Art. -Nr.: 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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Reinheit: 98.72%
CAS. Nr.: 2366132-45-6
Formel: C₅₅H₆₂N₁₀O₈
Molecular Weight:991.14

Speicherung:

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. Nr.: 2366132-45-6

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

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. Nr. 2366132-45-6
Appearance Solid
Molecular Weight 991.14
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
Handling Instructions (2659 KB)

Verweise

[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

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Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DD-03-171 Related Classifications

HY-122830 Related Classifications