DT2216 is a selective B-cell lymphoma extra large (BCL-XL) proteolysis-targeting chimera (PROTAC). DT2216 targets BCL-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.
In vivo, DT2216 (i.p.; 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.
|Solubility (25°C)||DMSO 20 mg/mL|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Cancer Discov. The PROTAC DT2216 Targets Cancer by Promoting BCL-X L Degradation
 Yonghan He, et al. J Hematol Oncol. DT2216-a Bcl-xL-specific degrader is highly active against Bcl-xL-dependent T cell lymphomas
 Sajid Khan, et al. Nat Med. A selective BCL-X L PROTAC degrader achieves safe and potent antitumor activity
|Related PROTAC Products|
dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on Cereblon ligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression.
Pomalidomide-PEG2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.
Thalidomide-NH-PEG3-propionic acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
U7D-1 is a first-in-class, potent and selective ubiquitin-specific protease 7 USP7 PROTAC depressant in RS4; The DC50 in 11 cells was 33 nM. U7D-1 has anti-cancer activity.
SR-1114 is a first-in-class PROTAC ENL depressant. SR-1114 in MV4; ENL degradation was observed in 11, MOLM-13 and OCI/AML-2 cells with DC50 values of 150 nM, 311 nM and 1.65 μM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.