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DT2216

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) [1].

Product Specifications

CAS Number

[2365172-42-3]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Bcl-2 Family; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/dt2216.html

Purity

99.97

Solubility

DMSO : 50 mg/mL (ultrasonic)

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

Molecular Formula

C77H96ClF3N10O10S4

Molecular Weight

1542.36

Precautions

H302, H315, H319, H335

References & Citations

[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.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C (Powder, stored under nitrogen)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

Von Hippel-Lindau (VHL)

Available Sizes

Curated Selection

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