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DD-03-171

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 ; Black: linker (HY-28875) ; Blue: Thalidomide-NH-CH2-COOH (HY-131717) )[2][3].

Product Specifications

CAS Number

2366132-45-6

UNSPSC

12352005

Hazard Statement

H301, H360

Target

Btk; NF-κB; PROTACs

Type

Reference compound

Related Pathways

NF-κB; PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/dd-03-171.html

Purity

98.72

Solubility

DMSO : 100 mg/mL (ultrasonic)

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

Molecular Formula

C55H62N10O8

Molecular Weight

991.14

Precautions

H301, H360

References & Citations

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

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

Cereblon

Available Sizes

Frequently Asked Questions

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