-171 is a PROTAC BTK degrader. DD-03-171 inhibits mantle cell lymphoma (MCL) cell proliferation (IC₅₀ = 5.1 nM) and prolongs the survival of mice bearing a lymphoma PDX model by degrading BTK, IKFZ1, and IKFZ3. DD-03-171 also inhibits platelet function and thrombosis. (Pink: BTK ligand 9 (HY-168292); Black: linker (HY-28875); Blue: Thalidomide-NH-CH2-COOH (HY-131717))^[1]^[2]^[3]. (Pink: Btk ligand (HY-168292); Blue: Cereblon ligand (HY-131717); Black: linker).

IC₅₀ & Target^[1]^[2]^[3]

Cereblon

Voir tous les produits spécifiques à Isoform PROTACs :

Voir tous les produits spécifiques à Isoform NF-κB :

Cellular Effect

Cell Line	Type	Value	Description	References
TMD8	IC₅₀	5.1 nM Compound: DD-03-171	Cytotoxicity against human TMD8 cells incubated for 48 hrs by celltitre glo 2.0 assay Cytotoxicity against human TMD8 cells incubated for 48 hrs by celltitre glo 2.0 assay	[PMID: 37195170]

In Vitro

DD-03-171 (1-10000 nM, 2-4 h) reduces cellular BTK levels in a proteasome- and CRBN-dependent manner in Ramos B cells^[1].
DD-03-171 (40-1000 nM, 16 h) overcomes Ibrutinib (HY-10997) resistance and synergizes with HCK inhibition in ABC DLBCL in TMD8 ABC DLBCL cells^[1].
DD-03-171 (100-1000 nM, 16 h) degrades IKZF1/3 and BTK, has antiproliferative effects on MCL cells (ED₅₀ = 12 nM) DD-03-171 (0-20 μM, 4-20 h) concentration-dependent degrades BTK in human platelets^[2].

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

Western Blot Analysis^[1]

Cell Line:

Ramos B cells
Concentration:

1, 10, 100, 1000, 10000 nM
Incubation Time:

2, 4 h
Result:

Significantly reduced cellular BTK levels at concentrations as low as 100 nM, inhibited phosphorylation of Erk1/2.
Remained below levels even 24 hours after washout.

Western Blot Analysis^[1]

Cell Line:

TMD8 ABC DLBCL cells that expressed WT- or C481S-BTK
Concentration:

40, 200, 1000 nM
Incubation Time:

16 h
Result:

Induced BTK degradation of WT- and C481S-BTK.

Western Blot Analysis^[1]

Cell Line:

MCL cells
Concentration:

100, 500, 1000 nM
Incubation Time:

16 h
Result:

Degraded IKZF1/3 as well as BTK, reduced levels of active (phosphorylated) p65 NF-κB.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_last
Mice^[1]	10 mg/kg	i.p.	2.28 h	0.42 h	200 ng/mL	28219 min·ng/mL
Mice^[1]	2 mg/kg	i.v.	1.64 h	0.08 h	864 ng/mL	50662 min·ng/mL

In Vivo

DD-03-171 (50 mg/kg, i.p., once a day, 3 days) induces degradation of BTK in c57BL/6 mice and NSG mice were engrafted with DFBL-18689/DFBL-39435/DFBL-39435/DFBL-44685/DFBL-98848 cells^[1].

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

Animal Model:

C57BL/6 mice model^[1]
Dosage:

50 mg/kg
Administration:

i.p., once a day, 3 days
Result:

Induced significant degradation of BTK in splenocytes.

Animal Model:

NSG mice were engrafted with DFBL-18689/DFBL-39435/DFBL-39435/DFBL-44685/DFBL-98848 cells models^[1]
Dosage:

50 mg/kg
Administration:

i.p., once a day
Result:

Induced degradation of BTK.

Chemical Information

CAS No. 2366132-45-6
Appearance Solid
Masse moléculaire 991.14
Formule C₅₅H₆₂N₁₀O₈
Color White to yellow
SMILES

O=C(NC1=CC=CC(C(N=C2NC3=CC=C(C(N4CCN(CCCCCCNC(CNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O)CC4)=O)C=C3)=CN(C)C2=O)=C1C)C8=CC=C(C(C)(C)C)C=C8
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (100.89 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

1.0089 mL

5.0447 mL

10.0894 mL

5 mM

0.2018 mL

1.0089 mL

2.0179 mL

10 mM

0.1009 mL

0.5045 mL

1.0089 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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 (2.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 KB)
SDS (643 KB)
- English - EN (643 KB)
- Français - FR (643 KB)
- Deutsch - DE (643 KB)
- Norwegian - NO (643 KB)
- Español - ES (643 KB)
- Swedish - SV (643 KB)
- Italian - IT (643 KB)
- Korean - KR (643 KB)
- Portuguese - PT (643 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Instruction de manipulation (2659 KB)

Références

[1]. Dobrovolsky D, et al. Bruton tyrosine kinase degradation as a therapeutic strategy for cancer. Blood. 2019 Feb 28;133(9):952-961. [Content Brief]

[2]. Trory JS, et al. Chemical degradation of BTK/TEC as a novel approach to inhibit platelet function. Blood Adv. 2023 May 9;7(9):1692-1696. [Content Brief]

[3]. Lu X, et al. Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. J Med Chem. 2020 Oct 8;63(19):10726-10741. [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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	1.0089 mL	5.0447 mL	10.0894 mL	25.2235 mL
	5 mM	0.2018 mL	1.0089 mL	2.0179 mL	5.0447 mL
	10 mM	0.1009 mL	0.5045 mL	1.0089 mL	2.5223 mL
	15 mM	0.0673 mL	0.3363 mL	0.6726 mL	1.6816 mL
	20 mM	0.0504 mL	0.2522 mL	0.5045 mL	1.2612 mL
	25 mM	0.0404 mL	0.2018 mL	0.4036 mL	1.0089 mL
	30 mM	0.0336 mL	0.1682 mL	0.3363 mL	0.8408 mL
	40 mM	0.0252 mL	0.1261 mL	0.2522 mL	0.6306 mL
	50 mM	0.0202 mL	0.1009 mL	0.2018 mL	0.5045 mL
	60 mM	0.0168 mL	0.0841 mL	0.1682 mL	0.4204 mL
	80 mM	0.0126 mL	0.0631 mL	0.1261 mL	0.3153 mL
	100 mM	0.0101 mL	0.0504 mL	0.1009 mL	0.2522 mL

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DD-03-171

Immunology/Inflammation Compound Library

NF-κB Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

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Anti-Cardiovascular Disease Compound Library

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Anti-Obesity Compound Library

Transcription Factor-Targeted Library

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Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform PROTACs

Voir tous les produits spécifiques à Isoform NF-κB

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

DD-03-171 Related Classifications

HY-122830 Related Classifications